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活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
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P407870-1ml |
1ml |
现货 ![]() |
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别名 | 吡格列酮 (AD-4833) |
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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. 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 lines: Concentrations: Incubation Time: Powder Purity:≥98% |
分子类型 | 小分子 |
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Canonical SMILES | CCC1=CC=C(CCOC2=CC=C(CC3SC(=O)NC3=O)C=C2)N=C1 |
分子量 | 356.44 |
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); |
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Concentration | 9-11(mmol/L) |
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Proton NMR spectrum | Conforms to Structure |