Pioglitazone (AD-4833), 过氧化物酶体增殖激活受体-γ 的激动剂;TRPM3 的通道阻断剂

PPARγ Selective Inhibitors | Activators | Agonists | Antagonists | Modulators
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货号 (SKU) 包装规格 是否现货 价格 数量
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Compound libraries (12332)

基本描述

别名 吡格列酮 (AD-4833)
英文别名 U 72107 | 5-​[[4-​[2-​(5-​ethyl-​2-​pyridinyl)​ethoxy]​phenyl]​methyl]​-2,​4-​thiazolidinedione
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Pioglitazone (AD-4833)
生化机理 吡格列酮(AD-4833,U 72107)是一种选择性过氧化物酶体增殖激活受体-γ(PPARγ)激动剂,用于治疗糖尿病;是全长 hPPARα 的弱激活剂,但不是全长 hPPARδ。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 激动剂
作用机制 过氧化物酶体增殖激活受体-γ 的激动剂;TRPM3 的通道阻断剂
产品介绍

Pioglitazone 是一种选择性过氧化物酶体增殖物激活受体γ激动剂。A PPAR agonist with potential antidiabetic characteristics.

Information

Pioglitazone (AD-4833, U 72107) is a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist, used to treat diabetes; A weak activator for full-length hPPARα, but not full-length hPPARδ.
In vitro

Pioglitazone\xa0is\xa0metabolised\xa0mainly by\xa0CYP2C8\xa0and to a lesser extent by\xa0CYP3A4\xa0in\xa0vitro.\xa0

In vivo

Pioglitazone\xa0significantly attenuates left\xa0ventricular\xa0(LV) cavity dilatation and dysfunction by echocardiography as well as LV end-diastolic pressure\xa0in mice with extensive anterior myocardial\xa0infarction.\xa0Pioglitazone partially normalizes LV dP/dt(max) and dP/dt(min), indices of LV contractile function, which are significantly reduced in MI mice. Pioglitazone\xa0results in a reduced activation\xa0of microglia, reduced\xa0induction\xa0of\xa0iNOS-positive cells and less glial fibrillary acidic protein positive cells in both striatum and substantia nigra pars compacta of MPTP mouse\xa0model\xa0of\xa0Parkinson\'s\xa0disease. Pioglitazone\xa0almost completely blocks staining of TH-positive neurons for nitrotyrosine, a marker of NO-mediated cell damage.\xa0 Pioglitazone\xa0(approximately 20 mg/kg/day) attenuates the MPTP-induced glial activation and prevents the dopaminergic cell loss in the substantia nigra pars compacta (SNpc) in MPTP mouse\xa0model\xa0of\xa0Parkinson\'s\xa0disease. Pioglitazone results in a reduction in the number of activated microglia and reactive astrocytes in the hippocampus and cortex of 10-month-old\xa0APPV717I\xa0transgenic mice.\xa0Pioglitazone treatment\xa0reduces the expression of the proinflammatory enzymes cyclooxygenase 2 (COX2) and inducible nitric oxide synthase (iNOS).\xa0Pioglitazone decreases beta-secretase-1 (BACE1) mRNA and protein\xa0levels, and also a 27% reduction in the\xa0levels\xa0of soluble\xa0Abeta1-42\xa0peptide.\xa0
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥98%

关联靶点(人)

CA2 Tclin 碳酸酐酶2(Carbonic anhydrase 2) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ABCB11 Tchem 胆盐输出泵(Bile salt export pump) (6 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
MAOB Tclin 胺氧化酶[含黄素]B(Amine oxidase [flavin-containing] B) (4 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CISD1 Tchem CDGSH 铁硫结构域蛋白 1(CDGSH iron-sulfur domain-containing protein 1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
PPARG Tclin 过氧化物酶体增殖激活受体γ(Peroxisome proliferator-activated receptor gamma) (6 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES CCC1=CC=C(CCOC2=CC=C(CC3SC(=O)NC3=O)C=C2)N=C1
分子量 356.44

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 29 mg/mL (198.43 mM); Water: 29 mg/mL (198.43 mM); Ethanol: 29 mg/mL (198.43 mM);

安全和危险性(GHS)

技术规格说明书

Concentration 9-11(mmol/L)
Proton NMR spectrum Conforms to Structure

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

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