Terfenadine (Synonyms: (±)-Terfenadine; MDL-991)

Name: Terfenadine
Brand: MedChemExpress
SKU: HY-B1193
Rating: 5.0 (3 reviews)

Cat. No.: HY-B1193 Purity: 99.91%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC₅₀ of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca²⁺ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.

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

Terfenadine Chemical Structure

CAS No. : 50679-08-8

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 3 publication(s) in Google Scholar

Other Forms of Terfenadine:

Terfenadine-d3 Get quote
Terfenadine (Standard) Get quote

3 Publications Citing Use of MCE Terfenadine

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

Biological Activity
Purity & Documentation
References
Customer Review

Description

Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC₅₀ of 204 nM^[1]. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca²⁺ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9^[2].

IC₅₀ & Target

H₁ Receptor

Caspase-4

Caspase-2

Caspase-9

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.93 μM Compound: terfenadine	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
HEK293	IC₅₀	0.022 μM Compound: Terfenadine	Inhibition of human ERG expressed in HEK293 cells by patch clamp method Inhibition of human ERG expressed in HEK293 cells by patch clamp method	[PMID: 28481112]
HEK293	IC₅₀	0.03 μM Compound: Terfenadine	Inhibition of wild-type human ERG expressed in HEK293 cells by whole cell patch clamp method Inhibition of wild-type human ERG expressed in HEK293 cells by whole cell patch clamp method	[PMID: 19260734]
HEK293	IC₅₀	0.03 μM Compound: Terfenadine	Inhibition of human ERG td[wt:Y652A] mutant expressed in HEK293 cells by whole cell patch clamp method Inhibition of human ERG td[wt:Y652A] mutant expressed in HEK293 cells by whole cell patch clamp method	[PMID: 19260734]
HEK293	IC₅₀	0.03 μM Compound: Terfenadine	Inhibition of human ERG td[wt:F656A] mutant expressed in HEK293 cells by whole cell patch clamp method Inhibition of human ERG td[wt:F656A] mutant expressed in HEK293 cells by whole cell patch clamp method	[PMID: 19260734]
HEK293	IC₅₀	0.03 μM Compound: Terfenadine	Inhibition of human ERG S624A mutant expressed in HEK293 cells by whole cell patch clamp method Inhibition of human ERG S624A mutant expressed in HEK293 cells by whole cell patch clamp method	[PMID: 19260734]
HEK293	IC₅₀	0.056 μM Compound: figure 2, R2C1	Inhibition of human Erg expressed in HEK293 cells assessed as rubidium efflux after 4 hrs by atomic absorbance spectrometric analysis Inhibition of human Erg expressed in HEK293 cells assessed as rubidium efflux after 4 hrs by atomic absorbance spectrometric analysis	[PMID: 22542010]
HEK293	IC₅₀	0.086 μM Compound: Terfenadine	Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by manual patch clamp assay Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by manual patch clamp assay	[PMID: 30624934]
HEK293	IC₅₀	0.35 μM Compound: Terfenadine	Inhibition of human ERG Y652A mutant expressed in HEK293 cells by whole cell patch clamp method Inhibition of human ERG Y652A mutant expressed in HEK293 cells by whole cell patch clamp method	[PMID: 19260734]
HEK293	IC₅₀	0.96 μM Compound: Terfenadine	Inhibition of human ERG F656A mutant expressed in HEK293 cells by whole cell patch clamp method Inhibition of human ERG F656A mutant expressed in HEK293 cells by whole cell patch clamp method	[PMID: 19260734]
HEK293	IC₅₀	1.2 μM Compound: Terfenadine	Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay	[PMID: 32392053]
HEK293	IC₅₀	1.32 μM Compound: Terfenadine	Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit	[PMID: 22761000]
HEK293	IC₅₀	130 nM Compound: 1a, terfenadine	Displacement of [3H]astemizole from human ERG expressed in HEK293 cells by scintillation counting method Displacement of [3H]astemizole from human ERG expressed in HEK293 cells by scintillation counting method	[PMID: 25238555]
HEK293	IC₅₀	56 μM Compound: 41, Terfenadine	Inhibition of human ERG potassium channel in HEK293 cells by patch clamp assay Inhibition of human ERG potassium channel in HEK293 cells by patch clamp assay	[PMID: 16931010]
HEK293	IC₅₀	971 nM Compound: Terfenadine	Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA	[PMID: 21300721]
L929	IC₅₀	312 nM Compound: rac-1	Inhibition of human ERG in L929 cells by whole cell patch-clamp assay Inhibition of human ERG in L929 cells by whole cell patch-clamp assay	[PMID: 19660947]
L929	IC₅₀	312 nM Compound: rac-1	Inhibition of human ERG in L929 cells at 10 uM by whole cell patch-clamp assay Inhibition of human ERG in L929 cells at 10 uM by whole cell patch-clamp assay	[PMID: 19660947]
LLC-PK1	IC₅₀	1.4 μM Compound: Terfenadine	Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	2 μM Compound: Terfenadine	Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	23 μM Compound: Terfenadine	Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
Ventricular myocyte	IC₅₀	0.142 μM Compound: Terfenadine	Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes	[PMID: 22761000]
Ventricular myocyte	IC₅₀	0.25 μM Compound: Terfenadine	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	[PMID: 22761000]
Ventricular myocyte	IC₅₀	0.375 μM Compound: Terfenadine	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	[PMID: 22761000]
Ventricular myocyte	IC₅₀	375 nM Compound: Terfenadine	Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes	[PMID: 21300721]

In Vitro

Terfenadine ((±)-Terfenadine) (4-20 μM; 24 hours) induces dose and time-dependent apoptosis on A375 melanoma cells. The IC₅₀ after 24 h of TEF treatment in complete medium was 10.4 μM for A375 cells, 9.9 μM for Hs294T cells and 9.6 for HT144 cells^[2].
? Terfenadine (2-10 μM; 8 hours) induces dose-dependent cytotoxicity^[2].
? Terfenadine (10 μM; 8 hours) causes a massive vacuolization of the cytoplasm and autophagic vacuoles of both double and multiple membranes and at various stages. Terfenadine induces autophagy by ROS-dependent and -independent mechanisms^[2].

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

Apoptosis Analysis^[2]

Cell Line:	A375, HT144 and Hs294T cells
Concentration:	4, 8, 12, 16, 20 μM
Incubation Time:	24 hours
Result:	Induced dose and time-dependent apoptosis.

Cell Cytotoxicity Assay^[2]

Cell Line:	A375 melanoma cells
Concentration:	2, 4, 6, 8, 10 μM
Incubation Time:	8 hours
Result:	Induces dose-dependent cytotoxicity.

Cell Autophagy Assay^[2]

Cell Line:	A375 cells
Concentration:	10 μM
Incubation Time:	8 hours
Result:	Caused a massive vacuolization of the cytoplasm and autophagic vacuoles of both double and multiple membranes and at various stages.

In Vivo

Terfenadine (p.o.; 40 mg/kg; for 16 days) produces a significant inhibition of tumour growth rate and enhances the anti-cancer effect of EPI in chemo-resistant NSCLC xenograft models^[3].

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

Animal Model:	6-week-old male BALB/cA-nu mice^[3]
Dosage:	40 mg/kg
Administration:	P.o.; for 16 days
Result:	Produced a significant inhibition of tumour growth rate.

Molecular Weight

471.67

Formula

C₃₂H₄₁NO₂

CAS No.

50679-08-8

Appearance

Solid

Color

White to off-white

SMILES

OC(C1=CC=C(C(C)(C)C)C=C1)CCCN2CCC(C(C3=CC=CC=C3)(O)C4=CC=CC=C4)CC2

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 : ≥ 50 mg/mL (106.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1201 mL	10.6006 mL	21.2013 mL
5 mM	0.4240 mL	2.1201 mL	4.2403 mL
10 mM	0.2120 mL	1.0601 mL	2.1201 mL

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: ≥ 2.5 mg/mL (5.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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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 (277 KB) SDS (398 KB)

COA (246 KB) HNMR (290 KB) RP-HPLC (245 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. Kamiya K, et al. Molecular determinants of hERG channel block by terfenadine and cisapride. J Pharmacol Sci. 2008 Nov;108(3):301-307. [Content Brief]

[2]. Nicolau-Galmés F, et al. Terfenadine induces apoptosis and autophagy in melanoma cells through ROS-dependent and -independent mechanisms. Apoptosis. 2011 Dec;16(12):1253-67. [Content Brief]

[3]. An L, et al. Terfenadine combined with epirubicin impedes the chemo-resistant human non-small cell lung cancer both in vitro and in vivo through EMT and Notch reversal. Pharmacol Res. 2017 Oct;124:105-115. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1201 mL	10.6006 mL	21.2013 mL	53.0032 mL
	5 mM	0.4240 mL	2.1201 mL	4.2403 mL	10.6006 mL
	10 mM	0.2120 mL	1.0601 mL	2.1201 mL	5.3003 mL
	15 mM	0.1413 mL	0.7067 mL	1.4134 mL	3.5335 mL
	20 mM	0.1060 mL	0.5300 mL	1.0601 mL	2.6502 mL
	25 mM	0.0848 mL	0.4240 mL	0.8481 mL	2.1201 mL
	30 mM	0.0707 mL	0.3534 mL	0.7067 mL	1.7668 mL
	40 mM	0.0530 mL	0.2650 mL	0.5300 mL	1.3251 mL
	50 mM	0.0424 mL	0.2120 mL	0.4240 mL	1.0601 mL
	60 mM	0.0353 mL	0.1767 mL	0.3534 mL	0.8834 mL
	80 mM	0.0265 mL	0.1325 mL	0.2650 mL	0.6625 mL
	100 mM	0.0212 mL	0.1060 mL	0.2120 mL	0.5300 mL

Terfenadine 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:

Terfenadine50679-08-8(±)-Terfenadine MDL-991MDL991MDL 991MDL-991Potassium ChannelHistamine ReceptorNa+/Ca2+ ExchangerCaspaseApoptosisKcsAInhibitorinhibitorinhibit

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Terfenadine (Synonyms: (±)-Terfenadine; MDL-991)

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Other Forms of Terfenadine:

Terfenadine Related Antibodies

3 Publications Citing Use of MCE Terfenadine

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•Related Small Molecules:

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View All Histamine Receptor Isoform Specific Products:

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Biological Activity

Purity & Documentation

References

Customer Review

Terfenadine Related Antibodies

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Complete Stock Solution Preparation Table

Terfenadine Related Classifications

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