FG-2216

FG-2216 (YM-311) 是一种有效的、口服具有活力的HIF 脯氨酰羟化酶-2 (PHD2) 抑制剂,IC50=3.9 nM。它在体内能够诱导促红细胞生成素生成和胎儿血红蛋白的表达。

CAS号

223387-75-5

分子式

C12H9ClN2O4

主要靶点

HIF/HIF Prolyl-Hydroxylase

仅限科研使用

Cat No : CM04465

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Synonyms

YM-311|FG2216|FG 2216



产品信息

FG-2216 (YM-311) is a potent HIF-prolyl hydroxylase inhibitor for the PDH2 enzyme (IC50: 3.9 uM); orally bioavailable and induced reversible and significant Epo induction in vivo.

CAS号 223387-75-5
分子式 C12H9ClN2O4
主要靶点 HIF/HIF Prolyl-Hydroxylase
主要通路 表观遗传|代谢
分子量 280.66
纯度 99.00%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 YM-311|FG2216|FG 2216

靶点活性

PHD2:3.9 μM

体内活性

In male rhesus macaques, FG-2216 (60 mg/kg, p.o.), induces significant and reversible Epo induction, and induces a small elevation of HbF expression. [2]

体外活性

FG-2216 shows the ability to stabilize HIF-α to stimulate EPO secretion. [1]

溶解度

H2O:<1 mg/mL,DMSO:52 mg/mL (185.3 mM),Ethanol:<1 mg/mL

参考文献

1.Hong YR, et al. Bioorg Med Chem Lett. 2013, 23(21), 5953-5957.
2.Hsieh MM, et al. Blood. 2007, 110(6), 2140-2147.

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