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.
| 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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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