Esaxerenone-CS-3150-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEsaxerenoneCat. No.: HY-100471CAS No.: 1632006-28-0Synonyms: CS-3150; XL-550分式: CHFNOS分量: 466.47作靶点: Mineralocorticoid Receptor作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶

2、解性数据体外实验 DMSO : 125 mg/mL (267.97 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1438 mL 10.7188 mL 21.4376 mL5 mM 0.4288 mL 2.1438 mL 4.2875 mL10 mM 0.2144 mL 1.0719 mL 2.1438 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

3、前请先配制澄清的储备液，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；澄清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: 2.08 mg/mL (4.46 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.46 mM); Clear solution

4、1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.46 mM); Clear solution; Need warmingBIOLOGICAL ACTIVITY物活性 Esaxerenone种新型的，度有效且有选择性的类 醇盐质激素受体拮抗剂。IC50 & Target Mineralocorticoid receptor 1体内研究 After single oral administration of Esaxerenon

5、e at 0.1, 0.3, 1, and 3mg/kg, maximum plasma concentration(Cmax) and the area under the plasma concentration versus time curve (AUC) are increased with dose. Timeto reach the maximum plasma concentration (Tmax) of Esaxerenone ranges from 2.0 to 4.5h. Afterintravenous administration of Esaxerenone at

6、 0.1, 0.3, 1, and 3mg/kg, the total body clearance (CL) anddistribution volume at steady state (Vss) are 3.53 to 6.69mL/min/kg and 1.47 to 2.49L/kg, respectively, inrats, and 2.79 to 3.69mL/min/kg and 1.34 to 1.54L/kg, respectively, in cynomolgus monkeys. Up to 168hafter administration, 3.9% and 91.

7、4% of dosed radioactivity are excreted in rat urine and feces, respectively,and 95.2% in total. In monkeys, the excreted radioactivity up to 168h is 11.5% in urine, 82.3% in feces, and93.9% in total 1.PROTOCOLAnimal Esaxerenone dissolved in vehicle is administered orally or intravenously at doses of

8、 0.1, 0.3, 1, and 3mg/kgAdministration 1 to rats (8 weeks old, 285 to 313g, four animals per group) or to cynomolgus monkeys (3 to 5 years old, 3.37to 4.48kg, four animals per group). The blood is collected with heparinized needles and syringes at thedesignated sample collection times from the cervi

9、cal veins of the rats and from the femoral veins of themonkeys. Plasma is obtained by centrifugation (4C, 1710g, 15min) and stored at -80C before analysis.To rats (6 weeks old, 146 to 154g, 4 animals), 14C Esaxerenone is orally administered at a single dose of 1mg/kg prepared in vehicle. Urine and f

10、eces are collected for the designated periods. For the monkey study,14C Esaxerenone suspended in 0.5% Methylcellulose (MC) is orally administered to cynomolgus monkeys(3 years old, 2.9 to 3.5kg, three animals) at a single dose of 1mg/kg. Urine and feces are collected for adesignated period up to 168

11、h post-dose 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Yamada M, et al. Pharmacokinetics, distribution, and disposition of esaxerenone, a novel, highly potent and selective non-steroidalmineralocorticoid receptor antagonist, in rats and monkeys. Xenobiotica. 2017 Dec;47(12):1090-1103.McePdfHeightCaution: Product has n