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)

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£581.00

SKU:: 217386
Molekulargewicht:: 406.42
Reinheit:: >95% (HPLC)
Lagerbedingungen:: -20°C
Hersteller:: United States Biological
Format:: Supplied as an off-white solid.
Weitere Details:: 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 = 0.66uM 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 10uM. Formula: C₂₀H₁₇F₃N₂O₂S Solubility: DMSO (100mg/ml) Molecular Weight: 406.42 Storage and Stability: Store at -20°C under inert atmosphere. Protect from light. For maximum recovery of product, centrifuge the original vial prior to removing the cap.