Schisandrin A inhibits CYP3A activity with an IC₅₀ of 6.60 μM and K_i of 5.83 μM, respectively.

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 K_i 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 K_inact and K_i are estimated to be 0.134/min and 4.51 μM, respectively for Schisandrin A^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Schisandrin A (SchA) significantly inhibits CYP3A activity in rat hepatic microsomes and V_max 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 K_i 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)^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

416.51

C₂₄H₃₂O₆

61281-38-7

五味子甲素

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 50 mg/mL (120.05 mM; Need ultrasonic)

*

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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.00 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: 2.5 mg/mL (6.00 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (6.00 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.00 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. 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.

  [2]. 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.

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^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Rats^[2]
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^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. 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.

  [2]. 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.