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| Product Name | JNJ-42041935 |
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| Description | Purity >98%. 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. 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 (pKi s = 7.91, 7.29, and 7.65 for PHD1, 2, and 3, respectively). It is >100-fold selective for PHD compared to the related FIH (factor-inhibiting HIF) and a panel of various other enzymes. 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. |
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| Size | n/a |
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| Concentration | n/a |
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| Applications | n/a |
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| Other Names | 1-[6-chloro-5-(trifluoromethoxy)-1H-benzimidazol-2-yl]-1H-pyrazole-4-carboxylic acid, HIF-PHD Inhibitor II |
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| Gene, Accession, CAS # | CAS: 1193383-09-3 |
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| Catalog # | LS-H8296 |
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| Order / More Info | JNJ-42041935 from LIFESPAN BIOSCIENCES INC. |
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| Product Specific References | n/a |
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