daprodustat,GSK1278863 Chemical Properties

Melting point:

237-241oC

Density 

1.359±0.06 g/cm3(Predicted)

storage temp. 

Refrigerator

solubility 

Chloroform (Slightly), DMSO (Slightly)

pka

3.44±0.10(Predicted)

form 

Solid

color 

White to Off-White

daprodustat,GSK1278863 Usage And Synthesis

Uses

Daprodustat is a novel HIF (Hypoxia inducible factor)-prolyl hydroxylase inhibitor.

Biological Activity

daprodustat (gsk1278863) is a hif-prolyl hydroxylase inhibitor.hypoxia stimulates erythropoietin (epo) release through accumulation of hypoxia-inducible factor 1α (hif-1α), resulting in an increase of erythrocyte production by the bone marrow. hif-prolyl hydroxylase inhibitors have been used to selectively activate the phd-signaling pathway, leading to the stabilization of hifα subunits, which can affect the transcription of hif-responsive genes.

in vitro

in-vitro biotransformation data indicated that gsk1278863 was primarily metabolized by cyp2c8 [1].

References

[1] hara k,takahashi n,wakamatsu a,caltabiano s. 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.
[2] brigandi ra,johnson b,oei c,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.

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