T0901317

目錄號: HY-10626 純度: 99.93%: FAQs
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摩爾計算器

T0901317 是口服有效且高度選擇性的 LXR 激動劑，對 LXRα 的 EC₅₀ 為 20 nM。T0901317 激活 FXR，EC₅₀ 為 5 μM。T0901317 是 RORα 和 RORγ 雙重反向激動劑，K_i 值分別為 132 nM 和 51 nM。T0901317 誘導(dǎo)細胞凋亡 (apoptosis)，并抑制低密度脂蛋白 (LDL) 受體缺失小鼠動脈粥樣硬化的發(fā)展。

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T0901317 Chemical Structure

CAS No. : 293754-55-9

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規(guī)格	價格	是否有貨
10 mM * 1 mL in DMSO	￥660	In-stock
5 mg	￥375	In-stock
10 mg	￥600	In-stock
50 mg	￥1200	In-stock
100 mg	￥1950	In-stock
200 mg		詢價
500 mg		詢價

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 28 篇科研文獻

•Nat Commun. 2024 Jul 21;15(1):6152. [Abstract]
•J Exp Clin Cancer Res. 2024 May 3;43(1):133. [Abstract]
•Cell Death Dis. 2024 Oct 18;15(10):754. [Abstract]
•J Med Chem. 2024 Oct 15. [Abstract]
•Ecotoxicol Environ Saf. 2023 Oct 19:266:115605. [Abstract]
•J Med Chem. 2022 Jan 21. [Abstract]
•Biol Res. 2019 Dec 17;52(1):60. [Abstract]
•Anal Chem. 2019 Jan 15;91(2):1501-1506. [Abstract]
•FASEB J. 2024 Jul 15;38(13):e23806. [Abstract]
•Food Chem Toxicol. 2024 May:187:114631. [Abstract]
•Eur J Med Chem. 2024 Mar 20:269:116344. [Abstract]
•Chem Biol Interact. 2024 Jan 6:110865. [Abstract]

•Chin Med. 2024 Jan 5;19(1):5. [Abstract]
•Cancers (Basel). 2023 Aug 16, 15(16), 4126.
•Neural Regen Res. 2023 Jun;18(6):1339-1346. [Abstract]
•Nutr Metab. 2022 Dec 6;19(1):80. [Abstract]
•Viruses. 2022, 14(3), 514.
•J Funct Foods. January 2022, 104901.
•Int Immunopharmacol. 2021 Nov 18;108373. [Abstract]
•J Cell Mol Med. 2021 May 5. [Abstract]
•Atherosclerosis. 2021 Apr 14.
•J Atheroscler Thromb. 2021 Feb 3. [Abstract]
•Curr Issues Mol Biol. 2024 Mar 13, 46(3), 2386-2397.
•Br J Nutr. 2021 Sep 24;1-27. [Abstract]
•Gastroent Res Pract. 2020 Apr 21;2020:1343969. [Abstract]
•Research Square Preprint. 2023 May 25.
•bioRxiv. 2023 Mar 10.
•Universitetet i Oslo. 2021 Jul.

T0901317 相關(guān)產(chǎn)品

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RORγ RORα RORβ

生物活性
純度 & 產(chǎn)品資料
參考文獻

生物活性

T0901317 is an orally active and highly selective LXR agonist with an EC₅₀ of 20 nM for LXRα^[1]. T0901317 activates FXR with an EC₅₀ of 5 μM^[2]. T0901317 is RORα and RORγ dual inverse agonist with K_i values of 132 nM and 51 nM, respectively^[3]. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice^[4]^[5].

IC₅₀ & Target

EC50: 20 nM (LXRα) and 5 μM (FXR)^[1]^[2]
Ki: 132 nM (RORα) and 51 nM (RORγ)^[3]

細胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CHO	EC₅₀	16 nM Compound: 1, T0901317	Agonist activity at human recombinant LXRbeta expressed in CHO cells assessed as effect on secreted alkaline phosphatase by LAFbeta assay Agonist activity at human recombinant LXRbeta expressed in CHO cells assessed as effect on secreted alkaline phosphatase by LAFbeta assay	[PMID: 19853462]
CHO	EC₅₀	16 nM Compound: 3, TO901317	Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay	[PMID: 17034119]
CHO-K1	EC₅₀	0.41 μM Compound: T0901317	Agonist activity at GAL4 fused LXRbeta-LBD (unknown origin) transfected in CHOK1 cells after 24 hrs by luciferase reporter gene assay Agonist activity at GAL4 fused LXRbeta-LBD (unknown origin) transfected in CHOK1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 27283790]
CHO-K1	EC₅₀	0.41 μM Compound: 1, T0901317	Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 25677664]
CHO-K1	EC₅₀	0.49 μM Compound: T0901317	Agonist activity at GAL4 fused LXRalpha (unknown origin) transfected in CHOK1 cells after 24 hrs by luciferase reporter gene assay Agonist activity at GAL4 fused LXRalpha (unknown origin) transfected in CHOK1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 27283790]
CHO-K1	EC₅₀	0.49 μM Compound: 1, T0901317	Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 25677664]
COS-7	EC₅₀	0.011 μM Compound: T0901317	Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay	[PMID: 17587573]
COS-7	EC₅₀	0.011 μM Compound: T0901317	Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay	[PMID: 17416521]
CV-1	EC₅₀	0.03 μM Compound: 1, T0901317	Agonist activity at human LXRalpha expressed in African green monkey kidney CV1 cells co-expressing pTAL-LXRE including LXR response element incubated for 20 hrs by luciferase reporter gene assay Agonist activity at human LXRalpha expressed in African green monkey kidney CV1 cells co-expressing pTAL-LXRE including LXR response element incubated for 20 hrs by luciferase reporter gene assay	[PMID: 26238323]
CV-1	EC₅₀	0.13 μM Compound: 1, T0901317	Agonist activity at human LXRbeta expressed in African green monkey kidney CV1 cells co-expressing pTAL-LXRE including LXR response element incubated for 20 hrs by luciferase reporter gene assay Agonist activity at human LXRbeta expressed in African green monkey kidney CV1 cells co-expressing pTAL-LXRE including LXR response element incubated for 20 hrs by luciferase reporter gene assay	[PMID: 26238323]
CV-1	EC₅₀	140 nM Compound: 1a, TO-091317	Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase reporter gene assay Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase reporter gene assay	[PMID: 25435151]
CV-1	EC₅₀	28 nM Compound: 1a, TO-091317	Transactivation of LXRalpha (unknown origin) expressed in CV1 cells by luciferase reporter gene assay Transactivation of LXRalpha (unknown origin) expressed in CV1 cells by luciferase reporter gene assay	[PMID: 25435151]
H4	EC₅₀	0.02 μM Compound: 1; TO-091317	Agonist activity at LXRbeta (unknown origin) expressed in human H4 cells co-expressing ABCA1 promoter measured after 48 hrs by cell-based transactivation assay Agonist activity at LXRbeta (unknown origin) expressed in human H4 cells co-expressing ABCA1 promoter measured after 48 hrs by cell-based transactivation assay	[PMID: 27011007]
H4	IC₅₀	4.5 μM Compound: 4, TO901317	Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as reduction of Amyloid beta-38 formation by LPECL assay Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as reduction of Amyloid beta-38 formation by LPECL assay	[PMID: 17723298]
HEK293	IC₅₀	> 20 μM Compound: T0901317	Inverse agonist activity at human ROR-alpha1 expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay Inverse agonist activity at human ROR-alpha1 expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 24702856]
HEK293	EC₅₀	0.036 μM Compound: 8, T0901317	Agonist activity at PXR (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at PXR (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	0.066 μM Compound: 3, T0901317	Agonist activity at human LXR-beta transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay Agonist activity at human LXR-beta transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 26288691]
HEK293	EC₅₀	0.09 μM Compound: 3, T1317	Transactivational agonist activity at human LXRbeta transfected in HEK293 cells expressing CMX-Gal4N assessed as luciferase activity after 16 hrs by reporter gene assay Transactivational agonist activity at human LXRbeta transfected in HEK293 cells expressing CMX-Gal4N assessed as luciferase activity after 16 hrs by reporter gene assay	[PMID: 22873709]
HEK293	EC₅₀	0.12 μM Compound: T0901317	Agonist activity at human LXR-beta expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay Agonist activity at human LXR-beta expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 24702856]
HEK293	EC₅₀	0.16 μM Compound: 8, T0901317	Agonist activity at LXRbeta (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at LXRbeta (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	0.21 μM Compound: 3, T0901317	Agonist activity at human LXR-alpha transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay Agonist activity at human LXR-alpha transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 26288691]
HEK293	EC₅₀	0.23 μM Compound: 5; T0901317	Agonist activity at human LXRbeta transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay Agonist activity at human LXRbeta transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 26905831]
HEK293	EC₅₀	0.27 μM Compound: 5; T0901317	Agonist activity at human PXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay Agonist activity at human PXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 26905831]
HEK293	EC₅₀	0.29 μM Compound: T0901317	Agonist activity at human LXR-alpha expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay Agonist activity at human LXR-alpha expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 24702856]
HEK293	EC₅₀	0.34 μM Compound: 3, T1317	Transactivational agonist activity at human LXRalpha transfected in HEK293 cells expressing CMX-Gal4N assessed as luciferase activity after 16 hrs by reporter gene assay Transactivational agonist activity at human LXRalpha transfected in HEK293 cells expressing CMX-Gal4N assessed as luciferase activity after 16 hrs by reporter gene assay	[PMID: 22873709]
HEK293	EC₅₀	0.37 μM Compound: 8, T0901317	Agonist activity at LXRalpha (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at LXRalpha (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	0.4 μM Compound: 5; T0901317	Agonist activity at human LXRalpha transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay Agonist activity at human LXRalpha transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 26905831]
HEK293	EC₅₀	0.46 μM Compound: 8, T0901317	Agonist activity at RoRc (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at RoRc (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	1.3 μM Compound: 8, T0901317	Agonist activity at FXR (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at FXR (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	IC₅₀	3 μM Compound: 5; T0901317	Inverse agonist activity at human RORgamma transfected in HEK293 cells after 24 hrs by beta galactosidase luciferase reporter gene assay Inverse agonist activity at human RORgamma transfected in HEK293 cells after 24 hrs by beta galactosidase luciferase reporter gene assay	[PMID: 26905831]
HEK293	EC₅₀	3.4 μM Compound: 5; T0901317	Agonist activity at human FXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay Agonist activity at human FXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 26905831]
HEK293	EC₅₀	5 μM Compound: 8, T0901317	Agonist activity at RoRa (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at RoRa (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	6 μM Compound: 8, T0901317	Agonist activity at RoRb (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at RoRb (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	IC₅₀	6.5 μM Compound: T0901317	Inverse agonist activity at human ROR-gamma1 expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay Inverse agonist activity at human ROR-gamma1 expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 24702856]
HEK293	EC₅₀	85 nM Compound: T0901317	Agonist activity at human LXRbeta expressed in HEK293 cells by luciferase reporter gene assay Agonist activity at human LXRbeta expressed in HEK293 cells by luciferase reporter gene assay	[PMID: 25305688]
HEK-293T	EC₅₀	0.036 μM Compound: 1, T0901317	Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	0.156 μM Compound: 1, T0901317	Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	0.25 μM Compound: T0901317	Agonist activity at GAL4-fused LXR alpha (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay Agonist activity at GAL4-fused LXR alpha (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay	10.1039/C3MD00005B
HEK-293T	EC₅₀	0.373 μM Compound: 1, T0901317	Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	0.463 μM Compound: 1, T0901317	Inverse agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Inverse agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	0.8 μM Compound: 4; T0901317	Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay	[PMID: 28169169]
HEK-293T	EC₅₀	0.94 μM Compound: 4; T0901317	Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay	[PMID: 28169169]
HEK-293T	EC₅₀	1 μM Compound: 1, T0901317	Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	IC₅₀	1.7 μM Compound: T0901317	Inverse agonist activity at GAL4-fused ROR gamma (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay Inverse agonist activity at GAL4-fused ROR gamma (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay	10.1039/C3MD00005B
HEK-293T	IC₅₀	2 μM Compound: T0901317	Inverse agonist activity at GAL4-fused ROR alpha (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay Inverse agonist activity at GAL4-fused ROR alpha (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay	10.1039/C3MD00005B
HEK-293T	EC₅₀	5 μM Compound: 1, T0901317	Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	6 μM Compound: 1, T0901317	Inverse agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Inverse agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HeLa	EC₅₀	17 nM Compound: 1a, TO-091317	Transactivation of LXR (unknown origin) expressed in human HeLa cells by ABCA1 LXREx3 reporter assay Transactivation of LXR (unknown origin) expressed in human HeLa cells by ABCA1 LXREx3 reporter assay	[PMID: 25435151]
HepG2	EC₅₀	0.02 μM Compound: 1; TO-091317	Agonist activity at LXRalpha (unknown origin) expressed in human HepG2 cells co-expressing ABCA1 promoter measured after 48 hrs by cell-based transactivation assay Agonist activity at LXRalpha (unknown origin) expressed in human HepG2 cells co-expressing ABCA1 promoter measured after 48 hrs by cell-based transactivation assay	[PMID: 27011007]
HepG2	EC₅₀	137 nM Compound: 3, TO901317	Effect on LXR-mediated intracellular triglyceride level in human HepG2 cells after 4 to 5 days Effect on LXR-mediated intracellular triglyceride level in human HepG2 cells after 4 to 5 days	[PMID: 18023179]
HepG2	EC₅₀	190 nM Compound: 6, GW3965	Agonist activity at Homo sapiens (human) LXRalpha expressed in HepG2 cells assessed as transactivation of CYP7A1 gene expression after 48 hr by luciferase reporter gene assay Agonist activity at Homo sapiens (human) LXRalpha expressed in HepG2 cells assessed as transactivation of CYP7A1 gene expression after 48 hr by luciferase reporter gene assay	10.1007/s00044-012-0359-5
Huh-7	EC₅₀	0.067 μM Compound: 3, TO901317	Induction of SREBP-1C mRNA expression in human HuH7 cells after 18 hrs by RT-PCR Induction of SREBP-1C mRNA expression in human HuH7 cells after 18 hrs by RT-PCR	[PMID: 19394832]
Huh-7	EC₅₀	0.135 μM Compound: 1, T0901317	Agonist activity at human Gal4-LBD fused LXRbeta LBD expressed in Huh7 cells by transient transactivation assay Agonist activity at human Gal4-LBD fused LXRbeta LBD expressed in Huh7 cells by transient transactivation assay	[PMID: 20005711]
Huh-7	EC₅₀	0.135 μM Compound: 3, TO901317	Agonist activity at human LXRalpha ligand binding domain (205-448) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay Agonist activity at human LXRalpha ligand binding domain (205-448) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay	[PMID: 19394832]
Huh-7	EC₅₀	0.14 μM Compound: 1a	Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 20350005]
Huh-7	EC₅₀	0.14 μM Compound: 1 (TO901317)	Agonist activity at human LXRalpha ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay Agonist activity at human LXRalpha ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay	[PMID: 19962892]
Huh-7	EC₅₀	0.14 μM Compound: 1, T0901317	Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 18973288]
Huh-7	EC₅₀	0.17 μM Compound: 1a	Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 20350005]
Huh-7	EC₅₀	0.17 μM Compound: 1, T0901317	Agonist activity at human Gal4-LBD fused LXRalpha LBD expressed in Huh7 cells by transient transactivation assay Agonist activity at human Gal4-LBD fused LXRalpha LBD expressed in Huh7 cells by transient transactivation assay	[PMID: 20005711]
Huh-7	EC₅₀	0.17 μM Compound: 1 (TO901317)	Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay	[PMID: 19962892]
Huh-7	EC₅₀	0.17 μM Compound: 1, T0901317	Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 18973288]
Huh-7	EC₅₀	0.178 μM Compound: 3, TO901317	Agonist activity at human LXRbeta ligand binding domain (219-462) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay Agonist activity at human LXRbeta ligand binding domain (219-462) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay	[PMID: 19394832]
Huh-7	EC₅₀	135 nM Compound: 3, TO901317	Agonist activity at human LXRalpha expressed in Huh7 cells by Gal4 transactivation assay Agonist activity at human LXRalpha expressed in Huh7 cells by Gal4 transactivation assay	[PMID: 18023179]
Huh-7	EC₅₀	170 nM Compound: 1, T0901317	Agonist activity at human recombinant LXRbeta ligand binding domain in HuH7 cells by Gal4 transactivation assay Agonist activity at human recombinant LXRbeta ligand binding domain in HuH7 cells by Gal4 transactivation assay	[PMID: 20382019]
Huh-7	EC₅₀	178 nM Compound: 3, TO901317	Agonist activity at human LXRbeta expressed in Huh7 cells by Gal4 transactivation assay Agonist activity at human LXRbeta expressed in Huh7 cells by Gal4 transactivation assay	[PMID: 18023179]
J774.A1	EC₅₀	0.034 μM Compound: 3, TO901317	Induction of ABCA1 mRNA expression in mouse J774A1 cells after 18 hrs by RT-PCR Induction of ABCA1 mRNA expression in mouse J774A1 cells after 18 hrs by RT-PCR	[PMID: 19394832]
L02	EC₅₀	0.53 μM Compound: TO901317	Transactivation of recombinant GAL4-fused human LXRalpha LBD (163 to 447 residues) expressed in human L02 cells measured after 24 hrs by luciferase reporter gene assay Transactivation of recombinant GAL4-fused human LXRalpha LBD (163 to 447 residues) expressed in human L02 cells measured after 24 hrs by luciferase reporter gene assay	[PMID: 31095389]
LS180	IC₅₀	> 50 μM Compound: 6; T0901317	Cytotoxicity against human LS180 cells assessed as effect on cell viability measured after 24 hrs by MTT assay Cytotoxicity against human LS180 cells assessed as effect on cell viability measured after 24 hrs by MTT assay	[PMID: 27497733]
PBMC	EC₅₀	> 20 μM Compound: 1, T0901317	Cytotoxicity against human PBMC assessed as effect on cell physiology after 48 hrs by CellTiter-Glo assay Cytotoxicity against human PBMC assessed as effect on cell physiology after 48 hrs by CellTiter-Glo assay	[PMID: 24239186]
PBMC	EC₅₀	> 20 μM Compound: 1, T0901317	Inhibition of IFNgamma production in human PBMC after 48 hrs by Sandwich ELISA Inhibition of IFNgamma production in human PBMC after 48 hrs by Sandwich ELISA	[PMID: 24239186]
PBMC	EC₅₀	3 μM Compound: 1, T0901317	Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA	[PMID: 24239186]
Platelet	IC₅₀	> 50 nM Compound: T0901317	Inhibition of collagen-induced platelet aggregation in human platelet suspension preincubated for 10 mins followed by collagen stimulation by light transmission-based assay Inhibition of collagen-induced platelet aggregation in human platelet suspension preincubated for 10 mins followed by collagen stimulation by light transmission-based assay	[PMID: 32463237]
SH-SY5Y	IC₅₀	> 50 μM Compound: 6; T0901317	Cytotoxicity against human SH-SY5Y cells assessed as effect on cell viability measured after 24 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as effect on cell viability measured after 24 hrs by MTT assay	[PMID: 27497733]
SH-SY5Y	EC₅₀	0.075 μM Compound: 2, T0901317	Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay	[PMID: 19264481]
SH-SY5Y	EC₅₀	0.085 μM Compound: 2, T0901317	Agonist activity at human LXRalpha expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay Agonist activity at human LXRalpha expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay	[PMID: 19264481]
THP-1	IC₅₀	> 10 μM Compound: 3, T1317	Transrepressional activity at LXR in human TPA-activated THP1 cells assessed as inhibition of LPS-induced IL6 production incubated for 6 hrs prior to LPS-challenge measured after 18 hrs by ELISA Transrepressional activity at LXR in human TPA-activated THP1 cells assessed as inhibition of LPS-induced IL6 production incubated for 6 hrs prior to LPS-challenge measured after 18 hrs by ELISA	[PMID: 22873709]
THP-1	EC₅₀	0.033 μM Compound: T0901317	Induction of cholesterol efflux in THP1 cells after 18 hrs Induction of cholesterol efflux in THP1 cells after 18 hrs	[PMID: 17416521]
THP-1	IC₅₀	100 nM Compound: 3, T1317	Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production after 6 hrs by ELISA Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production after 6 hrs by ELISA	[PMID: 18800767]
THP-1	IC₅₀	26 μM Compound: 3, T0901317	Transrepression activity of LXR in human THP1 cells assessed as inhibition of LPS-induced IL-6 level after 18 hrs by ELISA Transrepression activity of LXR in human THP1 cells assessed as inhibition of LPS-induced IL-6 level after 18 hrs by ELISA	[PMID: 26288691]

體外研究
(In Vitro)

T0901317 (5-50 μM；72 小時) 以劑量依賴性和時間依賴性方式顯著抑制 CaOV3、SKOV3、A2780 (人卵巢癌細胞系) 的細胞增殖^[5]。
T0901317 (10 μM；24-72 小時) 降低處于 S 期的細胞百分比并增加處于 G0/G1 期的細胞百分比，表明細胞周期停滯在 G1-S 檢查點。G0/G1期細胞百分比呈時間依賴性增加^[5]。
T0901317 (10-40 μM；24 hours) 導(dǎo)致細胞早期凋亡顯著增加^[5]。
T0901317 (5-40 μM；48 小時) 導(dǎo)致 p21 和 p27 蛋白表達在 48 小時后以劑量依賴性方式增加^[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[5]

Cell Line:	A2780, CaOV3 and SKOV3 ovarian cancer cell lines
Concentration:	5, 10, 20, 40 or 50 μM
Incubation Time:	72 hours
Result:	Inhibited cellular proliferation in all cell lines in a dose-dependent and time-dependent manner.

Cell Cycle Analysis^[5]

Cell Line:	A2780, CaOV3 and SKOV3 cells
Concentration:	10 μM
Incubation Time:	24, 48 or 72 hours
Result:	Decreased the percentage of cells in S phase and increased the percentage of cells in the G0/G1 phase.

Apoptosis Analysis^[5]

Cell Line:	CaOV3 cells
Concentration:	10 to 40 μM
Incubation Time:	24 hours
Result:	Resulted in a significant increase of cells in early apoptosis.

Western Blot Analysis^[5]

Cell Line:	CaOV3 cells
Concentration:	5 to 40 μM
Incubation Time:	48 hours
Result:	Resulted in an increase of p21 and p27 protein expression in a dose-dependent manner.

體內(nèi)研究
(In Vivo)

T0901317 (10 毫克/公斤/天；口服；持續(xù) 12 周) 抑制動脈粥樣硬化的進展^[5]。
T0901317 (腹腔注射；50 毫克/公斤；每周兩次，持續(xù) 7 天) 可以保護雄性 C57BL/6 小鼠免受高脂飲食誘導(dǎo)的肥胖和胰島素抵抗^[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	8- to 10-week-old LDL receptor null mice^[5]
Dosage:	10 mg/kg
Administration:	Orally; daily; for 12 weeks
Result:	Inhibited the progression of atherosclerosis.

分子量

481.33

Formula

C₁₇H₁₂F₉NO₃S

CAS 號

293754-55-9

性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性數(shù)據(jù)

細胞實驗：

DMSO 中的溶解度 : 100 mg/mL (207.76 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

Ethanol 中的溶解度 : 100 mg/mL (207.76 mM; 超聲助溶)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.0776 mL	10.3879 mL	20.7758 mL
5 mM	0.4155 mL	2.0776 mL	4.1552 mL
10 mM	0.2078 mL	1.0388 mL	2.0776 mL

查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

摩爾計算器
稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動物實驗：

請根據(jù)您的實驗動物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

方案一

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (6.23 mM); 澄清溶液

此方案可獲得 ≥ 3 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 30.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (6.23 mM); 澄清溶液

此方案可獲得 ≥ 3 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 30.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案三

請依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 3 mg/mL (6.23 mM); 澄清溶液

此方案可獲得 ≥ 3 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。
以 1 mL 工作液為例，取 100 μL 30.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。
方案四

請依序添加每種溶劑： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 2.5 mg/mL (5.19 mM); 懸濁液; 超聲助溶
方案五

請依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.19 mM); 澄清溶液

動物溶解方案計算器

請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

每只動物的給藥體積

μL

動物數(shù)量

只

由于實驗過程有損耗，建議您多配一只動物的量

請輸入您的動物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購。，Tween 80，均可在 MCE 網(wǎng)站選購。

計算結(jié)果

工作液所需濃度 : mg/mL

儲備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。

動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。

請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.93%

選擇批次：

Data Sheet (652 KB) SDS (393 KB)

COA (197 KB) HNMR (272 KB) RP-HPLC (242 KB) LCMS (94 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻

[1]. J R Schultz, et al. Role of LXRs in Control of Lipogenesis. Genes Dev. 2000 Nov 15;14(22):2831-8. [Content Brief]

[2]. Keith A Houck, et al. T0901317 Is a Dual LXR/FXR Agonist. Mol Genet Metab. Sep-Oct 2004;83(1-2):184-7. [Content Brief]

[3]. Naresh Kumar, et al. The Benzenesulfoamide T0901317 [N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] Is a Novel Retinoic Acid Receptor-Related Orphan Receptor-Alpha/Gamma Inverse Agonist. Mol Pharmacol. 2010 Feb;77(2):228-36. [Content Brief]

[4]. Rough JJ, et al. Anti-proliferative effect of LXR agonist T0901317 in ovarian carcinoma cells. J Ovarian Res. 2010 May 26;3:13. [Content Brief]

[5]. Todd G Kirchgessner, et al. Beneficial and Adverse Effects of an LXR Agonist on Human Lipid and Lipoprotein Metabolism and Circulating Neutrophils. Cell Metab. 2016 Aug 9;24(2):223-33. [Content Brief]

[6]. Mingming Gao, et al. The Liver X Receptor Agonist T0901317 Protects Mice From High Fat Diet-Induced Obesity and Insulin Resistance. AAPS J. 2013 Jan;15(1):258-66. [Content Brief]

T0901317 相關(guān)分類

完整儲備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg	25 mg

DMSO / Ethanol	1 mM	2.0776 mL	10.3879 mL	20.7758 mL	51.9394 mL
	5 mM	0.4155 mL	2.0776 mL	4.1552 mL	10.3879 mL
	10 mM	0.2078 mL	1.0388 mL	2.0776 mL	5.1939 mL
	15 mM	0.1385 mL	0.6925 mL	1.3851 mL	3.4626 mL
	20 mM	0.1039 mL	0.5194 mL	1.0388 mL	2.5970 mL
	25 mM	0.0831 mL	0.4155 mL	0.8310 mL	2.0776 mL
	30 mM	0.0693 mL	0.3463 mL	0.6925 mL	1.7313 mL
	40 mM	0.0519 mL	0.2597 mL	0.5194 mL	1.2985 mL
	50 mM	0.0416 mL	0.2078 mL	0.4155 mL	1.0388 mL
	60 mM	0.0346 mL	0.1731 mL	0.3463 mL	0.8657 mL
	80 mM	0.0260 mL	0.1298 mL	0.2597 mL	0.6492 mL
	100 mM	0.0208 mL	0.1039 mL	0.2078 mL	0.5194 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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純度 & 產(chǎn)品資料

參考文獻

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稀釋計算器

T0901317 相關(guān)分類

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摩爾計算器

稀釋計算器

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完整儲備液配制表

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