JNJ-42041935
货号：
14316-1mg 基本售价：
686.0 元 规格：
1 mg
产品信息
概述| 货号 | 14316-1mg |
| 描述 | Hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) enzymes act as central gatekeepers of posttranscriptional and transcriptional adaptation to hypoxia, oxidative stress, and excitotoxicity. Their catalytic activity is dependent on iron, 2-oxoglutarate (2-OG), and oxygen, and leads to the stabilization of a host of proteins, including the hypoxia-inducible transcription factors in response to oxygen availability.1 Inhibitors of PHD have been used to mimic a hypoxic response in order to study a range of oxygen-deprivation-related disorders, including anemia, ulcerative colitis, myocardial ischemia, stroke, and metabolic disorders. JNJ-42041935 is a selective, 2-OG competitive, and reversible inhibitor of PHD enzymes (pKis = 7.91, 7.29, and 7.65 for PHD1, 2, and 3, respectively).2 It is >100-fold selective for PHD compared to the related FIH (factor-inhibiting HIF) and a panel of various other enzymes.2 In an inflammation-induced anemia model in rats, 100 µM/kg/day JNJ-42041935 significantly increased the number of circulating reticulocytes and red blood cells, increased blood hemoglobin and hematocrit, and restored mean corpuscular volume and mean cell hemoglobin of red bloods cells.2 |
| 别名 | HIF-PHD Inhibitor II; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Nguyen, L.K.,Cavadas, M.A.S.,Scholz, C.C., et al. A dynamic model of the hypoxia-inducible factor 1a (HIF-1a) network. Journal of Cell Science 126, 1454-1463 (2015).
2.Barrett, T.D.,Palomino, H.L.,Brondstetter, T.I., et al. Pharmacological characterization of 1-(5-chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (JNJ-42041935), a potent and selective hypoxia-inducible factor prolyl hydroxylase inhibitor. Molecular Pharmacology 79(6), 910-920 (2011).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 346.7 |
| 分子式 | C12H6ClF3N4O3 |
| CAS号 | 1193383-09-3 |
| 稳定性 | ≥ 2 years |
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