Pioglitazone

別名: AD-4833, U 72107 中文名稱：吡格列酮

目錄號(hào)：S2590 Purity: 99.83%

Pioglitazone是一種選擇性過氧化物酶體增殖物激活受體γ (PPARγ) 激動(dòng)劑，用于治療糖尿病。是全長(zhǎng)hPPARα的弱激活劑，對(duì)全長(zhǎng)hPPARδ沒有作用。

Pioglitazone Chemical Structure

CAS: 111025-46-8

規(guī)格	價(jià)格	庫存
10mM (1mL in DMSO)	1056.72	現(xiàn)貨
10mg	789.99	現(xiàn)貨
50mg	1372.45	現(xiàn)貨
200mg	3033.76	現(xiàn)貨
1g	7944.3	現(xiàn)貨
更大包裝有超大折扣
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產(chǎn)品質(zhì)控

批次：純度： 99.83%

99.83

Pioglitazone相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	PPARα PPARβ/δ PPARγ PPARδ	點(diǎn)擊展開
相關(guān)產(chǎn)品	T0070907 GW9662 GW6471 WY-14643 (Pirinixic Acid) GSK3787 GW0742 AZ6102 Astaxanthin Eupatilin GSK0660 Oroxin A Harmine Palmitoylethanolamide DG172 dihydrochloride Glabridin Ciprofibrate Clofibric Acid Alpinetin Elafibranor Daidzein Gypenoside XLIX	點(diǎn)擊展開
相關(guān)化合物庫	代謝化合物庫抗癌代謝化合物庫谷氨酰胺代謝化合物庫糖代謝化合物庫脂代謝化合物庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
HEK293T	Function assay	1 uM	24 hrs	Partial agonist activity at human PPARgamma-LBD expressed in HEK293T cells assessed as induction of receptor transactivation at 1 uM after 24 hrs by luciferase reporter gene assay	21030263
HEK293	Function assay	10 uM	24 hrs	Transactivation of PPAR-gamma (unknown origin) expressed in HEK293 cells at 10 uM after 24 hrs by luciferase reporter gene assay	24890090
THP1	Function assay	10 uM	24 hrs	Upregulation of ABCA1 mRNA expression in human THP1 cells at 10 uM after 24 hrs by qPCR method relative to control	27220065
THP1	Function assay	10 uM	24 hrs	Upregulation of ABCG1 mRNA expression in human THP1 cells at 10 uM after 24 hrs by qPCR method relative to control	27220065
PC3	Function assay	50 uM	24 hrs	Increase in p21(WAF1) protein expression in human PC3 cells at 50 uM incubated for 24 hrs by Western blot analysis	28395220
MDA-MB-231	Function assay	50 uM	24 hrs	Increase in p21(WAF1) protein expression in human MDA-MB-231 cells at 50 uM incubated for 24 hrs by Western blot analysis	28395220
SCC15	Cytotoxicity assay	50 uM	24 hrs	Cytotoxicity against human SCC15 cells transfected with PPARalpha siRNA assessed as reduction in cell viability at 50 uM after 24 hrs by resazurin reduction assay	29031063
SCC15	Cytotoxicity assay	50 uM	24 hrs	Cytotoxicity against human SCC15 cells transfected with PPARbeta siRNA assessed as reduction in cell viability at 50 uM after 24 hrs by resazurin reduction assay	29031063
3T3L1	Function assay	10 uM	24 hrs	Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in AP1 mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis	30594432
3T3L1	Function assay	10 uM	24 hrs	Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in CD36 mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis	30594432
3T3L1	Function assay	10 uM	24 hrs	Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in Glut4 mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis	30594432
3T3L1	Function assay	10 uM	24 hrs	Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in adiponectin mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis	30594432
K562-IMA[r]	Function assay	10 uM	72 hrs	Induction of sensitization to imatinib-induced cytotoxicity in imatinib-resistant human K562-IMA[r] cells assessed as induction of cell death at 10 uM after 72 hrs in presence of 1 uM imatinib by propidium iodide/Triton-X100 dye based FACS analysis	31648125
3T3L1	Function assay	100 umol/L		Increase in PPARgamma mRNA levels in mouse 3T3L1 cells at 100 umol/L by RT-PCR	20392645
HepG2	Function assay	30 uM		Binding affinity to NAF1 (unknown origin) expressed in human HepG2 cells assessed as inhibition of mitochondrial respiration at 30 uM	30770154
HepG2	Function assay	30 uM		Binding affinity to NAF1 in human HepG2 cells assessed as inhibition of mitochondrial respiration at 30 uM	30770154
Cos7	Function assay		14 hrs	Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay, EC50=0.3μM	20307981
CHO	Function assay		24 hrs	Partial agonist activity at human PPARgamma expressed in CHO cells co-transfected with Gal4-responsive luciferase reporter plasmid after 24 hrs by transactivation assay, EC50=0.39μM	21377875
HepG2	Function assay		20 hrs	Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay, EC50=0.57μM	22341573
HEK293	Function assay		18 hrs	Transactivation of human GAL4-fused PPARgamma ligand binding domain transfected in HEK293 cells after 18 hrs by dual luciferase reporter gene assay, EC50=0.8μM	23102891
THP1	Antiinflammatory assay		1 hr	Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion preincubated for 1 hr prior PMA-challenge measured after 48 hrs by ELISA, IC50=18.84μM	23811092
THP1	Antiinflammatory assay		2 hrs	Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion incubated for 2 hrs prior to PMA challenge measured after 72 hrs by ELISA, IC50=18.6μM	24531227
HEK293	Function assay		18 hrs	Agonist activity at human PPARgamma expressed in HEK293 cells incubated for 18 hrs by luciferase reporter gene assay, EC50=0.21μM	25333853
COS7	Function assay		42 hrs	Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay, EC50=0.5μM	27560282
COS7	Function assay		42 hrs	Transactivation at Gal4 fused PPARgamma LBD (unknown origin) expressed in African green monkey COS7 cells after 42 hrs by luciferase assay, EC50=0.32μM	27569195
COS7	Function assay		42 hrs	Transactivation of Gal4 fused human PPARgamma LBD expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay, EC50=0.38μM	27918994
HEK293	Function assay		24 hrs	Transactivation activity at Gal4 fused full length human PPARgamma LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay, EC50=1.1μM	28465099
HEK293	Function assay		4 hrs	Transrepression activity at human PPARgamma expressed in HEK293 cells assessed as inhibition of TNFalpha induced NF-kappaB promoter activity pretreated for 4 hrs followed by TNFalpha stimulation after 3 hrs by luciferase reporter gene assay, IC50=22μM	28465099
HepG2	Function assay		24 hrs	Agonist activity at PPARgamma in human HepG2 cells assessed as activation of PPRE incubated for 24 hrs by dual luciferase reporter gene assay, EC50=0.24μM	30001846
HEK293BENA	Function assay		24 hrs	Transactivation of GAL4-fused human PPARgamma transfected in HEK293BENA cells after 24 hrs by steady glo-luciferase reporter gene assay, EC50=2.053μM	30351933
HEK293	Function assay		18 hrs	Transactivation of human full length PPARgamma expressed in HEK293 cells after 18 hrs by luciferase reporter gene based luminescence assay, EC50=0.1μM	30362739
293H	Function assay		16 hrs	Transactivation of GAL4-DBD fused human PPARgamma ligand binding domain expressed in UAS-bla HEL 293H cells preincubated for 16 hrs followed by FRET substrate addition and measured after 2 hrs by TR-FRET assay, EC50=0.098μM	30429097
stem cells	Function assay		5 days	Induction of adipogenesis in human bone marrow-derived mesenchymal stem cells assessed as increase in adiponectin production measured on day 5 in presence of IDX by ELISA, EC50=0.35μM	30672698
HEK293T	Function assay		18 hrs	Transactivation of full length human PPARgamma2 expressed in HEK293T cells co-expressing PPRE after 18 hrs by luciferase reporter gene assay, EC50=0.25μM	30676741
HEK293T	Function assay		18 hrs	Transactivation of chimeric Gal4 yeast DBD fused-PPARgamma LBD (unknown origin) expressed in HEK293T cells co-expressing PPRE after 18 hrs by luciferase reporter gene assay, EC50=0.35μM	30676741
COS7	Function assay		39 hrs	Transactivation of Gal4-fused human PPARgamma transfected in COS7 cells co-transfected with pGAL5-TK-pGL3 and pRennilla-CMV incubated for 39 hrs by dual luciferase reporter assay, EC50=1.4μM	31648125
CV-1	Function assay			In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells, EC50=0.69μM	8576907
3T3-L1	Function assay			Effective concentration for 50% enhancement of insulin-induced triglyceride accumulation in 3T3-L1 cells, EC50=0.16μM	9599241
CV-1	Function assay			Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells, EC50=0.58884μM	9836620
CV-1	Function assay			Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay., EC50=0.58μM	11720854
HEK293	Function assay			Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with steroid receptor coactivator-1 by EYFP based reporter gene assay	16680159
HEK293	Function assay			Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with retinoid X-receptor alpha by EYFP based reporter gene assay	16680159
CV1	Function assay			Transactivation of PPARgamma in CV1 cells, EC50=0.55μM	16821769
CHO	Function assay			Activation of Gal4-tagged human PPARgamma expressed in CHO cells by luciferase reporter gene assay, EC50=0.14μM	20656494
COS-1	Function assay			Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells co-transfected with Gal4 by luciferase reporter gene assay, EC50=0.39μM	21130649
COS7	Function assay			Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay, EC50=0.3μM	21873070
Sf21	Function assay			Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50=0.3μM	21965623
Sf21	Function assay			Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50=2μM	21965623
COS7	Function assay			Transactivation of GAL4-fused human PPARgamma ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay, EC50=0.2μM	23130964
COS7	Function assay			Transactivation of human PPARgamma expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay, EC50=0.2μM	26595749
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點(diǎn)

PPARγ ^[2]

體外研究(In Vitro)
體外研究活性	Pioglitazone主要被CYP2C8代謝，其次被CYP3A4代謝。^[1]
實(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)圖片	PMID
實(shí)驗(yàn)圖片	Western blot	p-VEGFR2 / VEGFR Phopsho-RB / RB		29972411

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	在廣泛前壁心肌梗死小鼠中，Pioglitazone通過超聲心動(dòng)圖顯著減弱左心室（LV）腔擴(kuò)張和功能障礙，，以及左心室舒張末期壓力。Pioglitazone部分標(biāo)準(zhǔn)化左心房 DP/ DT（最大）和DP/ DT（最?。?，左室收縮功能，其指標(biāo)在MI小鼠中顯著減少。^[2] 在帕金森氏病的MPTP模型小鼠都紋狀體和黑質(zhì)致密部中，Pioglitazone導(dǎo)致小膠質(zhì)細(xì)胞的激活減少，減少的感應(yīng)的iNOS陽性細(xì)胞和少膠質(zhì)纖維酸性蛋白陽性細(xì)胞。Pioglitazone幾乎完全阻斷TH陽性神經(jīng)元的nitrotyrosine染色，nitrotyrosine是NO介導(dǎo)的細(xì)胞損傷的標(biāo)記物。^[3] 在帕金森氏病的MPTP模型小鼠的黑質(zhì)致密部（黑質(zhì)致密部）中，Pioglitazone (約20 毫克/千克/天）衰減MPTP誘導(dǎo)的神經(jīng)膠質(zhì)活化，并防止多巴胺能細(xì)胞的損失。^[4] 在10個(gè)月大的APPV717I轉(zhuǎn)基因小鼠的海馬和皮質(zhì)中，Pioglitazone導(dǎo)致活化的小膠質(zhì)細(xì)胞和活性星形細(xì)胞數(shù)量減少。Pioglitazone處理減少了促炎的表達(dá)酶環(huán)氧合酶-2（COX-2）和誘導(dǎo)型一氧化氮合酶（iNOS）的表達(dá)。Pioglitazone降低beta-secretase-1 (BACE1)的mRNA和蛋白質(zhì)水平，以及可溶性Abeta1-42肽的水平下降27％。^[5]

體內(nèi)研究(In Vivo)

體內(nèi)研究活性

在廣泛前壁心肌梗死小鼠中，Pioglitazone通過超聲心動(dòng)圖顯著減弱左心室（LV）腔擴(kuò)張和功能障礙，，以及左心室舒張末期壓力。Pioglitazone部分標(biāo)準(zhǔn)化左心房 DP/ DT（最大）和DP/ DT（最?。?，左室收縮功能，其指標(biāo)在MI小鼠中顯著減少。^[2]

在帕金森氏病的MPTP模型小鼠都紋狀體和黑質(zhì)致密部中，Pioglitazone導(dǎo)致小膠質(zhì)細(xì)胞的激活減少，減少的感應(yīng)的iNOS陽性細(xì)胞和少膠質(zhì)纖維酸性蛋白陽性細(xì)胞。Pioglitazone幾乎完全阻斷TH陽性神經(jīng)元的nitrotyrosine染色，nitrotyrosine是NO介導(dǎo)的細(xì)胞損傷的標(biāo)記物。^[3]

在帕金森氏病的MPTP模型小鼠的黑質(zhì)致密部（黑質(zhì)致密部）中，Pioglitazone (約20 毫克/千克/天）衰減MPTP誘導(dǎo)的神經(jīng)膠質(zhì)活化，并防止多巴胺能細(xì)胞的損失。^[4]

在10個(gè)月大的APPV717I轉(zhuǎn)基因小鼠的海馬和皮質(zhì)中，Pioglitazone導(dǎo)致活化的小膠質(zhì)細(xì)胞和活性星形細(xì)胞數(shù)量減少。Pioglitazone處理減少了促炎的表達(dá)酶環(huán)氧合酶-2（COX-2）和誘導(dǎo)型一氧化氮合酶（iNOS）的表達(dá)。Pioglitazone降低beta-secretase-1 (BACE1)的mRNA和蛋白質(zhì)水平，以及可溶性Abeta1-42肽的水平下降27％。^[5]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05946564	Not yet recruiting	ANCA Associated Vasculitis\|Rapidly Progressive Glomerulonephritis\|Crescentic Glomerulonephritis	Assistance Publique - H?pitaux de Paris\|Ministry of Health France	July 2023	Phase 3
NCT05305287	Recruiting	Non-Alcoholic Fatty Liver Disease\|Type 2 Diabetes\|Mitochondrial Metabolism Disorders	The University of Texas Health Science Center at San Antonio\|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)	November 1 2022	Phase 4
NCT05411965	Completed	Diabetes Mellitus Type 2	Boryung Pharmaceutical Co. Ltd	April 28 2022	Phase 1
NCT04501406	Recruiting	Type 2 Diabetes Mellitus (T2DM)\|Nonalcoholic Steatohepatitis	University of Florida\|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)	December 15 2020	Phase 2
NCT04535700	Completed	Type 2 Diabetes	Fundacion para la Investigacion Biomedica del Hospital Universitario Ramon y Cajal	September 18 2020	Phase 4
NCT00904046	Recruiting	Uric Acid Kidney Stone Disease	University of Texas Southwestern Medical Center\|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)\|Takeda Pharmaceuticals North America Inc.	September 5 2019	Not Applicable

參考文獻(xiàn)
[1] Jaakkola T, et al. Basic Clin Pharmacol Toxicol,?006, 99(1), 44-51. [2] Shiomi T, et al. Circulation,?002, 106(24), 3126-3132. [3] Dehmer T, et al. J Neurochem,?004, 88(2), 494-501. [4] Breidert T, et al. J Neurochem,?002, 82(3), 615-624. [5] Heneka MT, et al. Brain,?005, 128(Pt 6), 1442-1453. [6] Wang M, et al. J Cell Mol Med. 2022 Feb;26(4):1034-1049. + 展開

參考文獻(xiàn)

[1] Jaakkola T, et al. Basic Clin Pharmacol Toxicol,?006, 99(1), 44-51.
[2] Shiomi T, et al. Circulation,?002, 106(24), 3126-3132.
[3] Dehmer T, et al. J Neurochem,?004, 88(2), 494-501.

[4] Breidert T, et al. J Neurochem,?002, 82(3), 615-624.
[5] Heneka MT, et al. Brain,?005, 128(Pt 6), 1442-1453.
[6] Wang M, et al. J Cell Mol Med. 2022 Feb;26(4):1034-1049.

+ 展開

化學(xué)信息&溶解度

分子量	356.44	分子式	C₁₉H₂₀N₂O₃S
CAS號(hào)	111025-46-8	SDF	Download Pioglitazone SDF
Smiles	CCC1=CN=C(C=C1)CCOC2=CC=C(C=C2)CC3C(=O)NC(=O)S3
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 20 mg/mL ( (56.11 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 15 mg/mL ( (42.08 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 23 mg/mL ( (64.52 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 17 mg/mL ( (47.69 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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* 必填項(xiàng)

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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