| 中文名称: | 五味子甲素 | 中文别名: | 五味子甲素 |
|---|---|---|---|
| 英文名称: | Schisandrin A | CAS: | 61281-38-7 |
| 产品分类: | 小分子化合物 | 纯度: | ≥98% / HPLC≥98% |
| 产品编号 | 品牌 | 纯度 | 规格 | 库存 | 价格 |
|---|---|---|---|---|---|
| IS0050 | 索莱宝 | ≥98% | 10mM*1ml(inDMSO) | 现询 | 面议 |
| IS0050 | 索莱宝 | HPLC≥98% | 10mg | 有现货 | 96.00 元 |
| IS0050 | 索莱宝 | HPLC≥98% | 25mg | 有现货 | 192.00 元 |
| IS0050 | 索莱宝 | HPLC≥98% | 50mg | 有现货 | 334.00 元 |
| IS0050 | 索莱宝 | HPLC≥98% | 100mg | 有现货 | 576.00 元 |
| 标准名称: | 五味子甲素 | 英文名称: | Schisandrin A |
|---|---|---|---|
| CAS: | 61281-38-7 | 分子式: | C24H32O6 |
| 分子量: | 416.507287979126 | 颜色与性状: | Powder |
| 密度: | 1.0800 | 沸点: | 544.2°C at 760 mmHg |
| 熔点: | 112.0 to 116.0 deg-C | 水溶性: |
| CAS | 61281-38-7 |
| 中文名称 | 五味子甲素 |
| 英文名称 | Schisandrin A |
| 别名 | 五味子素A;Deoxyschizandrin;Wuweizisu-A |
| 分子式 | C24H32O6 |
| 分子量 | 416.51 |
| 规格 | 10mg ; 25mg ; 50mg ; 100mg |
| 溶解性 | Soluble in DMSO |
| 纯度 | HPLC≥98% |
| 级别 | Cell Culture |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
| 运输条件 | 冷藏运输 |
| MDL | MFCD09026934 |
| SMILES | C[C@H]1CC2=CC(OC)=C(OC)C(OC)=C2C3=C(OC)C(OC)=C(OC)C=C3C[C@H]1C |
| InChIKey | JEJFTTRHGBKKEI-OKILXGFUSA-N |
| InChI | InChI=1S/C24H32O6/c1-13-9-15-11-17(25-3)21(27-5)23(29-7)19(15)20-16(10-14(13)2)12-18(26-4)22(28-6)24(20)30-8/h11-14H,9-10H2,1-8H3/t13-,14+ |
| PubChem CID | 155256 |
| 靶点 | Adiponectin receptor 2;Cytochrome P450 |
| 通路 | GPCR & G Protein;Metabolic Enzyme&Protease |
| 背景说明 | 是五味子的活性成分,具有保肝、抗肿瘤和抗氧化活性。 也是脂联素受体 2 (AdipoR2) 的激动剂,可以抑制 CYP3A 活性。 |
| 生物活性 | Schisandrin A (Sch A, Deoxyschizandrin, Wuweizisu A) is an active component of Schisandrae Fructus with liver-protective, antitumor, and antioxidant activities. It is an agonist of the adiponectin receptor 2 (AdipoR2) with the IC50 value of 3.5 μM. Schisandrin A inhibits CYP3A activity with an IC50 of 6.60 μM and Ki of 5.83 μM, respectively.[1-3] |
| In Vitro | Schisandrin A(Sch A)strongly inhibits microsomal midazolam 1-hydroxylation catalyzed by CYP3A,with an IC50 of 6.60 μM. The recovery of enzyme activity in the absence or presence of Schisandrin A is shown in dilution assay plots. The Ki value for Schisandrin A is obtained from the Dixon plots and is 5.83 μM. The inactivation of rat liver microsomal midazolam 1-hydroxylation activity by Schisandrin A in the presence of NADPH is found to be time- and concentration-dependent. The Kinact and Ki are estimated to be 0.134/min and 4.51 μM,respectively for Schisandrin A[2]. |
| In Vivo | Schisandrin A(SchA)significantly inhibits CYP3A activity in rat hepatic microsomes and Vmax value of each group in a concentration-dependent manner. The double-reciprocal plots and the secondary plot show that Schisandrin 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 concentrations compared with the negative group(to levels similar to the positive group)[3]. |
| 动物实验 | Healthy male Sprague-Dawley rats,weighing 250-280 g and 2-3 months of age,are used. The rats are randomly divided into five groups with 16 rats in each group. The animals are administered once daily for three 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 administered with equal volume of vehicle in the negative control group and Ketoconazole(75 mg/kg)in the positive control group. All animals are allowed free access to food but are fasted overnight before scarification to reduce the intestinal content,and each group is randomly divided into two parts with eight rats in each part[3]. |
| 激酶实验 | For the inactivation of CYP3A4 activity,microsomes are preincubated with inhibitors(Schisandrin A,2.4 μM,7.2 μM and 12.0 μM; or Sch B)at 37°C for up to 15 min in the presence of NADPH. Reactions are initiated with the addition of substrate midazolam and incubated at 37°C for 10 min. The enzyme inactivation is analyzed. Duplicates are prepared and tested[2]. |
| 数据来源文献 | [1]. Sun Y, Zang Z, Zhong L, Wu M, Su Q, Gao X, Zan W, Lin D, Zhao Y, Zhang Z. Identification of adiponectin receptor agonist utilizing a fluorescence polarization based high throughput assay. PLoS One. 2013 May 14;8(5):e63354. [2]. Li WL, et al. Inhibitory effects of Schisandrin A and Schisandrin B on CYP3A activity. Methods Find Exp Clin Pharmacol. 2010 Apr;32(3):163-9. [3]. Li WL, et al. Inhibitory effects of continuous ingestion of Schisandrin A on CYP3A in the rat. Basic Clin Pharmacol Toxicol. 2012 Feb;110(2):187-92. |
| 单位 | 瓶 |
| 1mM-5mg | 12.0045mL |
| 1mM-1mg | 2.4009mL |
| 1mM-10mg | 24.009mL |
| 5mM-1mg | 0.4802mL |
| 5mM-5mg | 2.4009mL |
| 5mM-10mg | 4.8018mL |
| 10mM-1mg | 0.2401mL |
| 10mM-5mg | 1.2005mL |
| 10mM-10mg | 2.4009mL |
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| 企业认证: | 已认证 | 企业性质: | 生产研发 |
|---|---|---|---|
| 主营产品: | 先锋霉素 ; Hoechst 33342 荧光染料 ; 碘硝基氯化四氮唑蓝(INT) ; 莫能霉素钠 ; 甲基橙 ; | 供货范围: | 试剂 |
| 产品目录: | 119904 | 品牌: | 索莱宝 |
| 纯度 | 品牌 | 规格 | 发货地 |
|---|---|---|---|
| - | 索莱宝 | 25mg / 100mg / 1g | 北京 |