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CAS No. : 275371-94-3
MCE 国际站:Taspoglutide
产品活性:Taspoglutide是长效 GLP-1 受体激动剂, EC50值为0.06 nM,可用于 2 型糖尿病的相关研究。
研究领域:GPCR/G Protein
作用靶点:GCGR
In Vitro: Taspoglutide (R1583/BIM51077) is a long acting 10% formulation of (Aib8-35) human GLP-1 (7-36 amides) with 93% homology with the native polypeptide. It activates the GLP-1 receptor. Taspoglutide has comparable affinity (affinity constant 1.1±0.2 nM) to the natural ligand (affinity constant 1.5±0.3 nM) for the hGLP-1 receptor and exhibits comparable potency in stimulating cAMP production.
In Vivo: Taspoglutide has been shown to enhance the rate of glucose-induced insulin secretion from isolated, cultured rat islets and the perfused ZDF rat pancreas. Taspoglutide in Sprague-Dawley rats and diabetic db/db mice have shown a dose-related enhancement of glucose-dependent insulin release, which lower blood glucose in the db/db mouse model of type 2 diabetes. 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. 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.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Anti-diabetic Compound Library | Peptide Library | Protein-protein Interaction Inhibitor Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Dulaglutide | PF-06291874 | Neuropeptide Y, porcine | HAEGTFTSDVS | Glucagon receptor antagonists-5 | Oxyntomodulin TFA | Tirzepatide TFA | Liraglutide | GLP-1R agonist 1 | Exendin-4 acetate | GLP-1(7-37) acetate | Glucagon (1-29), bovine, human, porcine | GPCR modulator-1 | Oxyntomodulin (swine) | VU0453379 | Cotadutide | Elsiglutide | GLP-1 receptor agonist 7 | Exendin(9-39) amide | Glucagon-like peptide 1 (1-37), human TFA | Semaglutide TFA | Retatrutide acetate | GLP-1R modulator C5 | Glucagon (19-29), human | [Des-His1,Glu9]-Glucagon amide TFA | FC382K10W15 TFA | Exendin-3/4 (59-86) | FTSDVSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
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