Semaglutide Side Chain

Semaglutide is a once-daily glucagon-like peptide-1 analog that differs to others by the presence of an acyl group with a steric diacid at Lys26 and a large synthetic spacer and modified by the presence of a α-aminobutyric acid in position 8 which gives stability against the dipeptidylpeptidase-4.  It was developed by the Danish pharmaceutical company Novo Nordisk and FDA approved on December 5, 2017.

From the structure above,we can see PEG motif(AEEA-AEEA).Because ester protected AEEA is unstable, we usually provide AEEA as acid motif. AEEA-AEEA unit is quite importment, it will bind with albumin in sub-nano mole affinity,which is 500 fold increase from fatty acid alone.

SINOPEG is pleased to offer this C-18 fatty acid for your R&D and clinic research.

Reference:

1. Gotfredsen CF, etc: The human GLP-1 analogs liraglutide and semaglutide: absence of histopathological effects on the pancreas in nonhuman primates. Diabetes. 2014 Jul;63(7):2486-97;

2. Blundell J, etc: Effects of once-weekly semaglutide on appetite, energy intake, control of eating, food preference and body weight in subjects with obesity. Diabetes Obes Metab. 2017Sep;19(9):1242-1251;

3. Lee YS, etc: Anti-diabetic actions of glucagon-like peptide-1 on pancreatic beta-cells. Metabolism. 2014 Jan;63(1):9-19;

4. Jensen L, etc: Absorption, metabolism and excretion of the GLP-1 analogue semaglutide in humans and nonclinical species. Eur J Pharm Sci. 2017 Jun 15;104:31-41;

5. Barnett A. (2012). Type 2 diabetes (2nd ed.). Oxford.