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FG2216
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
FG2216图片
CAS NO:223387-75-5
规格:98%
分子量:280.66
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍
HIF-prolyl hydroxylase inhibitor
CAS:223387-75-5
分子式:C12H9ClN2O4
分子量:280.66
纯度:98%
存储:Store at -20°C

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]


Reference:
1.  Hsieh MM, Linde NS, Wynter A et al. HIF prolyl hydroxylase inhibition
results in endogenous erythropoietin induction, erythrocytosis, and modest fetal
hemoglobin expression in rhesus macaques.  Blood. 2007 Sep 15;110(6):2140-7.