Almorexant-ACT-078573-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAlmorexantCat. No.: HY-10805CAS No.: 871224-64-5Synonyms: ACT 078573分式: CHFNO分量: 512.56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 mon

2、th溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 46 mg/mL (89.75 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.9510 mL 9.7550 mL 19.5099 mL5 mM 0.3902 mL 1.9510 mL 3.9020 mL10 mM 0.1951 mL 0.9755 mL 1.9510 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。體內(nèi)實(shí)驗(yàn) Almorexant is prepared

3、in PBS5.BIOLOGICAL ACTIVITY物活性 Almorexant (ACT 078573)種有效的欲素受體 orexin 1 receptor (OX1)/orexin 2 receptor (OX2) 拮抗劑，Ki 分別為 1.3 和 0.17 nM。1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEIC50 & Target IC50: 1.3/0.7 nM(OX1/OX2 Receptor)戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Metab. 2018 Jul 3;28(1):118-129.e5. Oncotarget. 20

4、18 Jan 9;9(6):6952-6967.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Cruz HG, et al. Assessment of the abuse liability of a dual orexin receptor antagonist: a crossover study of almorexant and zolpidem inrecreational drug users. CNS Drugs. 2014 Apr;28(4):361-72.2. Malherbe P

5、, et al. Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor(OX2) antagonist: comparison with selective OX1 and OX2 antagonists. Mol Pharmacol. 2009 Sep;76(3):618-31.3. Sifferlen T, et al. Novel pyrazolo-tetrahydropyridines as potent

6、orexin receptor antagonists. Bioorg Med Chem Lett. 2010 Mar1;20(5):1539-42.4. Black SW, et al. Almorexant promotes sleep and exacerbates cataplexy in a murine model of narcolepsy. Sleep. 2013 Mar 1;36(3):325-36.5. Dayot S, et al. In vitro, in vivo and ex vivo demonstration of the antitumoral role of hypocretin-1/orexin-A and almorexant in pancreaticductal adenocarcinoma. Oncotarget. 2018 Jan 9;9(6):6952-6967.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.T