Properties
Description
RO-1138452, soluble in DMSO and ethanol and insoluble in water, inhibits the signaling pathway between G-protein-coupled receptors (GPCRs) and G proteins. It targets guinea-pig 5-HT4 receptor, human α2A adrenoceptor, human α2A adrenoceptor, human 5-HT1A receptor, human 5-HT1A receptor, human muscarinic M1 receptor, human muscarinic M1 receptor, human muscarinic M2 receptor, human muscarinic M2 receptor, and human muscarinic M4 receptor.
Molecular Formula
C19H23N3O
Targets
Guinea-pig 5-HT4 receptor: 8910 nM; Guinea-pig 5-HT4 receptor: 5.35 (pKi); Human α2A adrenoceptor: 724 nM; Human α2A adrenoceptor: 6.49 (pKi); Human 5-HT1A receptor: 8580 nM; Human 5-HT1A receptor: 5.37 (pKi); Human muscarinic M1 receptor: 2570 nM; Human muscarinic M1 receptor: 5.66 (pKi); Human muscarinic M2 receptor: 2220 nM; Human muscarinic M2 receptor: 5.88 (pKi); Human Muscarinic M4 receptor: 1450 nM
Solubility
DMSO: 58 mg/mL (187.45 mM); Water: insoluble; Ethanol: 58 mg/mL (187.45 mM)
Stability
The product is stable for three years when stored at the recommended temperature in lyophilized powder.
Applications
RO-1138452 can be used to research and develop therapeutic strategies for certain diseases that involve excessive activation of GPCR-G protein signaling pathways.
Storage
Store at -20°C, and keep desiccated.
