Taspoglutide, Inhibitor

Taspoglutide

Cat. Num. AAA5754014

• Purity: 98.00%
• Synonyms: Taspoglutide; ITM077; R1583; BIM51077; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 28mg/mL (8.38mM); (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C152H232N40O45
• SMILES: [H-{Aib}-EGTFTSDVSSYLEGQAAKEFIAWLVK-{Aib}-R-NH2]
• CAS Number: 275371-94-3
• Target & IC50: GLP-1: ic50 0.06nM (EC50)
• In Vitro: The rate of glucose-induced insulin secretion from isolated enhanced by Taspoglutide, cultured rat islets and the perfused ZDF rat pancreas. Taspoglutide showed dose-dependent enhancement of glucose-dependent insulin release in Sprague-Dawley rats and diabetic db/db mice, thereby reducing blood glucose in the type 2 diabetic db/db mouse model[3]. Acute treatment with taspoglutide reduces glucose excursion and increased insulin response during oGTT. In chronically treated rats, glucose excursion and levels of GIP, PYY and triglycerides during oGTT on day 21 are significantly reduced[4]. Hepatic triglyceride levels are significantly reduced in livers from taspoglutide-treated. Taspoglutide does not reduce plaque area or lipid content in the aortic arch or abdominal aorta, and no significant change in aortic macrophage accumulation is detected after taspoglutide or metformin mice[5].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Related Product Information for Taspoglutide, inhibitor

Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist(EC50 value of 0.06nM), and for treatment,of type 2 diabetes

References

Sebokova E, et al. Taspoglutide, an analog of human glucagon-like Peptide-1 with enhanced stability and in vivo potency. Endocrinology. 2010 Jun;151(6):2474-82.
Sebokova E, et al. Taspoglutide, an analog of human glucagon-like Peptide-1 with enhanced stability and in vivo potency. Endocrinology. 2010 Jun;151(6):2474-82.
Retterstol K, et al. Taspoglutide: a long acting human glucagon-like polypeptide-1 analogue. Expert Opin Investig Drugs. 2009 Sep;18(9):1405-11.
Retterstol K, et al. Taspoglutide: a long acting human glucagon-like polypeptide-1 analogue. Expert Opin Investig Drugs. 2009 Sep;18(9):1405-11.
Nauck MA, et al. treatment,with the human once-weekly glucagon-like peptide-1 analog taspoglutide in combination with metformin improves glycemic control and lowers body weight in patients with type 2 diabetes inadequately controlled with metformin alone: a double-blind placebo-controlled study. Diabetes Care. 2009 Jul;32(7):1237-43.
Nauck MA, et al. treatment,with the human once-weekly glucagon-like peptide-1 analog taspoglutide in combination with metformin improves glycemic control and lowers body weight in patients with type 2 diabetes inadequately controlled with metformin alone: a double-blind placebo-controlled study. Diabetes Care. 2009 Jul;32(7):1237-43.
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.
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.
Panjwani N, et al. GLP-1 receptor activation indirectly reduces hepatic lipid accumulation but does not attenuate development of atherosclerosis in diabetic male ApoE(-/-) mice. Endocrinology. 2013 Jan;154(1):127-39.
Panjwani N, et al. GLP-1 receptor activation indirectly reduces hepatic lipid accumulation but does not attenuate development of atherosclerosis in diabetic male ApoE(-/-) mice. Endocrinology. 2013 Jan;154(1):127-39.