371830

GPR40 Antagonist, GW1100

The GPR40 Antagonist, GW1100, also referenced under CAS 306974-70-9, controls the biological activity of GPR40. This small molecule/inhibitor is primarily used for Biochemicals applications.

• Synonyme(s) : GPR40 Antagonist, GW1100, 1-(4-Ethoxycarbonylphenyl)-2-(4-fluorobenzylthio)-5-(2-ethoxy-5-pyrimidinylmethyl)-4-pyrimidinone, SB376752
• Formule empirique (notation de Hill): C₂₇H₂₅FN₄O₄S
• Numéro CAS: 306974-70-9
• Poids moléculaire : 520.58
• Numéro MDL: MFCD09953714
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥97% (HPLC)
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white
• Solubilité: DMSO: 50 mg/mL
• Conditions d'expédition: wet ice
• Température de stockage: 2-8°C
• Chaîne SMILES: FC(C=C1)=CC=C1CSC(N(C2=CC=C(C(OCC)=O)C=C2)C=C3CC4=CN=C(N=C4)OCC)=NC3=O
• InChI: 1S/C27H25FN4O4S/c1-3-35-25(34)20-7-11-23(12-8-20)32-16-21(13-19-14-29-26(30-15-19)36-4-2)24(33)31-27(32)37-17-18-5-9-22(28)10-6-18/h5-12,14-16H,3-4,13,17H2,1-2H3
• Clé InChI: PTPNCCWOTBBVJR-UHFFFAOYSA-N

Description

Description générale

A cell-permeable pyrimidinylmethyl-pyrimidinone compound that acts as potent, reversible and non-competitive GPR40 antagonist. Selectively blocks GPR40-mediated intracellular Ca²⁺ release stimulated by GPR40 Agonist GW9508 (Cat. No. 371706) and linoleic acid (pIC₅₀ of 5.99 in GPR40 expressing HEK293 cells) with no effect on GPR120-mediated activation. Shown to significantly reverse glucose-induced insulin secretion potentiated by GW9508 and only partially reduce linoleic acid effect in MIN6 cells.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Autres remarques

Stoddart, L.A., et al. 2007. Mol. Pharmacol.71, 994.
Briscoe, C.P., et al. 2006. Br. J. Pharmacol.148, 619.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 2
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable