keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist(EC50 value of 0.06 nM),and for treatment of type 2 diabetes
产品描述 | Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist(EC50 value of 0.06 nM),and for treatment of type 2 diabetes |
靶点活性 | GLP1:(EC50)0.06 nM |
体外活性 | Taspoglutide (R1583/BIM51077) with 93% homology with the native polypeptide, and is a long acting 10% formulation of (Aib8-35) human GLP-1 (7-36 amides) . It activates the GLP-1 receptor. Taspoglutide has comparable affinity (affinity constant 1.1±0.2 nM) to the natural ligand affinity constant 1.5±0.3 nM for the hGLP-1 receptor and exhibits comparable potency in stimulating cAMP production[2]. |
体内活性 | The rate of glucose-induced insulin secretion from isolated enhanced by Taspoglutide, cultured rat islets and the perfused ZDF rat pancreas. Taspoglutide showed dose-dependent enhancement of glucose-dependent insulin release in Sprague-Dawley rats and diabetic db/db mice, thereby reducing blood glucose in the type 2 diabetic db/db mouse model[3]. Acute treatment with taspoglutide reduces glucose excursion and increased insulin response during oGTT. In chronically treated rats, glucose excursion and levels of GIP, PYY and triglycerides during oGTT on day 21 are significantly reduced[4]. Hepatic triglyceride levels are significantly reduced in livers from taspoglutide-treated. Taspoglutide does not reduce plaque area or lipid content in the aortic arch or abdominal aorta, and no significant change in aortic macrophage accumulation is detected after taspoglutide or metformin mice[5]. |
别名 | R1583, BIM51077, ITM077 |
分子量 | 3339.763 |
分子式 | C152H232N40O45 |
CAS No. | 275371-94-3 |
keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 28 mg/mL (8.38 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 0.2994 mL | 1.4971 mL | 2.9942 mL | 7.4856 mL |
5 mM | 0.0599 mL | 0.2994 mL | 0.5988 mL | 1.4971 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。
Taspoglutide 275371-94-3 Others R 1583 R-1583 R1583 BIM 51077 ITM 077 BIM-51077 BIM51077 ITM-077 ITM077 Inhibitor inhibitor inhibit