Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Bempedoic acid (ETC1002) 是一种 ATP-柠檬酸裂解酶抑制剂,可激活AMPK。它是脂质和碳水化合物代谢的调节剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 287 | 现货 | ||
5 mg | ¥ 448 | 现货 | ||
10 mg | ¥ 663 | 现货 | ||
25 mg | ¥ 1,250 | 现货 | ||
50 mg | ¥ 2,230 | 现货 | ||
100 mg | ¥ 3,730 | 现货 | ||
500 mg | ¥ 7,880 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 493 | 现货 |
产品描述 | Bempedoic acid (ETC1002) is an orally available, once-daily LDL-C lowering small molecule designed to lower elevated levels of LDL-C and to avoid side effects associated with existing LDL-C lowering therapies. Bempedoic acid(ETC1002) is absorbed rapidly in the small intestine and enters the liver through cell surface receptors different from those transporters that selectively take up statins. Bempedoic acid(ETC1002) is a regulator of lipid and carbohydrate metabolism. |
体外活性 | ETC-1002是一种处于非活化状态的前体药物,在体内通过内源性肝脏ACS活性转化为ACL抑制剂(活化状态,ECT-1002-CoA).ETC-1002抑制硫胶质诱导的白血球向小鼠腹膜腔的迁移.ETC-1002可恢复饮食诱导型肥胖症的小鼠模型中脂肪AMPK活性,降低JNK磷酸化,减少巨噬细胞特异marker 4F/80的表达. |
体内活性 | TC-1002作用机制主要是靶向两种肝酶: 腺苷三磷酸-枸橡酸裂解酶(ACL)和腺苷酸活化蛋白激酶(AMPK),抑制甾醇和脂肪酸合成并促进线粒体长链脂肪酸的氧化。ETC-1002提高AMPK磷酸化水平,降低MAPKs的活性以及减少促炎细胞因子和趋化因子的产生。 |
激酶实验 | 7.5× compounds are added to a 96-well PolyPlate containing 60 μL of Buffer per well with substrates CoA (200 μM), ATP (400 μM), and [14C]citrate. Reaction is started with 4 μL (300 ng/well) ACL, and the plate is incubated at 37°C for 3 h. Th |
细胞实验 | Primary rat hepatocytes and differentiated human MDMs are treated with indicated concentrations of ETC-1002 for 12 h. Working solutions of ETC-1002 are prepared in serum-free RPMI 1640 containing 12 mM HEPES, 10,000 U/ml penicillin, and 100 μg/ml streptomycin. (Only for Reference) |
别名 | ETC1002, ESP-55016, ETC 1002, ETC-1002 |
分子量 | 344.49 |
分子式 | C19H36O5 |
CAS No. | 738606-46-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 63 mg/mL (182.9 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.9028 mL | 14.5142 mL | 29.0284 mL | 72.571 mL |
5 mM | 0.5806 mL | 2.9028 mL | 5.8057 mL | 14.5142 mL | |
10 mM | 0.2903 mL | 1.4514 mL | 2.9028 mL | 7.2571 mL | |
20 mM | 0.1451 mL | 0.7257 mL | 1.4514 mL | 3.6286 mL | |
50 mM | 0.0581 mL | 0.2903 mL | 0.5806 mL | 1.4514 mL | |
100 mM | 0.029 mL | 0.1451 mL | 0.2903 mL | 0.7257 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。
Bempedoic acid 738606-46-7 Chromatin/Epigenetic Metabolism PI3K/Akt/mTOR signaling ATP Citrate Lyase AMPK ESP 55016 inhibit Inhibitor ESP55016 AMP-activated protein kinase ETC1002 ACLY ESP-55016 ETC 1002 ETC-1002 inhibitor