Daprodustat

Daprodustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 1 (HIF-PH1), HIF-PH2, and HIF-PH3 (IC50s = 3.5, 22.2, 5.5 nM, respectively). It is selective for HIF-PH1, -2, and -3 over factor-inhibiting HIF (FIH) and collagen prolyl hydroxylase (CP4H, IC50s = 9,800 and >200,000 nM, respectively). Daprodustat (25 and 50 µM) induces accumulation of HIF-1alpha and HIF-2alpha in Hep3B cells. In vivo, daprodustat (60 mg/kg) increases plasma levels of erythropoietin (EPO) in mice. It increases the number of reticulocytes and levels of hemoglobin in mice when administered at doses of 3, 10, and 30 mg/kg.Formal Name: N-[(1,3-dicyclohexylhexahydro-2,4,6-trioxo-5-pyrimidinyl)carbonyl]-glycine. CAS Number: 960539-70-2. Synonyms: GSK1278863. Molecular Formula: C19H27N3O6. Formula Weight: 393.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMSO: 3 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 1 mg/ml. lambdamax: 210, 265 nm. SMILES: O=C(N(C(C1C(NCC(O)=O)=O)=O)C2CCCCC2)N(C3CCCCC3)C1=O. InChi Code: InChI=1S/C19H27N3O6/c23-14(24)11-20-16(25)15-17(26)21(12-7-3-1-4-8-12)19(28)22(18(15)27)13-9-5-2-6-10-13/h12-13,15H,1-11H2,(H,20,25)(H,23,24). InChi Key: RUEYEZADQJCKGV-UHFFFAOYSA-N.