Schisandrin-A-Schizandrin-A-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESchisandrin ACat. No.: HY-N0693CAS No.: 61281-38-7Synonyms: Schizandrin-A; Wuweizisu-A; Deoxyschizandrin分式: CHO分量: 416.51作靶點(diǎn): Cytochrome P450; Autophagy作通路: Metabolic Enzyme/Protease; Autophagy儲存式: Powder -20C 3 years4C 2 yearsI

2、n solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (120.05 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.00 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.00 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.Me

3、dChemEBIOLOGICAL ACTIVITY物活性 Schisandrin A 抑制 CYP3A 活性，IC50 和 Ki 分別為 6.60 M 和 5.83 M。IC50 & Target CYP3A Autophagy6.6 M (IC50)體外研究 Schisandrin A (Sch A) strongly inhibits microsomal midazolam 1-hydroxylation catalyzed by CYP3A, with anIC50 of 6.60 M. The recovery of enzyme activity in the absence or

4、 presence of Schisandrin A is shown indilution assay plots. The Ki value for Schisandrin A is obtained from the Dixon plots and is 5.83 M. Theinactivation of rat liver microsomal midazolam 1-hydroxylation activity by Schisandrin A in the presence ofNADPH is found to be time- and concentration-depend

5、ent. The Kinact and Ki are estimated to be 0.134/minand 4.51 M, respectively for Schisandrin A 1.體內(nèi)研究 Schisandrin A (SchA) significantly inhibits CYP3A activity in rat hepatic microsomes and Vmax value of eachgroup in a concentration-dependent manner. The double-reciprocal plots and the secondary pl

6、ot show thatSchisandrin A inhibits CYP3A activity, with an apparent Ki value of 30.67 mg/kg. In each Schisandrin A-treated group, Schisandrin A also significantly decreases 1-hydroxymidazolam plasma concentrationscompared with the negative group (to levels similar to the positive group) 2.PROTOCOLKi

7、nase Assay 1 For the inactivation of CYP3A4 activity, microsomes are preincubated with inhibitors (Schisandrin A, 2.4 M,7.2 M and 12.0 M; or Sch B) at 37C for up to 15 min in the presence of NADPH. Reactions are initiatedwith the addition of substrate midazolam and incubated at 37C for 10 min. The e

8、nzyme inactivation isanalyzed. Duplicates are prepared and tested 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats 2Administration 2 Healthy male Sprague-Dawley rats, weighing 250-280 g and 2-3 months of age, are used. The rats arerandomly

9、divided into five groups with 16 rats in each group. The animals are administered once daily forthree consecutive days. The Schisandrin A-treated groups are administered intragastrically with doses of 32,16 or 8 mg/kg of Schisandrin A (physiological saline as vehicle), and the rats are similarly adm

10、inistered withequal volume of vehicle in the negative control group and Ketoconazole (75 mg/kg) in the positive controlgroup. All animals are allowed free access to food but are fasted overnight before scarification to reduce theintestinal content, and each group is randomly divided into two parts w

11、ith eight rats in each part 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Eur J Pharmacol. 2019 Apr 24. pii: S0014-2999(19)30244-4.See more customer validations on HYPERLINK / www.MedChemE2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE

12、REFERENCES1. Li WL, et al. Inhibitory effects of Schisandrin A and Schisandrin B on CYP3A activity. Methods Find Exp Clin Pharmacol. 2010Apr;32(3):163-9.2. Li WL, et al. Inhibitory effects of continuous ingestion of Schisandrin A on CYP3A in the rat. Basic Clin Pharmacol Toxicol. 2012Feb;110(2):187-92.McePdfHeightCaution: P