FG2216

FG2216

Catalog Number:
L002371289APE
Mfr. No.:
APE-B5851
Price:
$276
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      • Overview
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          Background

          FG-2216 is a potent HIF-prolyl hydroxylase inhibitor. IC50 = 3.9 μM for PDH2 enzyme.
          HIFs (hypoxia inducible factors) are transcription factor that activated by low oxygen availability. It leads to cellular, tissue and organismal adaptive response to hypoxia. Increased hemoglobin
          levels are associated with intrauterine hypoxia. In cooperation with other transcriptional coactivators, HIF induces transcription of genes that ameliorate the effects of hypoxia, including erythropoietin and its receptor.
          In rhesus macaques, FG-2216 reversibly activates endogenous erythropoietin (82- to 309-fold at 60 mg/kg), and as early as 4 hours after oral administration of FG-2216, circulating plasma Epo levels increases. [1]
          Chronic administration of FG-2216 is well tolerated and induces erythropoiesis in rhesus macaques. It also induced a small elevation of hemoglobin expression in vivo. FG-2216–treated animals exerts rise in the percentage of hemoglobin-containing reticulocytes (% F+ retics) 1 to 2 weeks after chronic dosing began. [1]

      • Properties
        • Alternative Name
          (Z)-2-(((1-chloro-4-hydroxyisoquinolin-3-yl)(hydroxy)methylene)amino)acetic acid
          CAS Number
          223387-75-5
          Molecular Formula
          C12H9ClN2O4
          Molecular Weight
          280.66
          Appearance
          A solid
          Purity
          98.55%
          Solubility
          insoluble in H2O; ≥14.05 mg/mL in DMSO; ≥5.12 mg/mL in EtOH with ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

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