Tetrandrine (Synonyms: NSC-77037; d-Tetrandrine)

Name: Tetrandrine
Brand: MedChemExpress
SKU: HY-13764
Rating: 5.0 (12 reviews)

Cat. No.: HY-13764 Purity: 99.91%: FAQs
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Tetrandrine (NSC-77037; d-Tetrandrine) is a bis-benzyl-isoquinoline alkaloid, which inhibits voltage-gated Ca²⁺ current (ICa) and Ca²⁺-activated K⁺ current.

For research use only. We do not sell to patients.

Tetrandrine Chemical Structure

CAS No. : 518-34-3

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Based on 12 publication(s) in Google Scholar

Other Forms of Tetrandrine:

Tetrandrine (Standard) Get quote

9 Publications Citing Use of MCE Tetrandrine

: 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.

: 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.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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]
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]

In Vitro

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.

In Vivo

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.

Clinical Trial

Molecular Weight

622.75

Formula

C₃₈H₄₂N₂O₆

CAS No.

518-34-3

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.5 mg/mL (0.80 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.5 mg/mL (0.80 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.5 mg/mL (0.80 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (16.06 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.91%

Select Batch:

Data Sheet (285 KB) SDS (393 KB)

COA (259 KB) LCMS (265 KB)

Handling Instructions (2659 KB)

References

[1]. Wang G, et al. Tetrandrine blocks a slow, large-conductance, Ca(2+)-activated potassium channel besides inhibiting a non-inactivating Ca2+ current in isolated nerve terminals of the rat neurohypophysis. Pflugers Arch. 1992 Sep;421(6):558-65. [Content Brief]

[2]. Zhang Z, et al. The plant alkaloid tetrandrine inhibits metastasis via autophagy-dependent Wnt/β-catenin and metastatic tumor antigen 1 signaling in human liver cancer cells. J Exp Clin Cancer Res. 2018 Jan 15;37(1):7. [Content Brief]

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.
References	[1]. Wang G, et al. Tetrandrine blocks a slow, large-conductance, Ca(2+)-activated potassium channel besides inhibiting a non-inactivating Ca2+ current in isolated nerve terminals of the rat neurohypophysis. Pflugers Arch. 1992 Sep;421(6):558-65. [Content Brief] [2]. Zhang Z, et al. The plant alkaloid tetrandrine inhibits metastasis via autophagy-dependent Wnt/β-catenin and metastatic tumor antigen 1 signaling in human liver cancer cells. J Exp Clin Cancer Res. 2018 Jan 15;37(1):7. [Content Brief]

Complete Stock Solution Preparation Table

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
DMSO	5 mM	0.3212 mL	1.6058 mL	3.2116 mL	8.0289 mL

Tetrandrine Related Classifications

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.

Keywords:

Tetrandrine518-34-3NSC-77037 d-TetrandrineNSC77037NSC 77037Calcium ChannelPotassium ChannelParasiteCa2+ channelsCa channelsKcsAInhibitorinhibitorinhibit

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Tetrandrine (Synonyms: NSC-77037; d-Tetrandrine)

Customer Review

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Tetrandrine Related Antibodies

9 Publications Citing Use of MCE Tetrandrine

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Customer Review

Tetrandrine Related Antibodies

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Complete Stock Solution Preparation Table

Tetrandrine Related Classifications

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