Sermaglutide

GLP-1 receptor

His-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-N6-[N-(17-carboxy-1-oxoheptadecyl-L-γ-glutamyl[2-(2-aminoethoxy)ethoxy] acetyl[2-(2-aminoethoxy) ethoxy]acetyl]-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly-OH

4113.64

H2O : 3.85 mg/mL (0.94 mM; ultrasonic and adjust pH to 1 with 1 M HCL)
DMSO : 5 mg/mL (1.22 mM; ultrasonic and warming and heat to 60°C)

powder

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[1]. Semaglutide is a GLP-1 analogue with 94% sequence omology to human GLP-1.

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 liraglutide in most parameters. Semaglutide lowers blood glucose by stimulating the release of insulin and also lowers body weight.

索玛鲁肽；司美格鲁肽

C₁₈₇H₂₉₁N₄₅O₅₉

910463-68-2