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  1. Metabolic Enzyme/Protease Autophagy Anti-infection
  2. Cytochrome P450 Autophagy Virus Protease
  3. Schisandrin A

Schisandrin A  (Synonyms: 五味子甲素; Schizandrin-A; Wuweizisu-A; Deoxyschizandrin)

目錄號: HY-N0693 純度: 99.89%
COA 產(chǎn)品使用指南

Schisandrin A 抑制 CYP3A 活性,IC50Ki 分別為 6.60 μM 和 5.83 μM。

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Schisandrin A Chemical Structure

Schisandrin A Chemical Structure

CAS No. : 61281-38-7

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10 mM * 1 mL in DMSO ¥116
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10 mg ¥106
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25 mg ¥202
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50 mg ¥344
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100 mg ¥585
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Customer Review

Other Forms of Schisandrin A:

    Schisandrin A purchased from MCE. Usage Cited in: Eur J Pharmacol. 2019 Jul 15;855:10-19.  [Abstract]

    Western analysis of Cleaved-PARP, Cleaved-Caspase3 and Bcl2 expression in HCC827GR cells with the treatment of SchA , Gefi and the combination, respectively.

    Schisandrin A purchased from MCE. Usage Cited in: Eur J Pharmacol. 2019 Jul 15;855:10-19.  [Abstract]

    Western analysis of Cyclin D1 and Cdk-4 expression in HCC827GR cells with the treatment of SchA , Gefi and the combination, respectively.
    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

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

    IC50 & Target[1]

    CYP3A

    6.6 μM (IC50)

    Autophagy

     

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    > 100 μM
    Compound: Schisandrin A
    Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
    Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
    [PMID: 18063366]
    HCT-15 IC50
    > 100 μM
    Compound: Schisandrin A
    Antiproliferative activity against human HCT15 cells after 72 hrs by SRB assay
    Antiproliferative activity against human HCT15 cells after 72 hrs by SRB assay
    [PMID: 18063366]
    K562 IC50
    > 100 μM
    Compound: Schisandrin A
    Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
    Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
    [PMID: 18063366]
    MDA-MB-231 IC50
    > 100 μM
    Compound: Schisandrin A
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
    [PMID: 18063366]
    SK-HEP1 IC50
    42 μM
    Compound: Schisandrin A
    Antiproliferative activity against human SK-HEP1 cells after 72 hrs by SRB assay
    Antiproliferative activity against human SK-HEP1 cells after 72 hrs by SRB assay
    [PMID: 18063366]
    SNU-638 IC50
    53.1 μM
    Compound: Schisandrin A
    Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay
    Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay
    [PMID: 18063366]
    T47D IC50
    40 μM
    Compound: Schisandrin A
    Antiproliferative activity against human T47D cells after 72 hrs by SRB assay
    Antiproliferative activity against human T47D cells after 72 hrs by SRB assay
    [PMID: 18063366]
    體外研究
    (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[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    體內(nèi)研究
    (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)[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    416.51

    Formula

    C24H32O6

    CAS 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    五味子甲素

    結(jié)構(gòu)分類
    初始來源
    運輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細胞實驗: 

    DMSO 中的溶解度 : 50 mg/mL (120.05 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.4009 mL 12.0045 mL 24.0090 mL
    5 mM 0.4802 mL 2.4009 mL 4.8018 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
    儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗:

    請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
    ——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用;
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.00 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (6.00 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.5 mg/mL的均勻懸濁液,懸濁液可用于口服和腹腔注射。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

      2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
    動物溶解方案計算器
    請輸入動物實驗的基本信息:

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    由于實驗過程有損耗,建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上,請謹慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.89%

    參考文獻
    Kinase Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    參考文獻

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
    儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4009 mL 12.0045 mL 24.0090 mL 60.0226 mL
    5 mM 0.4802 mL 2.4009 mL 4.8018 mL 12.0045 mL
    10 mM 0.2401 mL 1.2005 mL 2.4009 mL 6.0023 mL
    15 mM 0.1601 mL 0.8003 mL 1.6006 mL 4.0015 mL
    20 mM 0.1200 mL 0.6002 mL 1.2005 mL 3.0011 mL
    25 mM 0.0960 mL 0.4802 mL 0.9604 mL 2.4009 mL
    30 mM 0.0800 mL 0.4002 mL 0.8003 mL 2.0008 mL
    40 mM 0.0600 mL 0.3001 mL 0.6002 mL 1.5006 mL
    50 mM 0.0480 mL 0.2401 mL 0.4802 mL 1.2005 mL
    60 mM 0.0400 mL 0.2001 mL 0.4002 mL 1.0004 mL
    80 mM 0.0300 mL 0.1501 mL 0.3001 mL 0.7503 mL
    100 mM 0.0240 mL 0.1200 mL 0.2401 mL 0.6002 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    產(chǎn)品名稱:
    Schisandrin A
    目錄號:
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