371721

GPR40 Agonist II

The GPR40 Agonist II controls the biological activity of GPR40. This small molecule/inhibitor is primarily used for Biochemicals applications.

• Sinonimo/i: GPR40 Agonist II, 3-(4-((2,6-Dichloropyridin-4-yl)ethynyl)phenyl)propanoic acid, FFA1 Agonist II, Free Fatty Acid Receptor 1 Agonist II, FFA1 Agonist II, Free Fatty Acid Receptor 1 Agonist II, 3-(4-((2,6-Dichloropyridin-4-yl)ethynyl)phenyl)propanoic acid
• Formula empirica (notazione di Hill): C₁₆H₁₁Cl₂NO₂
• Numero CAS: 1206629-08-4
• Peso molecolare: 320.17
• Numero MDL: MFCD30290778
• Codice UNSPSC: 51111800
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥98% (HPLC)
• Forma fisica: powder
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: off-white
• Solubilità: DMSO: 100 mg/mL, clear, colorless
• Condizioni di spedizione: wet ice
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: ClC1=NC(Cl)=CC(C#CC2=CC=C(CCC(O)=O)C=C2)=C1

Descrizione

Descrizione generale

A cell-permeable alkynedihydrocinnamic acid that acts as a potent GPR40/FFA1 agonist (EC₅₀ = 40.7 nM in inducing Ca²⁺ mobilization in hFFA1-expressing 1321N1 cells) with >100-fold selectivity over GPR43/FFA2, GPR41/FFA3, and a panel of 56 other receptors, ion channels, and transporters. Reported to enhance 12 mM glucose-induced insulin secretion from rat INS-1E β-cells (by 34% at 10 µM) and exhibit good aqueous solubility (199 µM in PBS at pH 7.4), as well as chemical (0.1% degradation after 12 days in PBS at 37 °C) and metabolic (3% metabolization by human liver S9 stability test) stability.

A cell-permeable alkynedihydrocinnamic acid that acts as a potent GPR40/FFA1 agonist (EC₅₀ = 40.7 nM in inducing Ca²⁺ mobilization in hFFA1-expressing 1321N1 cells) with >100-fold selectivity over GPR43/FFA2, GPR41/FFA3, and a panel of 56 other receptors, ion channels, and transporters. Reported to enhance 12 mM glucose-induced insulin secretion from rat INS-1E β-cells (by 34% at 10 µM) and exhibit good aqueous solubility (199 µM in PBS at pH 7.4), as well as chemical and metabolic stability.

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 6 months at -20°C>

Altre note

Christiansen, E., et al. 2011, J. Med. Chem.54, 6691.

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 2
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable