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。

Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist developed for treatment of type 2 diabetes, with an EC 50 value of 0.06 nM.

Solid

EC50: 0.06 nM (GLP-1)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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 metf

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and lightPowder -80°C 2 years；-20°C 1 year

H-{Aib}-EGTFTSDVSSYLEGQAAKEFIAWLVK-{Aib}-R-NH2

His-{Aib}-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-{Aib}-Arg-NH2

[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.

In Vitro: DMSO : 50 mg/mL (14.97 mM; Need ultrasonic)配制储备液