HIF-PHD Inhibitor II; JNJ-42041935

Code: 400093-10MG D2-231

General description

A cell-permeable benzimidazolopyrazole compound that acts as an active-site binding, iron insensitive, 2-oxoglutarate competitive, reversible and potent i...


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Your Price
€307.49 10MG
Discontinued
€378.21 inc. VAT

General description

A cell-permeable benzimidazolopyrazole compound that acts as an active-site binding, iron insensitive, 2-oxoglutarate competitive, reversible and potent inhibitor of PHD1, 2 and 3 isozymes (pKi = 7.91, 7.29 and 7.65, respectively). Displays >100-fold selectivity over FIH (factor inhibiting hydroxylase; pIC50 ~ 4) and minimal affinity towards a panel of receptors, enzymes and kinases. Shown to elevate HIF-1α levels in Hep3B cells and stimulate erythropoietin secretion in mice, and reverse inflammation-induced anemia in rats (100 µM/kg). Shown to inhibit malate dehydrogenase 2 (MDH2) activity and suppress mitochondrial respiration.

A cell-permeable benzimidazolopyrazole compound that acts as an active-site binding, iron insensitive, 2-oxoglutarate competitive, reversible and potent inhibitor of PHD1, 2 and 3 isozymes (pKi = 7.91, 7.29 and 7.65, respectively). Displays >100-fold selectivity over FIH (factor inhibiting hydroxylase; pIC50 ~ 4) and minimal affinity towards a panel of receptors, enzymes and kinases. Shown to elevate HIF-1α levels in Hep3B cells and stimulate erythropoietin secretion in mice, and reverse inflammation-induced anemia in rats (100 µM/kg).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Lee, K., et al., 2013. Angew. Chem. Int. Ed.52, In press.Barrett, T.D., et al. 2011. Mol. Pharmacol.79, 910.Rosen, M.D., et al. 2010. ACS Med. Chem. Lett. 1, 526.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)

assay≥99% (HPLC)
colorwhite
formsolid
manufacturer/tradenameCalbiochem®
Quality Level100
shipped inambient
SMILES stringClC1=CC2=C(NC(N3C=C(C=N3)C(O)=O)=N2)C=C1OC(F)(F)F
solubilityDMSO: 100 mg/mL
storage conditionprotect from light, OK to freeze
storage temp.2-8°C
Cas Number1193383-09-3
This product has met the following criteria to qualify for the following awards:



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