An orally active PHD2 inhibitor (IC50 = 3.9 µM); stabilizes HIF-α and reversibly stimulate erythropoietin secretion at 100 µM in vitro; increases hematocrit

FG-2216 – 10 mg

Brand:
Cayman
CAS:
223387-75-5
Storage:
-20
UN-No:
Non-Hazardous - /

Hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) enzymes act as central gatekeepers of post-transcriptional and transcriptional adaptation to hypoxia, oxidative stress, and excitotoxicity. FG-2216 is an orally active PHD2 inhibitor (IC50 = 3.9 µM) that stabilizes HIF-α.{30802} It has been shown to reversibly stimulate erythropoietin secretion at 100 µM in vitro and to increase hematocrit, red blood cell count, and hemoglobin levels at 50 mg/kg in mice.{30802,25021}  

 

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Description

An orally active PHD2 inhibitor (IC50 = 3.9 µM); stabilizes HIF-α and reversibly stimulate erythropoietin secretion at 100 µM in vitro; increases hematocrit, red blood cell count, and hemoglobin levels at 50 mg/kg in mice ,

Formal name: N-[(1-chloro-4-hydroxy-3-isoquinolinyl)carbonyl]-glycine

Synonyms:  IOX3|YM-311

Molecular weight: 280.7

CAS: 223387-75-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors

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