| Identification | Back Directory | [Name]
1-(6-chloro-5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid | [CAS]
1193383-09-3 | [Synonyms]
CS-1577
JNJ-42041935
HIF-PHD Inhibitor II
JNJ 42041935;JNJ42041935;HIF-PHD INHIBITOR II
1-[6-chloro-5-(trifluoromethoxy)-1H-benzimidazol-2-yl]pyrazole-4-carboxylic acid
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
1H-Pyrazole-4-carboxylic acid, 1-[6-chloro-5-(trifluoromethoxy)-1H-benzimidazol-2-yl]-
1-(6-Chloro-5-(trifluoromethoxy)-1H-benzo[d]imidazol-2-yl)-1H-pyrazole-4-carboxylic acid
1-(5-Chloro-6-(trifluoromethoxy)-1H-benzo[d]imidazol-2-yl)-1H-pyrazole-4-carboxylic acid | [Molecular Formula]
C12H6ClF3N4O3 | [MDL Number]
MFCD25541711 | [MOL File]
1193383-09-3.mol | [Molecular Weight]
346.65 |
| Chemical Properties | Back Directory | [Boiling point ]
555.9±60.0 °C(Predicted) | [density ]
1.82±0.1 g/cm3(Predicted) | [storage temp. ]
Hygroscopic, -20°C Freezer, Under inert atmosphere | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
Solid | [pka]
3.52±0.10(Predicted) | [color ]
White to Off-White |
| Hazard Information | Back Directory | [Uses]
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]
| [Uses]
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. | [in vivo]
JNJ-42041935 is used to compare the effect of selective inhibition of PHD to intermittent, high doses (50 μg/kg i.p.) of an exogenous erythropoietin receptor agonist in an inflammation induced anemia model in rats. JNJ-42041935 (100 μmol/kg, once a day for 14 days) is effective in reversing inflammation induced anemia, whereas erythropoietin has no effect. Administration of JNJ-42041935 (100 μmol/kg p.o.) for 5 consecutive days resulted in a 2-fold increase in reticulocytes, an increase in hemoglobin by 2.3 g/dl, and an increase in the hematocrit of 9%. Two hours after oral administration of 300 μmol/kg JNJ-42041935, the bioluminescence over the peritoneal area is increased by 2.2 ± 0.3-fold relative to luciferase-treated vehicle controls in the mouse [1]. | [storage]
Store at -20°C |
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