Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 497 | 现货 | ||
2 mg | ¥ 739 | 现货 | ||
5 mg | ¥ 996 | 现货 | ||
10 mg | ¥ 1,890 | 现货 | ||
25 mg | ¥ 3,820 | 现货 | ||
50 mg | ¥ 5,570 | 现货 | ||
100 mg | ¥ 7,780 | 现货 | ||
500 mg | ¥ 15,600 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 996 | 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 shows the ability to stabilize HIF-α to stimulate EPO secretion. [1] |
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] |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 52 mg/mL (185.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.563 mL | 17.8152 mL | 35.6303 mL | 89.0758 mL |
5 mM | 0.7126 mL | 3.563 mL | 7.1261 mL | 17.8152 mL | |
10 mM | 0.3563 mL | 1.7815 mL | 3.563 mL | 8.9076 mL | |
20 mM | 0.1782 mL | 0.8908 mL | 1.7815 mL | 4.4538 mL | |
50 mM | 0.0713 mL | 0.3563 mL | 0.7126 mL | 1.7815 mL | |
100 mM | 0.0356 mL | 0.1782 mL | 0.3563 mL | 0.8908 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
FG-2216 223387-75-5 Chromatin/Epigenetic Metabolism HIF/HIF Prolyl-Hydroxylase IOX 3 fetal IOX3 inhibit HIFs Hypoxia-inducible factors prolyl YM-311 IOX-3 FG2216 erythropoietin HIF-PH YM311 hydroxylase hemoglobin FG 2216 PHD2 YM 311 HIF Inhibitor inhibitor