1-(6-chloro-5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid suppliers
1-(6-chloro-5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid
- CAS:
- 1193383-09-3
- MF:
- C12H6ClF3N4O3
- MW:
- 346.65
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Properties
- 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
Safety Information
- Symbol(GHS)
GHS07
- Signal word
- Warning
- Hazard statements
- H302-H315-H319-H335
- Precautionary statements
- P261-P305+P351+P338
Use
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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