BIQ
中文名称 | BIQ |
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中文同义词 | [[(1-氯-4-羟基异喹啉-3-基)羰基]氨基]乙酸;2-(1-氯-4-羟基异喹啉-3-甲酰氨基)乙酸;2-(1-氯-4-羟基异喹啉-3-甲酰胺)乙酸;化合物FG-2216;FG-2216 游离;2-(1-氯-4-羟基异喹啉-3-甲酰胺基)乙酸 |
英文名称 | FG 2216 |
英文同义词 | FG 2216;FG2216;FG-2216;[[(1-Chloro-4-hydroxyisoquinolin-3-yl)carbonyl]amino]acetic acid;FG 2216 (erythropoietic agent);YM 311;(Z)-2-(((1-CHLORO-4-HYDROXYISOQUINOLIN-3-YL)(HYDROXY)METHYLENE)AMINO)ACETIC ACID;N-[(1-Chloro-4-hydroxy-3-isoquinolinyl)carbonyl]glycine |
CAS号 | 223387-75-5 |
分子式 | C12H9ClN2O4 |
分子量 | 280.66 |
EINECS号 | |
相关类别 | 小分子抑制剂,天然产物;小分子抑制剂;Inhibitors |
Mol文件 | 223387-75-5.mol |
结构式 |
BIQ 性质
沸点 | 670.6±55.0 °C(Predicted) |
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密度 | 1.571±0.06 g/cm3(Predicted) |
储存条件 | -20°C |
溶解度 | 不溶于水; DMSO 中≥14.05 mg/mL; ≥5.12 mg/mL,乙醇溶液,超声波 |
形态 | 粉末 |
酸度系数(pKa) | 3.20±0.10(Predicted) |
颜色 | 白色至米色 |
Target | Value |
PHD2
(Cell-free assay) | 3.9 μM |
在雄性恒河猴中,FG-2216 (60 mg/kg, p.o.)诱导显著且可逆的Epo诱导,并诱导HbF表达小幅增高。
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. |
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/08/19 | HY-15641 | BIQ FG-2216 | 223387-75-5 | 2mg | 900元 |
2024/08/19 | HY-15641 | BIQ FG-2216 | 223387-75-5 | 5 mg | 1300元 |