生物活性 | |||
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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]. |
实验方案 | |||
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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 |
参考文献 |
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