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Daprodustat

Cat. No. M8924
Daprodustat Structure
Synonym:

GSK1278863

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 80  USD80 In stock
10mg USD 130  USD130 In stock
25mg USD 220  USD220 In stock
50mg USD 380  USD380 In stock
100mg USD 550  USD550 In stock
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Quality Control & Documentation
Biological Activity

Daprodustat (GSK1278863) is a novel, first-in-class, orally active inhibitor of hypoxia-induced factor prolyl hydroxylase (HIF-PHI). Reversible inhibition of HIF-PHD activity under normal partial oxygen pressure can temporarily inhibit HIF-α degradation and promote the expression of related hypoxia metabolism genes.

Chemical Information
Molecular Weight 393.43
Formula C19H27N3O6
CAS Number 960539-70-2
Solubility (25°C) DMSO 16 mg/mL (ultrasonic and warming)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Brigandi RA, et al. Am J Kidney Dis. A Novel Hypoxia-Inducible Factor-Prolyl Hydroxylase Inhibitor (GSK1278863) for Anemia in CKD: A 28-Day, Phase 2A Randomized Trial.

[2] Hara K, et al. Drug Metab Pharmacokinet. Pharmacokinetics, pharmacodynamics and safety of single, oral doses of GSK1278863, a novel HIF-prolyl hydroxylase inhibitor, in healthy Japanese and Caucasian subjects.

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Keywords: Daprodustat, GSK1278863 supplier, HIF, inhibitors, activators


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