Tirzepatide is a GIP-analogue that activates both the GLP-1 and GIP receptors. It was approved for improve blood-sugar control in adults with type 2 diabetes.
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描述 | Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are hormones involved in blood-sugar control. Tirzepatide is a GIP-analogue that activates both the GLP-1 and GIP receptors, leading to improved blood-sugar control. It is a linear polypeptide of 39 amino acids that has been chemically modified by lipidation to improve its uptake into cells and its stability to metabolism. In pharmacokinetic (PK) studies in healthy volunteers for doses ranging from 0.25 to 15 mg peak plasma concentration (Cmax), it was found to be dose proportional ranging between 26 and 874 ng/mL. The maximal concentration (Tmax) for tirzepatide was observed after 1–2 days of administration, and the mean half-life (T1/2) was found to be 116.7 h (i.e., 5 days), thus favoring a weekly dose regimen. It was approved for improve blood-sugar control in adults with type 2 diabetes[1]. |
作用机制 | Tirzepatide is an analogue of gastric inhibitory polypeptide (GIP), but has a greater affinity to GIP receptors than to GLP-1 receptors[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
0.21mL 0.04mL 0.02mL |
1.04mL 0.21mL 0.10mL |
2.08mL 0.42mL 0.21mL |
CAS号 | 2023788-19-2 |
分子式 | C225H348N48O68 |
分子量 | 4813.452 |
别名 | LY3298176 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 50 mg/mL(10.39 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |