1-(6-chloro-5-trifluoromethoxy-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid manufacturers and suppliers

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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