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Semaglutide

CAS No. : 910463-68-2

產(chǎn)品活性：Semaglutide, a long-acting GLP-1 analogue, is a glucagon-like peptide-1 (GLP-1) receptor agonist. Semaglutide has the potential for type 2 diabetes treatment.

研究領(lǐng)域：GPCR/G Protein

作用靶點(diǎn)：GCGR

In Vitro: Semaglutide has two amino acid substitutions compared to human GLP-1 (Aib⁸, Arg³⁴) and is derivatized at lysine 26. The GLP-1R affinity of Semaglutide is 0.38±0.06 nM. Semaglutide is a GLP-1 analogue with 94% sequence omology to human GLP-1.

In Vivo: The plasma half-life of Semaglutide is 46h in mini-pigs following i.v. administration and semaglutide has an MRT of 63.6h after s.c. dosing to mini-pigs. Semaglutide improves 1-methyl-4-phenyl-1,2,3,6- tetrahydropyridine (MPTP)-induced motor impairments. In addition, Semaglutide rescues the decrease of tyrosine hydroxylase (TH) levels, alleviates the inflammation response, reduces lipid peroxidation, inhibits the apoptosis pathway, and also increases autophagy- related protein expression, to protect dopaminergic neurons in the substantia nigra and striatum. Moreover, the long-acting GLP-1 analogue semaglutide is superior to NN-2211 in most parameters.

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