5.05854

TGR5 Receptor Agonist, Cpd23g

• Sinonimo/i: 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
• Formula empirica (notazione di Hill): C₂₅H₂₅N₃O₂
• Numero CAS: 1415407-60-1
• Peso molecolare: 399.48
• Codice UNSPSC: 12352200

Proprietà

• Saggio: ≥98% (HPLC)
• Livello qualitativo: 100
• Forma fisica: powder
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: white
• Solubilità: DMSO: 50 mg/mL
• Temperatura di conservazione: 2-8°C

Descrizione

Descrizione generale

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 6.2 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).

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 6.2 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).

Azioni biochim/fisiol

Primary Target
TGR5

Reversible: yes

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Altre note

Duan, H., et al. 2012, J. Med. Chem.55, 10475.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable