TGR5 Receptor Agonist, Cpd23g ((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)

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£442.00

SKU:: 217831
Reinheit:: ~98% (HPLC)
Lagerbedingungen:: 4°C
Hersteller:: United States Biological
Format:: Supplied as a white powder.
Weitere Details:: 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 = 1.5h, Cmax = 56ng/ml; and AUC = 147ng.h/ml following an oral dose of 5mg/kg). Solubility: DMSO Primary Target: TGR5 Storage and Stability: May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.