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Semaglutide (Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217) is a long-acting human GLP-1 analog, it is also a GLP-1 receptor agonist with the potential for the treatment of type 2 diabetes mellitus (T2DM). 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 (0.38 ± 0.06 nM) is three-fold decreased compared to liraglutide, whereas the albumin affinity is increased.
In vivo, the plasma half-life is 46.1 h in mini-pigs following i.v. administration, and semaglutide has an MRT of 63.6 h after s.c. dosing to mini-pigs.
| Cell Experiment | |
|---|---|
| Cell lines | SH-SY5Y cell |
| Preparation method | For selecting an adaptive concentration of Aβ25-35 the cells were respectively treated with different concentrations of Aβ25-35 (0, 10, 20, 30, 40 μmol/L). More obvious cytotoxicity was seen in cells treated by 20, 30, 40 µM Aβ25-35. Concentration of 20 µM Aβ25-35 was selected in continuing experimental study. The cells, which were treated with 20 µM Aβ25-35, were further treated with different concentrations of semaglutide (0, 5, 10, 15 nmol/L). |
| Concentrations | 0, 5, 10, 15 nmol/L |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | Male C57BL/6J mice |
| Formulation | Not mentioned |
| Dosages | 0.1 mg/kg |
| Administration | i.p. |
| Molecular Weight | 4113.58 |
| Formula | C187H291N45O59 |
| CAS Number | 910463-68-2 |
| Solubility (25°C) | DMSO 1 mg/mL Water (pH=7) 1 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related GLP Receptor Products |
|---|
| Dulaglutide (Activated main chain)
Dulaglutide (Activated main chain) is a glucagon-like peptide-1 receptor agonist (GLP-1 agonist) consisting of GLP-1(7-37) covalently linked to an Fc fragment of human IgG4. |
| Shanzhiside-methylester
Shanzhiside Methyl ester was isolated from Lactobacillus rotaformis. Shanzhiside Methyl ester, a small molecule glucagon-like peptide 1 (GLP-1 receptor) agonist, has the ability to induce anti-abnormal pain tolerance. |
| Tirzepatide hydrochloride
Tirzepatide Hydrochloride is a glucose-dependent insulin-stimulating peptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. |
| PF-07081532
PF-07081532 is a next-generation orally active GLP-1 receptor agonist. |
| BETP
BETP is an agonist of glucagon-like peptide-1 (GLP-1) receptor, with EC50s of 0.66 and 0.755 μM for human and rat GLP-1 receptor, respectively. |
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