Bioactivity | Daprodustat (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor being developed for the treatment of anemia associated with chronic kidney disease. | ||||||||||||
Invitro | GSK1278863 is an orally administered small-molecule PHI, and stimulates endogenous EPO synthesis and induce effective erythropoiesis[1]. GSK1278863 has been shown to increase erythropoietin levels, leading to increases in hemoglobin, hematocrit and red blood cell numbers[2]. | ||||||||||||
Name | Daprodustat | ||||||||||||
CAS | 960539-70-2 | ||||||||||||
Formula | C19H27N3O6 | ||||||||||||
Molar Mass | 393.43 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Brigandi RA, et al. A Novel Hypoxia-Inducible Factor-Prolyl Hydroxylase Inhibitor (GSK1278863) for Anemia in CKD: A 28-Day, Phase 2A Randomized Trial. Am J Kidney Dis. 2016 Jun;67(6):861-71 [2]. Hara K, et al. Pharmacokinetics, pharmacodynamics and safety of single, oral doses of GSK1278863, a novel HIF-prolyl hydroxylase inhibitor, in healthy Japanese and Caucasian subjects. Drug Metab Pharmacokinet. 2015 Dec;30(6):410-8 |