R-BMS-816336-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE(R)-BMS-816336Cat. No.: HY-101930BCAS No.: 1009583-83-8分式: CHNO分量: 341.44作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 300 mg/mL (878.63 mM; Need ultrasonic)Mass Sol

2、vent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9288 mL 14.6439 mL 29.2877 mL5 mM 0.5858 mL 2.9288 mL 5.8575 mL10 mM 0.2929 mL 1.4644 mL 2.9288 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分指该溶剂在您

3、配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 7.5 mg/mL (21.97 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 7.5 mg/mL (21.97 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 7.5 mg/mL (21.97 mM); Clear solution1/2

4、Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 (R)-BMS-816336 (Compound 6n-1)种有效的服活性的，和蟹猴 11-羟类醇脱氢酶 1 型 (11-HSD1) 抑制剂，其 IC50 分别为 14.5 nM，50.3 nM 和 16 nM。IC50 & Target IC50: 14.5 nM (Human 11-HSD1), 50.3 nM (Mouse 11-HSD1) and 16 nM (Cynomolgus monkey 11-HSD1) 1体内研究 During the in

5、 vivo studies of BMS-816336 (Compound 6n-2) in animals, its enantiomer (R)-BMS-816336(Compound 6n-1) in the plasma samples, together with trace amount of Ketone A are detected. Theinterconversion of BMS-816336 and (R)-BMS-816336 take place via the intermediate Ketone A throughphysiological oxidation

6、 and reduction process. In vivo studies in rat, dog, and cynomolgus monkey, theplasma ratios of (R)-BMS-816336/BMS-816336 decrease in the order: dog rat cynom olgus m onkey 1.REFERENCES1. Ye XY, et al. Discovery of Clinical Candidate 2-(2S,6S)-2-Phenyl-6-hydroxyadamantan-2-yl)-1-(3-hydroxyazetidin-1-yl)ethanone BMS-816336, an Orally Active Novel Selective 11-Hydroxysteroid Dehydrogenase Type 1 Inhibitor. J Med Chem. 2017 Jun 22;60(12):4932-4948.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only