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346007 Glucagon-Like Peptide 1 Receptor Agonist II - Calbiochem

346007
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₀H₁₇F₃N₂O₂S

Products

Catalogue NumberPackaging Qty/Pack
346007-10MG Glass bottle 10 mg
Description
OverviewA 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 Number346007
Brand Family Calbiochem®
Synonyms4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine , Glucagon-Like Peptide 1 Receptor Agonist II, Compound B
References
ReferencesSloop, KW., et al. 2010. Diabetes. 59, 3099.
Product Information
FormOff-white solid
Hill FormulaC₂₀H₁₇F₃N₂O₂S
Chemical formulaC₂₀H₁₇F₃N₂O₂S
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity>95% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

Glucagon-Like Peptide 1 Receptor Agonist II - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Glucagon-Like Peptide 1 Receptor Agonist II - Calbiochem Certificates of Analysis

TitleLot Number
346007

References

Reference overview
Sloop, KW., et al. 2010. Diabetes. 59, 3099.
Data Sheet

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.

Revision23-February-2011 RFH
Synonyms4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine , Glucagon-Like Peptide 1 Receptor Agonist II, Compound B
DescriptionA 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.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₀H₁₇F₃N₂O₂S
Structure formulaStructure formula
Purity>95% by HPLC
SolubilityDMSO (100 mg/ml)
Storage -20°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesSloop, KW., et al. 2010. Diabetes. 59, 3099.