Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Elafibranor (GFT505) 是过氧化物酶体增殖物激活受体-α (PPAR-α) 和过氧化物酶体增殖物激活受体-δ (PPAR-δ) 的激动剂,EC50 值分别为 45 和 175 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 243 | 现货 | ||
5 mg | ¥ 538 | 现货 | ||
10 mg | ¥ 783 | 现货 | ||
25 mg | ¥ 1,810 | 现货 | ||
50 mg | ¥ 2,880 | 现货 | ||
100 mg | ¥ 4,260 | 现货 | ||
500 mg | ¥ 8,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 593 | 现货 |
产品描述 | Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor-α (PPAR-α) and peroxisome proliferator-activated receptor-δ (PPAR-δ) with EC50 values of 45 and 175 nM, respectively. |
靶点活性 | PPARα:45 nM (EC50), PPARδ:175 nM (EC50) |
体外活性 | GFT505 is being developed as a dual PPAR-α/PPAR-δ agonist for the treatment of T2DM and non-alcoholic fatty liver disease. GFT505 has an active metabolite, GFT1007, and both have potent agonist activity for PPAR-α and to a lesser extent for PPAR-δ |
体内活性 | GFT505 improves insulin sensitivity and early studies indicate it may be useful in non-alcoholic fatty liver disease which is being tested in a Phase IIb study. Elafibranor is well tolerated and does not cause weight gain or cardiac events, but does produce a mild, reversible increase in serum creatinine. Elafibranor improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation. GFT505 treatment improves glucose control and plasma lipids in diabetic db/db mice. A significant dose-dependent reduction of hepatic expression of the key gluconeogenic enzymes glucose 6-phosphatase (G6Pase), PEPCK, and fructose 1,6-bisphosphatase 1 (FBP1) is observed with GFT505. GFT505 does not induce cardiac adverse effects of PPARγ-activating agonists in monkeys |
别名 | GFT505 |
分子量 | 384.49 |
分子式 | C22H24O4S |
CAS No. | 923978-27-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (130.04 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6008 mL | 13.0042 mL | 26.0085 mL | 65.0212 mL |
5 mM | 0.5202 mL | 2.6008 mL | 5.2017 mL | 13.0042 mL | |
10 mM | 0.2601 mL | 1.3004 mL | 2.6008 mL | 6.5021 mL | |
20 mM | 0.13 mL | 0.6502 mL | 1.3004 mL | 3.2511 mL | |
50 mM | 0.052 mL | 0.2601 mL | 0.5202 mL | 1.3004 mL | |
100 mM | 0.026 mL | 0.13 mL | 0.2601 mL | 0.6502 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。
Elafibranor 923978-27-2 DNA Damage/DNA Repair Metabolism PPAR inhibit GFT-505 Peroxisome proliferator-activated receptors GFT 505 GFT505 Inhibitor inhibitor