1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESB-674042Cat. No.: HY-10898CAS No.: 483313-22-0分式: CHFNOS分量: 448.51作靶點(diǎn): Orexin Receptor (OX Receptor)作通路: GPCR/G Protein; Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 3

2、2 mg/mL (71.35 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.2296 mL 11.1480 mL 22.2960 mL5 mM 0.4459 mL 2.2296 mL 4.4592 mL10 mM 0.2230 mL 1.1148 mL 2.2296 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 SB-674042肽類(lèi)欲肽OX1受體拮抗劑，Kd

3、為3.76 nM，對(duì)OX2受體的抑制性100倍。REFERENCES1. Heifetz, Alexander; Morris, G. Benjamin; Biggin, Philip C. et al. Study of Human Orexin-1 and -2 G-Protein-Coupled Receptors withNovel and Published Antagonists by Modeling, Molecular Dynamics Simulations, and Site-Directed Mutagenesis. Biochemistry (2011/2 Maste

4、r of Small Molecules 您邊的抑制劑師www.MedChemE2. Malherbe, Pari; Roche, Olivier; Marcuz, Anne et al. Mapping the binding pocket of dual antagonist Almorexant to human orexin 1 andorexin 2 receptors: comparison with the selective OX1 antagonist SB-674042 and the selective OX2 antagonist N-ethyl-2-(6-me3. M

5、alherbe, Pari; Borroni, Edilio; Pinard, Emmanuel et al. Biochemical and electrophysiological characterization of almorexant, a dualorexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists. Molecular P4. Ellis, James; Pediani, John D.; Canals, Meri

6、txell et al. Orexin-1 Receptor-Cannabinoid CB1 Receptor Heterodimerization Results in BothLigand-dependent and -independent Coordinated Alterations of Receptor Localization and Function. Journal of Biological C5. Langmead, Christopher J.; Jerman, Jeffrey C.; Brough, Stephen J. et al. Characterisation of the binding of 3H-SB-674042, a novelnonpeptide antagonist, to the human orexin-1 receptor. British Journal of Pharmacology (2004), 141(2), 340-346.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only