HIF-PHD-IN-1

• CAT Number: I045759
• CAS Number: 1567657-46-8
• Molecular Formula: C17H12Cl2N6O3
• Molecular Weight: 419.22
• Purity: ≥95%
• Synonyms: 1-[1-[(1S)-1-(2,5-dichlorophenyl)ethyl]-7-oxo-6H-pyrazolo[4,3-d]pyrimidin-5-yl]pyrazole-4-carboxylic acid
• InChI: InChI=1S/C17H12Cl2N6O3/c1-8(11-4-10(18)2-3-12(11)19)25-14-13(6-21-25)22-17(23-15(14)26)24-7-9(5-20-24)16(27)28/h2-8H,1H3,(H,27,28)(H,22,23,26)/t8-/m0/s1
• InChIKey: BJMKDEGQDAVFGT-QMMMGPOBSA-N
• SMILES: CC(C1=C(C=CC(=C1)Cl)Cl)N2C3=C(C=N2)N=C(NC3=O)N4C=C(C=N4)C(=O)O

HIF-PHD-IN-1 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), with an IC50 of 54 nM for hHIF-PHD2. HIF-PHD-IN-1 is promising therapeutic agents for renal anemia[1].
HIF-PHD-IN-1 (compound 19) (0.5-2 mg/kg; p. o. once daily for 4 weeks) improves hemoglobin levels in anemic rats[1].
HIF-PHD-IN-1 (10 mg/kg; single p.o.) increases serum erythropoietin (EPO) concentration at 8 h after administration in SD rats[1].
HIF-PHD-IN-1 (1 mg/kg; p.o.) shows good bioavailability (F=77%) in male SD rats[1].

Reference

[1]. Goi T, et, al. Pyrazolo[4,3- d]pyrimidine Derivatives as a Novel Hypoxia-Inducible Factor Prolyl Hydroxylase Domain Inhibitor for the Treatment of Anemia. ACS Med Chem Lett. 2020 Jun 4; 11(7): 1416-1420.
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