A selective inhibitor of HIF-PH enzymes
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JNJ-42041935

Item No. 14316

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 10 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    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).1 It is >100-fold selective for HIF-PH compared to the related FIH (factor-inhibiting HIF) and a panel of various other enzymes.1 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.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Barrett, T.D., Palomino, H.L., Brondstetter, T.I., et al. Pharmacological characterization of 1-(5-chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (JNJ-42041935), a potent and selective hypoxia-inducible factor prolyl hydroxylase inhibitor. Mol. Pharmacol. 79(6), 910-920 (2011).