Pioglitazone HCl

别名: AD-4833, U-72107E 中文名称：盐酸吡格列酮

目录号：S2046 Purity: 99.88%

Pioglitazone HCl (AD-4833, U-72107E) 是一种 cytochrome P450 (CYP)2C8 和 CYP3A4 酶的抑制剂。Pioglitazone HCl 抑制CYP2C8、CYP3A4和CYP2C9的Ki值分别为1.7 μM、11.8 μM和32.1 μM。Pioglitazone HCl 也是一种选择性的 peroxisome proliferator-activated receptor-gamma (PPARγ) 激动剂，对人PPARγ和小鼠PPARγ的EC50值分别为0.93 μM和0.99 μM。Pioglitazone HCl 可抑制线粒体内铁的摄取、脂质过氧化和随后的铁死亡。

Pioglitazone HCl Chemical Structure

CAS: 112529-15-4

规格	价格	库存
10mM (1mL in DMSO)	RMB 647.01	现货
10mg	RMB 647.01	现货
50mg	RMB 1387.89	现货
200mg	RMB 3019.29	现货
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客户使用Selleck的Pioglitazone HCl发表文献10篇

客户使用该产品的2个实验数据

产品质控

批次：纯度： 99.88%

99.88

Pioglitazone HCl相关产品

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P450 (e.g. CYP17)抑制剂选择性比较

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
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	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
HepG2 cells	Function assay			Peroxisome proliferator activated receptor gamma agonistic activity in HepG2 cells, EC50=7.6 μM	10714503
COS cells	Function assay			Transcriptional activation in COS cells expressing PPAR gamma and RXR alpha; values in the parentheses indicates 95% confidence interval, EC50=0.49 μM	11906293
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
点击查看更多细胞系数据

生物活性

产品描述

靶点

Ferroptosis ^[8]	hPPARγ ^[1] (Cell-free assay)	rPPARγ ^[6] (Cell-free assay)	CYP2C8 ^[7] (Cell-free assay)	CYP3A4 ^[7] (Cell-free assay)	点击更多
	0.93 μM(EC50)	0.99 μM(EC50)	1.7 μM(Ki)	11.8 μM(Ki)	点击更多

体外研究(In Vitro)
体外研究活性	Pioglitazone抑制LPS诱导的iNOS表达和NO的产生，并抑制iNOS表达足以保护多巴胺神经元抗LPS损伤。Pioglitazone保护多巴胺能神经元免受LPS，至少通过抑制iNOS的表达和NO的产生，这是通过抑制p38蛋白激酶的活性介导的。Pioglitazone抑制p38蛋白的LPS诱导的磷酸化。^[1]

体内研究(In Vivo)
体内研究活性	在雄性肥胖鼠中，Pioglitazone口服（0.3-3毫克/公斤/天7天）剂量依赖性地降低了高血糖症，高脂血症，和高胰岛素血症。在大鼠中，Pioglitazone改善葡萄糖耐受性和增加外源性胰岛素和血浆甘油三酯的清除。^[2] 在未处理的SOD1-G93A小鼠中，Pioglitazone处理转基因小鼠显示改进的肌肉力量和体重，表现出延迟疾病发作和显著较长生存比。^[3] 在大鼠和小鼠中，Pioglitazone显著降低高血糖症，高脂血症，高胰岛素血症，葡萄糖不耐症，其特征如胰岛素抵抗状态。在黄色的KK小鼠的隔膜和脂肪组织中，Pioglitazone在的胰岛素介导的葡萄糖代谢。在Zucker肥胖大鼠中，Pioglitazone增强在源性胰岛素的血糖反应。^[4] 在APPV717I转基因小鼠的海马和皮层活性星形细胞中，Pioglitazone导致激活的小胶质细胞的数量减少。在APPV717I转基因小鼠中，Pioglitazone降低β-分泌-1（BACE1）的mRNA和蛋白水平。^[5]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05946564	Not yet recruiting	ANCA Associated Vasculitis\|Rapidly Progressive Glomerulonephritis\|Crescentic Glomerulonephritis	Assistance Publique - Hôpitaux 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

参考文献
[1] Xing B, et al. J Neuroinflammation,?008, 5, 4. [2] Sugiyama Y, et al. Arzneimittelforschung,?990, 40(3), 263-267. [3] Burkhard Schütz, et al. J Neurosci,?005, 25(34), 7805-7812. [4] Ikeda H, et al. Arzneimittelforschung,?990, 40(2 Pt 1), 156-162. [5] Kondo T, et al. Arzneimittelforschung,?996, 46(6), 594-600. [6] Kenji Kuwabara, et al. J Pharmacol Exp Ther . 2004 Jun;309(3):970-7. [7] Jasminder Sahi, et al. Drug Metab Dispos . 2003 Apr;31(4):439-46. [8] Hua Yuan, et al. Biochem Biophys Res Commun . 2016 Sep 16;478(2):838-44. + 展开

参考文献

+ 展开

化学信息&溶解度

分子量	392.9	分子式	C₁₉H₂₀N₂O₃S.HCl
CAS号	112529-15-4	SDF	Download Pioglitazone HCl SDF
Smiles	CCC1=CN=C(C=C1)CCOC2=CC=C(C=C2)CC3C(=O)NC(=O)S3.Cl
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 79 mg/mL ( (201.06 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 4 mg/mL

Water : Insoluble

摩尔浓度计算器

体内溶解度批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂					动物体内配方计算器
体内溶解度批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂	澄清溶液	5%DMSO 1 Corn oil	5mg/ml (12.73mM)	以 1 mL 工作液为例，取50μL100mg/ml的澄清DMSO储备液加到950μL玉米油中，混合均匀。工作液请现配现用！	动物体内配方计算器
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5mg/ml (12.73mM)	以 1 mL 工作液为例,取50μL100mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	2mg/ml (5.09mM)	以 1 mL 工作液为例，取50μL40mg/ml的澄清DMSO储备液加到400μL PEG300中，混合均匀使其澄清；向上述体系中加入50μLTween80，混合均匀使其澄清；然后继续加入500μL ddH2O定容至 1 mL。工作液请现配现用！

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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