1. Membrane Transporter/Ion Channel Neuronal Signaling Anti-infection
  2. Calcium Channel Potassium Channel Parasite
  3. Tetrandrine

Tetrandrine  (Synonyms: 汉防己甲素; NSC-77037; d-Tetrandrine)

目录号: HY-13764 纯度: 99.91%
COA 产品使用指南

Tetrandrine (NSC-77037; d-Tetrandrine) 是一种双苯基异喹啉生物碱,抑制电压门控钙离子通道 (ICa) 和 Ca2+ 激活的钾离子通道。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Tetrandrine Chemical Structure

Tetrandrine Chemical Structure

CAS No. : 518-34-3

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Customer Review

Other Forms of Tetrandrine:

    Tetrandrine purchased from MCE. Usage Cited in: Front Pharmacol. 2020 Jan 10;10:1530.  [Abstract]

    RAW264.7 cells are harvested after induced by RANKL (50ng/mL) and tetrandrine (0, 0.125, 0.25, 0.5 ,1μM) for 5days. The proteins were used to detect osteoclastogenic proteins levels of NFATc1, CTR9, CTSK, TRAP, and MMP9. D) Tetrandrine down‐regulates osteoclastogenic gene expression of NFATc1, TRAP, CTSK, and c-fos. RAW264.7 cells are stimulated with RANKL and cultured with different concentrations of tetrandrine.

    Tetrandrine purchased from MCE. Usage Cited in: Front Pharmacol. 2020 Jan 10;10:1530.  [Abstract]

    Phosphorylation of key proteins in NF-kB pathways, including P50, P65 and IκBα, are detected by Western blotting.

    Tetrandrine purchased from MCE. Usage Cited in: Front Pharmacol. 2020 Jan 10;10:1530.  [Abstract]

    Tetrandrine inhibits osteoclast function in vitro A) Tetrandrine suppresses RANKL-induced actin ring formation in BMMs. Osteoclasts having actin rings and nucleuses inside these osteoclasts are counted.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Tetrandrine (NSC-77037; d-Tetrandrine) is a bis-benzyl-isoquinoline alkaloid, which inhibits voltage-gated Ca2+ current (ICa) and Ca2+-activated K+ current.

    IC50 & Target

    Ca2+ current[1]
    K+ current[1]

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A673 GI50
    4 μM
    Compound: 16
    Antiproliferative activity against human A673 assessed as cell growth inhibition after 48 hrs by SRB assay
    Antiproliferative activity against human A673 assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 33226219]
    CCRF-CEM IC50
    15.8 μM
    Compound: 1
    Antiproliferative activity against vincristine-resistant human CEM cells assessed as reduction in cell viability measured after 48 hrs by Celltiter-blue cell viability assay
    Antiproliferative activity against vincristine-resistant human CEM cells assessed as reduction in cell viability measured after 48 hrs by Celltiter-blue cell viability assay
    [PMID: 32942071]
    ECa-109 cell line IC50
    29.37 nM
    Compound: TET
    Reversal of VCR -resistance in human Eca-109 cells assessed as vincristine IC50 by measuring cell viability incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)
    Reversal of VCR -resistance in human Eca-109 cells assessed as vincristine IC50 by measuring cell viability incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)
    [PMID: 36892076]
    ECa-109 cell line IC50
    29.4 nM
    Compound: TET
    Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 5 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)
    Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 5 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)
    [PMID: 36892076]
    HCC1806 GI50
    5.1 μM
    Compound: 16
    Antiproliferative activity against human HCC1806 assessed as cell growth inhibition after 48 hrs by SRB assay
    Antiproliferative activity against human HCC1806 assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 33226219]
    HCC1937 GI50
    4.2 μM
    Compound: 16
    Antiproliferative activity against human HCC1937 assessed as cell growth inhibition after 48 hrs by SRB assay
    Antiproliferative activity against human HCC1937 assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 33226219]
    HCC70 GI50
    3.4 μM
    Compound: 16
    Antiproliferative activity against human HCC70 assessed as cell growth inhibition after 48 hrs by SRB assay
    Antiproliferative activity against human HCC70 assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 33226219]
    HEK-293T CC50
    > 1 μM
    Compound: 1; tet
    Cytotoxicity against HEK293T cells assessed as reduction in cell viability by CellTiter-Glo assay
    Cytotoxicity against HEK293T cells assessed as reduction in cell viability by CellTiter-Glo assay
    [PMID: 37043739]
    HEL IC50
    16.78 μM
    Compound: Tetrandrine
    Cytotoxicity against human HEL cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human HEL cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 29133049]
    HEL IC50
    19.74 μM
    Compound: Tetrandrine
    Cytotoxicity against human HEL cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human HEL cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 31784186]
    HEL IC50
    7.45 μM
    Compound: Tet
    Antiproliferative activity against HEL cells after 48 hrs by MTT assay
    Antiproliferative activity against HEL cells after 48 hrs by MTT assay
    [PMID: 30109000]
    HeLa IC50
    2.16 μM
    Compound: Tetrandrine
    Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
    Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
    [PMID: 29624387]
    HepG2 IC50
    6.82 μM
    Compound: Tetrandrine
    Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
    [PMID: 28057423]
    K562 IC50
    11.76 μM
    Compound: Tet
    Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
    Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
    [PMID: 30109000]
    K562 IC50
    13.81 μM
    Compound: Tetrandrine
    Cytotoxicity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 29133049]
    K562 IC50
    6.43 μM
    Compound: Tetrandrine
    Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 31784186]
    KB ED50
    5800 nM
    Compound: 16
    Cytotoxicity against human KB cells after 72 hrs by SRB assay
    Cytotoxicity against human KB cells after 72 hrs by SRB assay
    [PMID: 9917283]
    L02 IC50
    44.25 μM
    Compound: Tet
    Cytotoxicity against human HL7702 cells after 48 hrs by MTT assay
    Cytotoxicity against human HL7702 cells after 48 hrs by MTT assay
    [PMID: 30109000]
    MCF7 IC50
    19.58 μM
    Compound: Tetrandrine
    Cytotoxicity against human MCF-7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human MCF-7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 31784186]
    MCF7 IC50
    8.62 μM
    Compound: Tetrandrine
    Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
    [PMID: 28057423]
    MDA-MB-231 IC50
    18.45 μM
    Compound: Tetrandrine
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 31784186]
    MDA-MB-231 IC50
    21.97 μM
    Compound: Tetrandrine
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 29133049]
    MDA-MB-231 GI50
    5 μM
    Compound: 16
    Antiproliferative activity against human MDA-MB-231 assessed as cell growth inhibition after 48 hrs by SRB assay
    Antiproliferative activity against human MDA-MB-231 assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 33226219]
    MDA-MB-231 IC50
    8.94 μM
    Compound: Tet
    Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
    [PMID: 30109000]
    MDA-MB-453 GI50
    3.3 μM
    Compound: 16
    Antiproliferative activity against human MDA-MB-453 assessed as cell growth inhibition after 48 hrs by SRB assay
    Antiproliferative activity against human MDA-MB-453 assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 33226219]
    PC-3 IC50
    5.86 μM
    Compound: Tet
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    [PMID: 30109000]
    PC-3 IC50
    7.87 μM
    Compound: Tetrandrine
    Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 29133049]
    PLC-PRF-5 IC50
    18.46 μM
    Compound: Tetrandrine
    Cytotoxicity against human PLC/PRF/5 cells assessed as growth inhibition after 24 hrs by MTT assay
    Cytotoxicity against human PLC/PRF/5 cells assessed as growth inhibition after 24 hrs by MTT assay
    [PMID: 28109948]
    SJRH30 GI50
    3 μM
    Compound: 16
    Antiproliferative activity against human SJRH30 assessed as cell growth inhibition after 48 hrs by SRB assay
    Antiproliferative activity against human SJRH30 assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 33226219]
    U-937 IC50
    > 50 μM
    Compound: 16, NSC 77037
    Cytotoxicity against human U937 cells after 24 hrs by alamar blue assay
    Cytotoxicity against human U937 cells after 24 hrs by alamar blue assay
    [PMID: 22766217]
    Vero CC50
    14.92 μM
    Compound: Tetrandrine
    Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
    Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
    10.1101/2020.03.20.999730
    Vero IC50
    3 μM
    Compound: Tetrandrine
    Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
    Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
    10.1101/2020.03.20.999730
    Vero C1008 EC50
    1.1 μM
    Compound: Hanfangchin A
    Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs
    Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs
    [PMID: 32511357]
    体外研究
    (In Vitro)

    Tetrandrine (NSC-77037) 是一种双苄基异喹啉类生物碱。通过膜片钳技术研究其对大鼠神经垂体分离神经末端的电压门控 Ca2+ 电流 (ICa) 和 Ca2+ 激活 K+ 电流 (IK (Ca) ) 及通道的影响。外源性 Tetrandrine (NSC-77037) 以电压和剂量依赖性方式抑制 ICa 的非失活成分,其 IC50=10.1 μM。在突发期间,Tetrandrine (NSC-77037) 减少通道开放概率,IC50=0.21 μM[1]。在 HCC 细胞中的评估表明,0.5-2 μM Tetrandrine 对 HCC 细胞增殖几乎没有抑制作用。然而,Tetrandrine (NSC-77037) 以剂量依赖性方式抑制 HCC 细胞迁移。伤口愈合和 Transwell 实验显示,2 μM Tetrandrine 显著抑制 HCC 细胞的迁移和侵袭[2]

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

    体内研究
    (In Vivo)

    为了评估Tetrandrine (NSC-77037) 对体内肿瘤转移的抑制作用,用无胸腺裸鼠建立了 HCCLM9 皮下肿瘤异种移植模型。当肿瘤体积达到约 50 mm3 时,裸鼠每隔一天口服给药载体或Tetrandrine (NSC-77037) (30 mg/kg),共 37 天。Tetrandrine (NSC-77037) 治疗通过减少肿瘤体积和重量来抑制肿瘤生长[2]

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

    Clinical Trial
    分子量

    622.75

    Formula

    C38H42N2O6

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    汉防己甲素;汉防己碱;粉防乙碱;汉防己硷; 粉防己碱

    结构分类
    初始来源
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 5 mg/mL (8.03 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.6058 mL 8.0289 mL 16.0578 mL
    5 mM 0.3212 mL 1.6058 mL 3.2116 mL
    查看完整储备液配制表

    * 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    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

    • 方案 一

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

      Solubility: ≥ 0.5 mg/mL (0.80 mM); 澄清溶液

      此方案可获得 ≥ 0.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

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

      Solubility: ≥ 0.5 mg/mL (0.80 mM); 澄清溶液

      此方案可获得 ≥ 0.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 5.0 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。

      2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

    以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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。

    • 方案 一

      请依序添加每种溶剂: 50% PEG300    50% Saline

      Solubility: 10 mg/mL (16.06 mM); 悬浊液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.91%

    参考文献
    Cell Assay
    [2]

    Huh7, HCCLM9 and Hep3B cells are seeded in a 96-well plate at a cell density of 5 × 103 cells/well. The cells are treated with the indicated concentrations (0-4 μM) of Tetrandrine (NSC-77037) for 24 h. The cells are subsequently stained with 20 μL of MTS for 1-2 h, and the plates are read at 490 nm on a BioTek ELx800[2].

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

    Animal Administration
    [2]

    Mice[2] Four-week-old male athymic BALB/c nu/nu SPF mice (body weight range from 18 g to 20 g) are used. HCCLM9 WT and HCCLM9 ATG7 KO cells (5 million) resuspended in 0.2 mL of PBS are subcutaneously implanted into the right flank of each mouse. When the tumor volume reach approximately 50 mm3, the tumor-bearing mice are randomly divided into control and treatment groups (n = 6). The control and treatment groups are administered oral injection of vehicle (0.5% methylcellulose) and Tetrandrine at 30 mg/kg of body weight every other day for 37 days. During the treatment, the tumor volumes are measured every day and are calculated.

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

    参考文献

    完整储备液配制表

    * 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.6058 mL 8.0289 mL 16.0578 mL 40.1445 mL
    5 mM 0.3212 mL 1.6058 mL 3.2116 mL 8.0289 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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    产品名称:
    Tetrandrine
    目录号:
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