FG-2216 (Synonyms:IOX3; YM311)
目录号 : KM7112 CAS No. : 223387-75-5 纯度 : 98%

FG-2216 (IOX3) 是一种有效和口服活性的 HIF 脯氨酰羟化酶-2 (PHD2) 抑制剂,IC50 值为 3.9 nM。FG-2216 在体内诱导促红细胞生成素生成和胎儿血红蛋白的表达。

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2mg
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5mg
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10mg
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25mg
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50mg
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100mg
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200mg 询价 In-stock
500mg 询价 In-stock
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生物活性

FG-2216 (IOX3) is a potent and orally active inhibitor of HIF prolyl hydroxylase-2 (PHD2), with an IC50 of 3.9 nM. FG-2216 induces robust erythropoietin and modest fetal hemoglobin in vivo.

体外研究

FG-2216 (50-100 μM; 24 h) stimulates erythropoietin (Epo) secretion by PHD2 inhibition in Hep3B cells.
FG-2216 (3-100 μM; 24 h) stabilizes HIF-1α and HIF-2α in Hep3B cells.

体内研究

FG-2216 (40-60 mg/kg; p.o. twice a week for 150 d) induces erythropoiesis and a small elevation of hemoglobin (HbF) expression, and is well tolerated in rhesus macaques.
FG-2216 (50 mg/kg; p.o. once daily for 4 or 12 d) increases hematocrit, red blood cell counts, and hemoglobin levels in mice.
FG-2216 (40-60 mg/kg; a single p.o) reversibly induces endogenous Epo in rhesus macaques.

Animal Model: Male rhesus macaques (3-6 years; 4-7 kg) mice are treated with large-volume phlebotomy with iron supplementation
Dosage: 40, 60 mg/kg
Administration: P.o. (40 mg/kg) twice a week for 6-8 weeks
P.o. (60 mg/kg) twice a week for 6-8 weeks
P.o. (60 mg/kg) twice a week for 6-8 weeks
Result: Exhibited reticulocytosis within 1-2 weeks of dosing.
Increased total hemoglobin levels at the end of the study duration.
分子式
C12H9ClN2O4
分子量
280.66
CAS号
223387-75-5
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 31 mg/mL (110.45 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5630 mL 17.8151 mL 35.6303 mL
5 mM 0.7126 mL 3.5630 mL 7.1261 mL
10 mM 0.3563 mL 1.7815 mL 3.5630 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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