Filorexant-MK-6096-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEFilorexantCat. No.: HY-15653CAS No.: 1088991-73-4Synonyms: MK-6096分式: CHFNO分量: 420.48作靶點: Orexin Receptor (OX Receptor)作通路: GPCR/G Protein; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month

2、溶解性數(shù)據(jù)體外實驗 DMSO : 12.61 mg/mL (29.99 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.3782 mL 11.8912 mL 23.7823 mL5 mM 0.4756 mL 2.3782 mL 4.7565 mL10 mM 0.2378 mL 1.1891 mL 2.3782 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Filorexant (MK-6096)欲素受體OX

3、1和OX2雙重 抑制劑，Ki 值于3nM。IC50 & Target Ki: 3 nM(Orexin receptor) 1.體外研究In radioligand binding and functional cell based assays Filorexant (MK-6096) demonstrated potent bindingand antagonism of both human OX(1)R and OX(2)R (170 receptors and enzymes. Filorexant (MK-6096)1/2 Master of Small Molecules 您邊的抑

4、制劑師www.MedChemEoccupies 90% of human OX(2)Rs expressed in transgenic rats at a plasma concentration of 142 nM.體內(nèi)研究 Filorexant (MK-6096) dose-dependently reduced locomotor activity and significantly increased sleep in rats(3-30 mg/kg) and dogs (0.25 and 0.5 mg/kg).PROTOCOLAnimal Animal administration

5、 1Administration 1 The male Sprague Dawley rats (n = 8/study; age: 3-6 months; weight: 450-600 g) were singly housed withwater and food ad libitum and a 12 h light: 12 h dark cycle with lights on at 04:00 and off at 16:00. Sleepstudies were conducted to evaluate Filorexant (3 and 10 mg/kg, p.o.), DO

6、RA-22 (10 mg/kg, p.o.) andalmorexant (3 and 30 mg/kg, p.o.), employing a counterbalanced crossover design in which all animals werealternatively treated with drug and vehicle daily for either 3 or 7 consecutive days (for DORA-22 andFilorexant, respectively): 2 baseline days (no dosing), a 2 day vehi

7、cle-only run-in, a 3 or 7-day arm of drug orvehicle followed by 3 or 7 days of conditional crossover. Effects of compound treatments relative to vehicle(20% Vitamin E TPGS, p.o.) were evaluated following administration in the active phase).MCE has not independently confirmed the accuracy of these me

8、thods. They are for reference only.REFERENCES1. Winrow CJ, et al. Pharmacological characterization of MK-6096 - a dual orexin receptor antagonist for insomnia. Neuropharmacology.2012 Feb;62(2):978-87.2. Coleman PJ, et al. Discovery of (2R,5R)-5-(5-fluoropyridin-2-yl)oxymethyl-2-methylpiperidin-1-yl5-methyl-2-(pyrimidin-2-yl)phenylmethanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties. ChemMedChem. 2012 Mar5;7(3):415-24, 337.McePdfHeightCaution: Product has not been fully validated for medical appl