1-(6-chloro-5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid
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1-(6-chloro-5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid
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CAS No:
1193383-09-3
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Formula:
C12H6ClF3N4O3
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Chemical Name:
1-(6-chloro-5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid
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Synonyms:
1-(6-chloro-5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid;1-[6-Chloro-5-(trifluoromethoxy)-1H-benzimidazol-2-yl]-1H-pyrazole-4-carboxylic acid;HIF-PHD Inhibitor II;CS-1577;JNJ 42041935;JNJ42041935;HIF-PHD INHIBITOR II;1-(5-Chloro-6-(trifluoromethoxy)-1H-benzo[d]imidazol-2-yl)-1H-pyrazole-4-carboxylic acid;1H-Pyrazole-4-carboxylic acid, 1-[6-chloro-5-(trifluoromethoxy)-1H-benzimidazol-2-yl]-;1-[6-chloro-5-(trifluoromethoxy)-1H-benzimidazol-2-yl]pyrazole-4-carboxylic acid
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CAS No:
1-(6-chloro-5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid Basic Attributes
346.65
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Characteristics
1.82±0.1 g/cm3(Predicted)
555.9±60.0 °C(Predicted)
3.52±0.10(Predicted)
Hygroscopic, -20°C Freezer, Under inert atmosphere
1-(6-chloro-5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid Use and Manufacturing
JNJ 42041935 is a selective hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) enzyme inhibitor. It can potentially be used for the treatment of inflammation-induced anemia.
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 (pKis = 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.[Cayman Chemical]
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