1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel
  3. dl-Tetrandrine

dl-Tetrandrine is an orally active and brain-penetrant calcium channel blocker that inhibits voltage-dependent calcium channels. dl-Tetrandrine selectively blocks Ca2+ influx with an IC50 value of approximately 1-10 μM. dl-Tetrandrine exerts anti-inflammatory, immunosuppressive, and anti-arrhythmic activities by inhibiting intracellular calcium overload, and can reverse multidrug resistance in tumor cells. dl-Tetrandrine is promising for research of autoimmune diseases (such as rheumatoid arthritis), cardiovascular diseases, and tumor drug resistance reversal.

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dl-Tetrandrine

dl-Tetrandrine Chemical Structure

CAS No. : 23495-89-8

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Description

dl-Tetrandrine is an orally active and brain-penetrant calcium channel blocker that inhibits voltage-dependent calcium channels. dl-Tetrandrine selectively blocks Ca2+ influx with an IC50 value of approximately 1-10 μM. dl-Tetrandrine exerts anti-inflammatory, immunosuppressive, and anti-arrhythmic activities by inhibiting intracellular calcium overload, and can reverse multidrug resistance in tumor cells. dl-Tetrandrine is promising for research of autoimmune diseases (such as rheumatoid arthritis), cardiovascular diseases, and tumor drug resistance reversal[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 CC50
>33 μM
Compound: Tetrandrine (Fanchinine)
Toxicity CC50 against VERO-E6 cells determined at 48 hours by high content imaging (same conditions as 2_LEY without exposure to 0.01 MOI SARS CoV-2 virus)
Toxicity CC50 against VERO-E6 cells determined at 48 hours by high content imaging (same conditions as 2_LEY without exposure to 0.01 MOI SARS CoV-2 virus)
10.6019/CHEMBL4495565
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
Vero C1008 IC50
>5.01 × 105M
Compound: COVC-2820786116
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of VERO-E6 cells after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of VERO-E6 cells after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
10.6019/CHEMBL4651402
Vero C1008 IC50
11.66 μM
Compound: Tetrandrine (Fanchinine)
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of VERO-E6 cells after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of VERO-E6 cells after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
10.6019/CHEMBL4495565
VSMC IC50
1.48 μM
Compound: Tetrandrine
Antivegetative activity against rat VSMC
Antivegetative activity against rat VSMC
[PMID: 20708932]
Molecular Weight

622.75

Formula

C38H42N2O6

CAS No.
SMILES

COC1=C2C3=C(C=C1OC)CCN(C)[C@@]3([H])CC4=CC=C(OC)C(OC5=CC=C(C[C@@]6([H])C7=CC(O2)=C(C=C7CCN6C)OC)C=C5)=C4

Structure Classification
Initial Source
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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    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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dl-Tetrandrine
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