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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
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议

产品介绍
FG2216 (IOX3) 是一种有效的、具有口服活性的 HIF 脯氨酰羟化酶 2 (PHD2) 抑制剂,IC50 为 3.9 μM。
Cas No.223387-75-5
别名IOX3; YM311
化学名(Z)-2-(((1-chloro-4-hydroxyisoquinolin-3-yl)(hydroxy)methylene)amino)acetic acid
Canonical SMILESClC1=NC(/C(O)=N/CC(O)=O)=C(O)C2=CC=CC=C21
分子式C12H9ClN2O4
分子量280.66
溶解度≥ 14.05mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.