JNJ-42041935

JNJ-42041935 is a selective, 2-OG competitive, and reversible inhibitor of HIF-PH enzymes (pKis = 12.3, 51.3, and 22.4 nM for HIF-PH1, HIF-PH2, and HIF-PH3, respectively). It is >100-fold selective for HIF-PH 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.Formal Name: 1-[6-chloro-5-(trifluoromethoxy)-1H-benzimidazol-2-yl]-1H-pyrazole-4-carboxylic acid. CAS Number: 1193383-09-3. Synonyms: HIF-PHD Inhibitor II. Molecular Formula: C12H6ClF3N4O3. Formula Weight: 346.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 10 mg/ml. lambdamax: 252, 302 nm. SMILES: ClC1=CC2=C(NC(N3C=C(C(O)=O)C=N3)=N2)C=C1OC(F)(F)F. InChi Code: InChI=1S/C12H6ClF3N4O3/c13-6-1-7-8(2-9(6)23-12(14,15)16)19-11(18-7)20-4-5(3-17-20)10(21)22/h1-4H,(H,18,19)(H,21,22). InChi Key: FXHHASJVTYRJHH-UHFFFAOYSA-N.