Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TAK-875 Hemihydrate (Fasiglifam) 是一种选择性 GPR40 激动剂,EC50 为 14 nM,比油酸强 400 倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 5,970 | 6-8周 | ||
50 mg | ¥ 7,921 | 6-8周 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,935 | 6-8周 |
TAK-875 Hemihydrate 的其他形式现货产品:
产品描述 | TAK-875 Hemihydrate (Fasiglifam) is a selective GPR40 agonist with EC50 of 14 nM, 400-fold more potent than oleic acid. |
靶点活性 | FFA1/GPR40:14 nM(EC50) |
体外活性 | TAK-875 exhibits potent agonist activity and high binding affinity to the human GPR40 receptor with Ki of 38 nM. TAK-875 displays weaker affinity toward the rat GPR40 receptor with Ki of 140 nM. TAK-875 displays excellent selectivity, as TAK-875 has little agonist potency to other members of the FFA receptor family with EC50 of >10 μM. [1] TAK-875 treatment induces a concentration-dependent increase in intracellular IP production in CHO-hGPR40 with EC50 of 72 nM, more potently than that of endogenous ligand agonist oleic acid which requires much higher ligand concentrations to activate the receptor with EC50 of 29.9 μM. Neither TAK-875 nor oleic acid elicits an IP response in control CHO cells devoid of hGPR40. Consistent with the activation of the Gqα-mediated signaling pathway, TAK-875 augments glucose-dependent insulin secretion in pancreatic β cells. Prolonged stimulation of GPR40/FFA1 by TAK-875 does not cause pancreatic β Cell dysfunction or induction of apoptosis. [2] |
体内活性 | In a rat model of diabetes, single oral dosing of TAK-875 at 0.3-3 mg/kg reduces the blood glucose excursion and augments insulin secretion during an oral glucose tolerance test, when TAK-875 is administered 1 hour before an oral glucose challenge. [1] In type 2 diabetic N-STZ-1.5 rats, administration of TAK-875 (1-10 mg/kg p.o.) shows a clear improvement in glucose tolerance and augments insulin secretion. Additionally, TAK-875 (10 mg/kg, p.o.) significantly augments plasma insulin levels and reduces fasting hyperglycemia in male Zucker diabetic fatty rats, whereas in fasted normal Sprague-Dawley rats, TAK-875 neither enhances insulin secretion nor causes hypoglycemia even at 30 mg/kg. [2] |
别名 | TAK-875, Fasiglifam |
分子量 | 533.63 |
分子式 | C29H32O7S·1/2H2O |
CAS No. | 1374598-80-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: <1 mg/mL
DMSO: 93 mg/mL (174.3 mM)
H2O: <1 mg/mL
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.874 mL | 9.3698 mL | 18.7396 mL | 46.8489 mL |
5 mM | 0.3748 mL | 1.874 mL | 3.7479 mL | 9.3698 mL | |
10 mM | 0.1874 mL | 0.937 mL | 1.874 mL | 4.6849 mL | |
20 mM | 0.0937 mL | 0.4685 mL | 0.937 mL | 2.3424 mL | |
50 mM | 0.0375 mL | 0.1874 mL | 0.3748 mL | 0.937 mL | |
100 mM | 0.0187 mL | 0.0937 mL | 0.1874 mL | 0.4685 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。
TAK-875 Hemihydrate 1374598-80-7 Endocrinology/Hormones GPCR/G Protein GPR TAK-875 TAK875 TAK875 Hemihydrate Fasiglifam TAK 875 Hemihydrate TAK 875 Inhibitor inhibitor inhibit