FG-4592 (ASP1517)

FG-4592 (ASP1517)

Catalog Number:
L002369080APE
Mfr. No.:
APE-A4187
Price:
$188
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      • Overview
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          Background

          FG-4592 (also known as ASP1517), 2-(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxamido)acetic acid, is a potent small molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH), an enzyme up-regulating the expression of endogenous human erythropoietin (Epo). It is currently being investigated as an oral treatment for anemia associated with chronic kidney disease (CKD). Unlike other anemia treating agents, erythropoiesis-stimulating agents (ESAs), FG-4592 inhibits HIF, through a distinctive mechanism, by stabilization of HIF. According to previous studies, FG-4592 is capable of correcting and maintaining hemoglobin levels in CKD patients not receiving dialysis and in patients of end-stage renal disease who receives dialysis but do not need intravenous iron supplement.

      • Properties
        • Alternative Name
          2-[(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)amino]acetic acid
          CAS Number
          808118-40-3
          Molecular Formula
          C19H16N2O5
          Molecular Weight
          352.34
          Appearance
          A solid
          Purity
          99.62%
          Solubility
          insoluble in H2O; ≥17.62 mg/mL in DMSO; ≥2.9 mg/mL in EtOH with gentle warming and ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Nicholson HE, Tariq Z, et al. "HIF-independent synthetic lethality between CDK4/6 inhibition and VHL loss across species." Sci Signal. 2019 Oct 1;12(601). pii: eaay0482. PMID:31575731
          2. LUKE ERBER. "Functional Proteomics Analysis To Discover And Characterize Oxygen-Dependent Cellular Pathways." UNIVERSITY OF MINNESOTA. 2019.
          3. Kiriakidis S, Hoer SS, et al. "Complement C1q is hydroxylated by collagen prolyl 4 hydroxylase and is sensitive to off-target inhibition by prolyl hydroxylase domain inhibitors that stabilize hypoxia-inducible factor." Kidney Int. 2017 May 12. pii: S0085-2538(17)30180-1. PMID:28506759

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