Pioglitazone HCl
别名: AD-4833, U-72107E 中文名称：盐酸吡格列酮
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
产品质控
批次：
纯度：
99.88%
99.88
Pioglitazone HCl相关产品
相关信号通路图
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 | 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。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点 |
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| 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] |
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|---|---|---|---|---|
| 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] |
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|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| 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 |
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) | |||
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体外溶解度 |
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 (10.18 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 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 | ||||
实验计算
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）
mg/kg
g
μL
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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