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Chemical Structure| 518-34-3 Chemical Structure| 518-34-3

Structure of Tetrandrine
CAS No.: 518-34-3

Chemical Structure| 518-34-3

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Tetrandrine, a bis-benzylisoquinoline alkaloid derived from Stephania tetrandra, is a calcium channel blocker that inhibits voltage-gated Ca2+ current (ICa) and Ca2+-activated K+ current.

Synonyms: NSC-77037; d-Tetrandrine; TTD.

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Product Details of Tetrandrine

CAS No. :518-34-3
Formula : C38H42N2O6
M.W : 622.75
SMILES Code : CN1CCC2=CC(OC)=C(O3)C=C2[C@]1([H])CC4=CC=C(OC5=C(OC)C=CC(C[C@@]6([H])C7=C3C(OC)=C(OC)C=C7CCN6C)=C5)C=C4
Synonyms :
NSC-77037; d-Tetrandrine; TTD.
MDL No. :MFCD08689909
InChI Key :WVTKBKWTSCPRNU-KYJUHHDHSA-N
Pubchem ID :73078

Safety of Tetrandrine

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • Calcium Channel

In Vitro:

Cell Line
Concentration Treated Time Description References
HepG2 cells 2 μg/mL 12 hours To detect TET-CTM/L induced apoptosis in HepG2 cells, results showed that TET-CTM/L significantly induced apoptosis. Int J Nanomedicine. 2024 Jan 23;19:727-742.
Huh7 cells 0, 0.5, 1, 2 or 4 µM 24 hours Tetrandrine significantly inhibited the migration and invasion of Huh7 cells J Exp Clin Cancer Res. 2018 Jan 15;37(1):7.
HCCLM9 cells 0, 0.5, 1, 2 or 4 µM 24 hours Tetrandrine significantly inhibited the migration and invasion of HCCLM9 cells J Exp Clin Cancer Res. 2018 Jan 15;37(1):7.
Hep3B cells 0, 0.5, 1, 2 or 4 µM 24 hours Tetrandrine significantly inhibited the migration and invasion of Hep3B cells J Exp Clin Cancer Res. 2018 Jan 15;37(1):7.
HepG2 cells 0.675-20 μg/mL 24 hours To evaluate the cytotoxicity of TET-CTM/L against HepG2 cells, results showed that TET-CTM/L has significant anti-tumor efficacy. Int J Nanomedicine. 2024 Jan 23;19:727-742.
Murine peritoneal macrophages 100 µM 3 hours Tetrandrine inhibited NLRP3 inflammasome activation and reduced the release of IL-1β and IL-18. Acta Pharmacol Sin. 2022 May;43(5):1274-1284.
Cardiac myocytes 10 µM 30 minutes Tetrandrine significantly inhibited Ang II-induced ROS generation Br J Pharmacol. 2010 Feb;159(4):970-81.
K562 2 µM 48 hours Tetrandrine inhibited the proliferation of K562 cells and induced cell cycle arrest at the G0/G1 phase. Cell Death Dis. 2018 May 1;9(5):473.
THP-1 2 µM 48 hours Tetrandrine inhibited the proliferation of THP-1 cells and induced cell cycle arrest at the G0/G1 phase. Cell Death Dis. 2018 May 1;9(5):473.
HL60 2 µM 48 hours Tetrandrine inhibited the proliferation of HL60 cells and induced cell cycle arrest at the G0/G1 phase. Cell Death Dis. 2018 May 1;9(5):473.
U937 2 µM 48 hours Tetrandrine inhibited the proliferation of U937 cells and induced cell cycle arrest at the G0/G1 phase. Cell Death Dis. 2018 May 1;9(5):473.
K562 cells 2 µM 48 hours Tetrandrine induced cell cycle arrest and megakaryocyte differentiation in K562 cells via activation of autophagy. Br J Pharmacol. 2017 Dec;174(23):4308-4328.
6133 cells 2 µM 48 hours Tetrandrine induced cell cycle arrest and megakaryocyte differentiation in 6133 cells via activation of autophagy. Br J Pharmacol. 2017 Dec;174(23):4308-4328.
CMK cells 2 µM 48 hours Tetrandrine induced cell cycle arrest and megakaryocyte differentiation in CMK cells via activation of autophagy. Br J Pharmacol. 2017 Dec;174(23):4308-4328.
HEL cells 2 µM 48 hours Tetrandrine induced cell cycle arrest and megakaryocyte differentiation in HEL cells via activation of autophagy. Br J Pharmacol. 2017 Dec;174(23):4308-4328.
RAW264.7 cells 0.3 µM 6 hours Tetrandrine significantly inhibited RANKL-induced osteoclastogenesis and enhanced the ubiquitination and degradation of Syk through the AhR/c-src/c-Cbl signaling pathway. Cell Death Dis. 2019 Jan 15;10(2):38.
BMMs 0.3 µM 6 hours Tetrandrine significantly inhibited RANKL-induced osteoclastogenesis and enhanced the ubiquitination and degradation of Syk through the AhR/c-src/c-Cbl signaling pathway. Cell Death Dis. 2019 Jan 15;10(2):38.
Human breast cancer cells (MDA-MB-231, MDA-MB-468, MCF-7) 0-5 µM 72 hours Tetrandrine alone or in combination with H89 exhibited antitumor effects on various cancer cells, and the combination showed synergistic effects. J Exp Clin Cancer Res. 2018 Jun 4;37(1):114.
Human hepatoma cells (Hep3B, Huh7) 0-5 µM 72 hours Tetrandrine alone or in combination with H89 exhibited antitumor effects on various cancer cells, and the combination showed synergistic effects. J Exp Clin Cancer Res. 2018 Jun 4;37(1):114.
Human renal carcinoma cells (769-P, ACHN, 786-O) 0-5 µM 72 hours Tetrandrine alone or in combination with H89 exhibited antitumor effects on various cancer cells, and the combination showed synergistic effects. J Exp Clin Cancer Res. 2018 Jun 4;37(1):114.
Human colon cancer cells (LOVO, HCT116) 0-5 µM 72 hours Tetrandrine alone or in combination with H89 exhibited antitumor effects on various cancer cells, and the combination showed synergistic effects. J Exp Clin Cancer Res. 2018 Jun 4;37(1):114.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice HepG2 xenograft tumor model Intraperitoneal injection 1.5 mg/kg Once every two days for 24 days To evaluate the in vivo anti-tumor efficacy of TET-CTM/L, results showed that TET-CTM/L significantly inhibited tumor growth. Int J Nanomedicine. 2024 Jan 23;19:727-742.
Mice Thy1-hTau.P301S transgenic mice Intraperitoneal injection 2.5 mg/kg, 5 mg/kg, 10 mg/kg Every two days for two months To study the effect of Tetrandrine on tau aggregation and cognitive dysfunction, results showed that Tetrandrine reduced tau aggregation in a dose-dependent manner and improved memory function in mice. J Biomed Sci. 2022 Oct 22;29(1):85
Nude mice (BALB/c) MDA-MB-231 xenograft model Oral and intraperitoneal injection 25 mg/kg Every other day for 28 days The combination of Tetrandrine and H89 significantly inhibited tumor growth in vivo, showing synergistic effects. J Exp Clin Cancer Res. 2018 Jun 4;37(1):114.
Nude mice Subcutaneous tumor xenograft model Oral 25 mg/kg or 50 mg/kg Once daily for 13 days Tetrandrine significantly inhibited tumor growth and promoted tumor cell differentiation. Cell Death Dis. 2018 May 1;9(5):473.
Nude mice HCCLM9 subcutaneous tumor xenograft model Oral 30 mg/kg Every other day for 37 days Tetrandrine significantly inhibited lung metastasis of HCCLM9 cells in vivo J Exp Clin Cancer Res. 2018 Jan 15;37(1):7.
Nude mice K562 tumor xenograft model Oral 50 mg/kg Once daily for 23 days Tetrandrine significantly inhibited the growth of K562 tumors, reducing tumor volume and weight. Br J Pharmacol. 2017 Dec;174(23):4308-4328.
C57BL/6J mice Silicosis model Gavage 50 mg/kg or 100 mg/kg Once daily for 4 weeks Tetrandrine alleviated pulmonary inflammation and fibrosis, and improved lung function in silicosis mice. Acta Pharmacol Sin. 2022 May;43(5):1274-1284.
C57/B6 mice Aortic banding (AB) model Oral gavage 50 mg/kg/day Three times a day for one week Tetrandrine significantly attenuated AB-induced cardiac hypertrophy, reduced heart weight/body weight and lung weight/body weight ratios, and inhibited fibrosis and inflammatory response Br J Pharmacol. 2010 Feb;159(4):970-81.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT04308317 Corona Virus Disease 2019,COVI... More >>D-19 Less << PHASE4 UNKNOWN 2021-05-01 Tetrandrine Tablets, Jinhua, Z... More >>hejiang, 321000, China Less <<
NCT05697029 COVID-19 PHASE4 WITHDRAWN 2025-12-12 Peking University Third Hospit... More >>al, Beijing, Beijing, 100191, China Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.61mL

0.32mL

0.16mL

8.03mL

1.61mL

0.80mL

16.06mL

3.21mL

1.61mL

References

 

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