产品描述: | 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. |
靶点: |
GLP-1 receptor;GlucagonReceptor |
体外研究: |
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. |
体内研究: |
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. |
参考文献: |
1. Marso SP, et al. Semaglutide and Cardiovascular Outcomes in Patients with Type 2 Diabetes. N Engl J Med. 2016 Nov 10;375(19):1834-1844. 2. Zhang L, et al. Neuroprotective effects of the novel GLP-1 long acting analogue semaglutide in the MPTP Parkinson's disease mouse model. Neuropeptides. 2018 Oct;71:70-80. 3. Dhillon S, et al. Semaglutide: First Global Approval. Drugs. 2018 Feb;78(2):275-284. |
溶解性: |
Soluble in DMSO、H2O(用HCL 调节,pH≈1) |
保存条件: |
-20℃ |
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注意: |
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