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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。
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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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 298 | 现货 | |
5 mg | ¥ 598 | 现货 | |
10 mg | ¥ 1,130 | 现货 | |
25 mg | ¥ 2,290 | 现货 | |
50 mg | ¥ 3,330 | 现货 | |
100 mg | ¥ 4,660 | 现货 | |
200 mg | ¥ 6,290 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 598 | 现货 |
产品描述 | 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. |
靶点活性 | PHD2:3.9 μM |
体外活性 | FG-2216 展现出稳定 HIF-α 以刺激 EPO 分泌的能力。[1] |
体内活性 | 在雄性恒河猴中,FG-2216(60 mg/kg,口服)可显著且可逆地诱导Epo产生,并引起HbF表达的小幅提升。[2] |
激酶实验 | Metabolic Labeling and Gel Electrophoresis: COLO 320DM cells (200,000) are injected into each well of 12-well plastic plates 2 days before incubation in the presence of KNK437 for 1 h before heat shock. The cells are then heat-shocked at 42°C for 90 min or kept at 37°C for the same length of time and incubated at 37°C for 2 h. For metabolic labeling, cells are washed with PBS without Ca2+ or Mg2+ and incubated for 1 h with 1.22 MBq of [35S]methionine in 250 μL of methionine-free DMEM supplemented with 10% dialyzed fetal bovine serum. After metabolic labeling, cells are washed twice with PBS and lysed in a buffer containing 1% NP40, 0.15 M NaCl, 50 mM Tris-HCl (pH 8.0), 5 mM EDTA, and protease inhibitors [0.2 mM 4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride, 2 mM N-ethylmaleimide, 1 μg/mL pepstatin, and 1 μg/mL leupeptin]. After centrifugation at 12,000×g for 20 min, cell extracts containing equal amounts of trichloroacetic acid-insoluble radioactivity are analyzed by two-dimensional gel electrophoresis (the one-dimensional gel electrophoresis is a nonequilibrium pH gradient gel electrophoresis, and the two-dimensional gel electrophoresis is 10% SDS-PAGE). |
别名 | YM-311, FG2216, FG 2216 |
分子量 | 280.66 |
分子式 | C12H9ClN2O4 |
CAS No. | 223387-75-5 |
Smiles | OC(=O)CNC(=O)c1nc(Cl)c2ccccc2c1O |
密度 | 1.571 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 50 mg/mL (178.15 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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