Taspoglutide (acetaat)

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].

1022150-16-8

ITM077 (acetate) ; R1583 (acetate) ; BIM51077 (acetate)

12352209

GLP Receptor

GPCR/G Protein

Metabolism-sugar/lipid metabolism

Metabolic Disease

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]

C152H232N40O45.xC2H4O2

3339.71 (free base)

[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.|[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.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-P0165B/

Peptides

Phase 3