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MilliporeSigma™ Calbiochem™ TGR5 Receptor Agonist, Cpd23g

Catalog No. 5058540001 Shop All MilliporeSigma Products
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50-585-40001 10 mg
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Catalog No. 50-585-40001 Supplier MilliporeSigma™ Supplier No. 5058540001
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A cell-permeable, orally available, phenoxypyrimidine carboxamide derivative that acts as a highly potent and selective agonist of Protein coupled receptor TGR5 (EC50 = 720 pM an

A 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 6.2nM 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 (50mg/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 5mg/kg).
TRUSTED_SUSTAINABILITY

Specifications

Color White
Description 98% by HPLC
Target Proteins TGR5
Molecular Formula C25H25N3O2
Solubility DMSO
Content And Storage Protect from light
Form Powder
Quantity 10 mg
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