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1246525-60-9

中文名稱 SR1078
英文名稱 SR 1078
CAS 1246525-60-9
分子式 C17H10F9NO2
分子量 431.25
MOL 文件 1246525-60-9.mol
更新日期 2024/12/15 19:35:21
1246525-60-9 結(jié)構(gòu)式 1246525-60-9 結(jié)構(gòu)式

基本信息

中文別名
化合物SR 1078
RORΑ/Γ激動劑(SR1078)
N-[4-[2,2,2-三氟-1-羥基-1-(三氟甲基)乙基]苯基]-4-(三氟甲基)苯甲酰胺
英文別名
SR 1078
SR 1078
SR-1078
SR 1078 USP/EP/BP
SR1078
SR 1078
SR-1078
SR1078,N-[4-(2,2,2-TRIFLUORO-1-HYDROXY-1-TRIFLUOROMETHYL-ETHYL)-PHENYL]-4-TRIFLU
N-[4-(1,1,1,3,3,3-Hexafluoro-2-hydroxy-2-propanyl)phenyl]-4-(trifluoromethyl)benzamide
N-[4-[2,2,2-Trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-4-(trifluoromethyl)benzamide
Benzamide, N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-4-(trifluoromethyl)-
SR1078,N-[4-(2,2,2-Trifluoro-1-hydroxy-1-trifluoroMethyl-ethyl)-phenyl]-4-trifluoroMethyl-benzaMide
N-[4-[2,2,2-Trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-4-(trifluoromethyl)benzamide SR1078
所屬類別
生物化工:蛋白酪氨酸激酶

物理化學(xué)性質(zhì)

熔點169℃
沸點362.9±42.0 °C(Predicted)
密度1.527±0.06 g/cm3(Predicted)
儲存條件-20°C冷凍
溶解度可溶于DMSO、甲醇(少許)
酸度系數(shù)(pKa)9.21±0.15(Predicted)
形態(tài)固體
顏色米白色

圖譜信息

SR1078價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2025/02/05HY-14422SR10781246525-60-91 mg427元
2025/02/05HY-14422SR1078
SR1078
1246525-60-910mM * 1mLin DMSO892元
2025/02/05HY-14422SR1078
SR1078
1246525-60-95mg940元

常見問題列表

生物活性
SR1078是RORα/γ的激活劑。
靶點
TargetValue
RORα
()
RORγ
()
體外研究

SR1078 is a synthetic RORα/RORγ ligand. SR1078 modulates the conformation of RORγ in a biochemical assay and activates RORα and RORγ driven transcription. Furthermore, SR1078 stimulates expression of endogenous ROR target genes in HepG2 cells that express both RORα and RORγ. In a cell-based chimeric receptor Gal4 DNA-binding domain-NR ligand binding domain cotransfection assay, SR1078 significantly inhibits the constitutive transactivation activity of RORα and RORγ, but has no effect on the activity of FXR, LXRα and LXRβ. In a RORα cotransfection assay, treatment of cells with SR1078 (10 μM) results in a significant increase in transcription. Similarly, in the RORγ cotransfection assay, SR1078 treatment results in a stimulation of RORγ-dependent transcription activity.
SR1078 (2-10 μM; 24 hours) shows a dose-dependent increase in expression of A2BP1, CYP19A1, NLGN1, and IPTR1 in SH-SY5Y cells. EC50’s are in the range of 3-5 μM.

體內(nèi)研究

The pharmacokinetic properties of SR1078 are examined in mice and noted significant exposure. Plasma concentrations reach 3.6 μM 1h after a 10 mg/kg i.p. injection of SR1078 and sustained levels of above 800 nM even 8h after the single injection. These levels are sufficient to perform a proof-of-principle experiment to determine if SR1078 treatment would stimulate ROR target gene expression in an animal model. Mice are treated with SR1078 (10 mg/kg; i.p.) and 2h after the injection the livers are harvested and mRNA purified for assessment of G6Pase and FGF21 gene expression.T he expression of both FGF21 and G6Pase is significantly stimulated by SR1078 treatment vs. vehicle control.
SR1078 (10 mg/kg; i.p.) shows a significant 25% reduction in repetitive grooming behavior in the BTBR mice.

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