1022150-16-8
Chemical Structure
Taspoglutide acetate
Synonym(s): ITM077 acetate; R1583 acetate; BIM51077 acetate
- CAS No.: 1022150-16-8
- Formula:C152H232N40O45.xC2H4O2
- Molecular Weight:3339.71 (free base)
SMILES: N=C(NCCC[C@H](NC(C(C)(NC([C@@H](NC([C@@H](NC([C@@H](NC([C@H](CC1=CNC2=CC=CC=C12)NC([C@@H](NC([C@@H](NC([C@H](CC3=CC=CC=C3)NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(CNC([C@@H](NC([C@@H](NC([C@H](CC4=CC=C(O)C=C4)NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@H](CC5=CC=CC=C5)NC([C@@H](NC(CNC([C@@H](NC(C(C)(NC([C@H](CC6=CN=CN6)N)=O)C)=O)CCC(O)=O)=O)=O)[C@@H](C)O)=O)=O)[C@@H](C)O)=O)CO)=O)CC(O)=O)=O)C(C)C)=O)CO)=O)CO)=O)=O)CC(C)C)=O)CCC(O)=O)=O)=O)CCC(N)=O)=O)C)=O)C)=O)CCCCN)=O)CCC(O)=O)=O)=O)[C@H](CC)C)=O)C)=O)=O)CC(C)C)=O)C(C)C)=O)CCCCN)=O)C)=O)C(N)=O)N.CC(O)=O.[x]
Biological Activity: Taspoglutide (R1583) acetate is an agonist of the glucagon-like peptide 1 receptor (GLP-1R) with an Ki 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].
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Taspoglutide acetate | Taspoglutide (R1583) acetate is an agonist of the glucagon-like peptide 1 receptor (GLP-1R) with an Ki 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. | |||||||||||||||||||||
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- [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]
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