Semaglutide Sodium

Catalog No.S9697 Batch:S969701

Technical Data

Formula	C₁₈₇H₂₉₁N₄₅O₅₉
Molecular Weight	4113.58(free base)	CAS No.	910463-68-2(free base)
Solubility (25°C)*	In vitro	4-Methylpyridine	4 mg/mL warmed with 50ºC water bath
		Water	Insoluble

* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Semaglutide Sodium (Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217), a long-acting glucagon-like peptide 1 (GLP-1) analogue, is a GLP-1 receptor agonist with the potential for the treatment of type 2 diabetes mellitus (T2DM).

Targets

GLP-1 receptor ^[1]

In vitro

Semaglutide is selected as the optimal once weekly candidate. 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.^[2]

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.^[2]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines BHK cells Concentrations 0.01 pM - 0.1 μM Incubation Time 3 h Method Frozen aliquots of BHK cells that express both the hGLP-1R and CRE firefly luciferase (clone FCW467-12A/KZ10-1) are thawed, washed twice in PBS, and suspended in assay buffer. Cells are plated out into 96-well plates at 5000 cells/well in a volume of 50 μL. Compounds to be tested are diluted in assay buffer and a 50 μL aliquot transferred to the plate containing the cells to reach final assay concentrations of 1 × 10⁻¹⁴ − 1 × 10⁻⁷ M. The plate is incubated for 3 h at 5% CO₂ at 37 °C. The plate was allowed to stand at room temperature for 15 min prior to adding 100 μL of steadylite plus reagent. The plate is covered to protect it from light and shaken at room temperature for 30 min. The plate is read in a TopCount NXT instrument.

Cell Assay:^{^[2]}

Cell lines
BHK cells
Concentrations
0.01 pM - 0.1 μM
Incubation Time
3 h
Method
Frozen aliquots of BHK cells that express both the hGLP-1R and CRE firefly luciferase (clone FCW467-12A/KZ10-1) are thawed, washed twice in PBS, and suspended in assay buffer. Cells are plated out into 96-well plates at 5000 cells/well in a volume of 50 μL. Compounds to be tested are diluted in assay buffer and a 50 μL aliquot transferred to the plate containing the cells to reach final assay concentrations of 1 × 10⁻¹⁴ − 1 × 10⁻⁷ M. The plate is incubated for 3 h at 5% CO₂ at 37 °C. The plate was allowed to stand at room temperature for 15 min prior to adding 100 μL of steadylite plus reagent. The plate is covered to protect it from light and shaken at room temperature for 30 min. The plate is read in a TopCount NXT instrument.

References

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SHIPPING AND STORAGE
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