Taspoglutide acetate  (Synonyms: ITM077 acetate; R1583 acetate; BIM51077 acetate)

Taspoglutide (R1583) acetate is an agonist of the glucagon-like peptide 1 receptor (GLP-1R) with an K_i value of 1.1 nM. Taspoglutide acetate induces cAMP accumulation in CHO-K1 cells expressing human GLP-1R (EC₅₀ = 0.06 nM). Taspoglutide acetate decreases blood levels of glucose and increases blood levels of insulin in a glucose tolerance test in Zucker diabetic obese rats. Taspoglutide acetate reduces blood levels of gastric inhibitory polypeptide (GIP), plasma levels of triglycerides, and body weight in the same model^[1][2].

3339.71 (free base)

C₁₅₂H₂₃₂N₄₀O₄₅.xC₂H₄O₂

1022150-16-8

His-{Aib}-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-{Aib}-Arg-NH2

H-{Aib}-EGTFTSDVSSYLEGQAAKEFIAWLVK-{Aib}-R-NH2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Dong JZ, et al. Discovery and characterization of taspoglutide, a novel analogue of human glucagon-like peptide-1, engineered for sustained therapeutic activity in type 2 diabetes. Diabetes Obes Metab. 2011 Jan;13(1):19-25.  [Content Brief]

  [2]. Sebokova E, et al. Taspoglutide, a novel human once-weekly analogue of glucagon-like peptide-1, improves glucose homeostasis and body weight in the Zucker diabetic fatty rat. Diabetes Obes Metab. 2010 Aug;12(8):674-82.  [Content Brief]