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Taspoglutide

Catalog No. T13091 CAS 275371-94-3

Synonyms: R1583, BIM51077, ITM077

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

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Taspoglutide, CAS 275371-94-3

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Biological Description

Chemical Properties

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Description	Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist(EC50 value of 0.06 nM),and for treatment of type 2 diabetes
Targets&IC50	GLP1:（EC50）0.06 nM
In vitro	Taspoglutide (R1583/BIM51077), exhibiting 93% homology with native polypeptides, is a long-acting formulation of (Aib8-35) human GLP-1 (7-36 amides) that activates the GLP-1 receptor. It demonstrates an affinity constant (1.1±0.2 nM) towards the hGLP-1 receptor, closely mirroring the natural ligand’s affinity constant of 1.5±0.3 nM, and shows similar potency in stimulating cAMP production [2].
In vivo	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].

Synonyms	R1583, BIM51077, ITM077
Molecular Weight	3339.763
Formula	C152H232N40O45
CAS No.	275371-94-3

Storage

keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 28 mg/mL (8.38 mM)

References and Literature

1. 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. 2. Retterstol K, et al. Taspoglutide: a long acting human glucagon-like polypeptide-1 analogue. Expert Opin Investig Drugs. 2009 Sep;18(9):1405-11. 3. 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. 4. 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. 5. 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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Taspoglutide 275371-94-3 Others R 1583 R-1583 R1583 BIM 51077 ITM 077 BIM-51077 BIM51077 ITM-077 ITM077 inhibitor inhibit

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