346007

Glucagon-Like Peptide 1 Receptor Agonist II

• Synonym(e): Glucagon-Like Peptide 1 Receptor Agonist II, 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine, Glucagon-Like Peptide 1 Receptor Agonist II, Compound B
• Empirische Formel (Hill-System): C₂₀H₁₇F₃N₂O₂S
• CAS-Nummer: 1371569-69-5
• Molekulargewicht: 406.42
• MDL number: MFCD23143626
• UNSPSC Code: 51111800
• NACRES: NA.77
• Assay: >95% (HPLC)
• Form: solid
• Quality level: 100
• Storage condition: OK to freeze, protect from light

Eigenschaften

• assay: >95% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: off-white
• solubility: DMSO: 100 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: FC(F)(F)c1nc(nc(c1)c2cc(ccc2)OCc3ccccc3)[S](=O)CC
• InChI: 1S/C20H17F3N2O2S/c1-2-28(26)19-24-17(12-18(25-19)20(21,22)23)15-9-6-10-16(11-15)27-13-14-7-4-3-5-8-14/h3-12H,2,13H2,1H3
• InChI key: NTDFYGSSDDMNHI-UHFFFAOYSA-N

Beschreibung

General description

A pyrimidine small molecule that acts as a GLP-1 allosteric agonist that induces cAMP signaling in HEK293 cells expressing the GLP-1 receptor with EC₅₀ = 0.66 µM and 99% efficacy (similar data with rat GLP-1 receptor), does not compete with radiolabelled GLP-1 in receptor binding assays, and is not active in cells expressing the GLP-2, GIP, PTH, or glucagon receptors. In rodent islets, insulin secretion increases in a dose-dependent and glucose-dependent manner, either alone or in an additive fashion when combined with the endogenous GLP-1 peptide. In vivo, this molecule exhibits insulinotropic effects when dosed at 10mg/kg in SD rats undergoing an IVGTT and a hyperglycemic clamp. It is also shown to increase insulin secretion in perifusion assays involving normal and diabetic human islets ex vivo, at concentrations between 1 and 10 µM.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Sloop, KW., et al. 2010. Diabetes.59, 3099.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable