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

Tetrandrine  (Synonyms: テトランドリン; NSC-77037; d-Tetrandrine)

製品番号: HY-13764 純度: 99.90%
COA 取扱説明書 Technical Support

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

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CAS 番号 : 518-34-3

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カスタマーレビュー

Based on 16 publication(s) in Google Scholar

Other Forms of Tetrandrine:

Top Publications Citing Use of Products

    Tetrandrine purchased from MedChemExpress. 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.

    Tetrandrine purchased from MedChemExpress. 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 MedChemExpress. 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.
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    製品説明

    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]

    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]
    KB-V1 ED50
    3.7 μg/mL
    Compound: 1
    Cytotoxicity against human multidrug-resistant KBV1 cells
    Cytotoxicity against human multidrug-resistant KBV1 cells
    [PMID: 8450318]
    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 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
    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 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]
    P388 ED50
    0.4 μg/mL
    Compound: 1
    Cytotoxicity against mouse P388 cells
    Cytotoxicity against mouse P388 cells
    [PMID: 8450318]
    Panel NCI-60 (60 carcinoma cell lines) GI50
    10 nM
    Compound: Fanchinin
    Growth inhibitory activity against human cancer cell line in the NCI's anticancer drug screening program
    Growth inhibitory activity against human cancer cell line in the NCI's anticancer drug screening program
    [PMID: 15743190]
    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]
    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
    10.1101/2020.04.16.044016
    VSMC IC50
    1.48 μM
    Compound: Tetrandrine
    Antivegetative activity against rat VSMC
    Antivegetative activity against rat VSMC
    [PMID: 20708932]
    体外実験

    The effects of Tetrandrine (NSC-77037), a bis-benzyl-isoquinoline alkaloid, on voltage-gated Ca2+ currents (ICa) and on Ca2+-activated K+ current (IK(Ca)) and channels in isolated nerve terminals of the rat neurohypophysis are investigated using patch-clamp techniques. The non-inactivating component of ICa is inhibited by external Tetrandrine (NSC-77037) in a voltage- and dose-dependent manner, with an IC50=10.1μM. Tetrandrine (NSC-77037) decreases the channel-open probability, within bursts, with an IC50=0.21 μM[1]. To evaluate the effects of Tetrandrine on HCC cells, Huh7, HCCLM9 and Hep3B cells are treated with 0 (DMSO), 0.5, 1, 2 or 4 μM of Tetrandrine for 24 h. The cell proliferation assay indicates that Tetrandrine exhibits almost no effect on the inhibition of HCC cell proliferation at 0.5-2 μM. However, Tetrandrine (NSC-77037) inhibits HCC cell migration in a dose-dependent manner. Furthermore, a wound-healing and transwell assay shows that 2 μM Tetrandrine significantly inhibits HCC cell migration and invasion[2].

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

    体内実験

    To evaluate the effect of Tetrandrine (NSC-77037) on the inhibition of tumor metastasis in vivo, HCCLM9 subcutaneous tumor xenograft models is established with athymic nude mice. When the tumor volume reach approximately 50 mm3, nude mice are orally administered vehicle or Tetrandrine (NSC-77037) (30 mg/kg) every other day for 37 days. Tetrandrine (NSC-77037) treatment inhibits tumor growth by reducing the tumor volume and weight[2].

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

    臨床実験
    分子量

    622.75

    分子式

    C38H42N2O6

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    COC1=CC(CCN(C)[C@@]2([H])CC3=CC(O4)=C(OC)C=C3)=C2C(OC5=C(OC)C=C6C([C@]([H])(CC7=CC=C4C=C7)N(C)CC6)=C5)=C1OC

    Structure Classification
    Initial Source
    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 5 mg/mL (8.03 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM --- --- ---
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    純度とドキュメンテーション

    純度: 99.90%

    参考文献
    細胞実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 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
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    製品名:
    Tetrandrine
    製品番号:
    HY-13764
    数量:
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