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Daprodustat

Cat. No. M8924
Daprodustat Structure
Synonym:

GSK1278863

Size Price Availability Quantity
10mg USD 180 In stock
50mg USD 520 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Daprodustat (GSK1278863) is a novel, orally active HIF-prolyl hydroxylase inhibitor. It is developed for treatment of anemia associated with chronic kidney disease. GSK1278863 stimulates endogenous EPO synthesis and induce effective erythropoiesis. Daprodustat (GSK1278863) has been shown to increase erythropoietin levels, leading to increases in hemoglobin, hematocrit and red blood cell numbers.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 393.43
Formula C19H27N3O6
CAS Number 960539-70-2
Purity >99%
Solubility DMSO 10 mg/mL warmed
Storage at -20°C
References

A Novel Hypoxia-Inducible Factor-Prolyl Hydroxylase Inhibitor (GSK1278863) for Anemia in CKD: A 28-Day, Phase 2A Randomized Trial.
Brigandi RA, et al. Am J Kidney Dis. 2016 Jun;67(6):861-71. PMID: 26827289.

Pharmacokinetics, pharmacodynamics and safety of single, oral doses of GSK1278863, a novel HIF-prolyl hydroxylase inhibitor, in healthy Japanese and Caucasian subjects.
Hara K, et al. Drug Metab Pharmacokinet. 2015 Dec;30(6):410-8. PMID: 26643993.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Daprodustat, GSK1278863 supplier, HIF, inhibitors

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