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505854 TGR5 Receptor Agonist, Cpd23g - CAS 1415407-60-1 - Calbiochem

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
1415407-60-1C₂₅H₂₅N₃O₂

Products

Catalog NumberPackaging Qty/Pack
5.05854.0001 Glass bottle 10 mg
Description
OverviewA cell-permeable, orally available, phenoxypyrimidine carboxamide derivative that acts as a highly potent and selective agonist of Protein coupled receptor TGR5 (EC50 = 720 pM and 6.2 nM for human and mouse TGR5, respectively). Does not exhibit any significant affinity towards other related targets such as GPR40, GPR119, and GPR120. Shown to increase glucagon-like peptide-1 (GLP-1) secretion in a dose-dependent manner and significantly reduce blood glucose levels in db/db mice following a single oral dose (50 mg/kg). Exhibits desirable pharmacokinetic properties in rodent models (t½ = 1.5 h, Cmax = 56 ng/ml; and AUC = 147 ng.h/ml following an oral dose of 5 mg/kg).
Catalogue Number505854
Brand Family Calbiochem®
Synonyms(4-cyclopropyl-3,4-dihydroquinoxalin-1(2H)-yl)(4-(2,5-dimethylphenoxy)pyridin-3-yl)methanone, Bile Acid Receptor GPBAR-1 Agonist, Bile Acid Receptor Agonist, G protein-coupled bile acid receptor 1 Agonist
References
ReferencesDuan, H., et al. 2012, J. Med. Chem. 55, 10475.
Product Information
CAS number1415407-60-1
FormWhite powder
Hill FormulaC₂₅H₂₅N₃O₂
Chemical formulaC₂₅H₂₅N₃O₂
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetTGR5
Purity≥98% 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 at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°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
Global Trade Item Number
Catalog Number GTIN
5.05854.0001 04055977263084

Documentation

TGR5 Receptor Agonist, Cpd23g - CAS 1415407-60-1 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Duan, H., et al. 2012, J. Med. Chem. 55, 10475.
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-December-2013 JSW
Synonyms(4-cyclopropyl-3,4-dihydroquinoxalin-1(2H)-yl)(4-(2,5-dimethylphenoxy)pyridin-3-yl)methanone, Bile Acid Receptor GPBAR-1 Agonist, Bile Acid Receptor Agonist, G protein-coupled bile acid receptor 1 Agonist
DescriptionA cell-permeable, orally available, phenoxypyrimidine carboxamide derivative that acts as a highly potent and selective agonist of Protein coupled receptor TGR5 (EC50 = 720 pM and 6.2 nM for human and mouse TGR5, respectively). Does not exhibit any significant affinity towards other related targets such as GPR40, GPR119, and GPR120. Shown to increase glucagon-like peptide-1 (GLP-1) secretion in a dose-dependent manner and significantly reduce blood glucose levels in db/db mice following a single oral dose (50 mg/kg). Exhibits desirable pharmacokinetic properties in rodent models (t1/2 = 1.5 h, Cmax = 56 ng/ml; and AUC = 147 ng.h/ml following an oral dose of 5 mg/kg).
FormWhite powder
Intert gas (Yes/No) Packaged under inert gas
CAS number1415407-60-1
Chemical formulaC₂₅H₂₅N₃O₂
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
+2°C to +8°C
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
ReferencesDuan, H., et al. 2012, J. Med. Chem. 55, 10475.