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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.
Catalogue Number
346007
Brand Family
Calbiochem®
Synonyms
4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine
, Glucagon-Like Peptide 1 Receptor Agonist II, Compound B
Glucagon-Like Peptide 1 Receptor Agonist II - CAS 1371569-69-5 - Calbiochem 分析证书
标题
批号
346007
参考
参考信息概述
Sloop, KW., et al. 2010. Diabetes.59, 3099.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
23-February-2011 RFH
Synonyms
4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine
, Glucagon-Like Peptide 1 Receptor Agonist II, Compound B
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.
Form
Off-white solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
1371569-69-5
Chemical formula
C₂₀H₁₇F₃N₂O₂S
Structure formula
Purity
>95% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
Protect from light
-20°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
