2. Membrane Transporter/Ion Channel Neuronal Signaling Immunology/Inflammation GPCR/G Protein Apoptosis
  3. Potassium Channel Histamine Receptor Na+/Ca2+ Exchanger Caspase Apoptosis
  4. Terfenadine

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

Cat. No.: HY-B1193 Purity: 99.91%
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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.

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Terfenadine Chemical Structure

Terfenadine Chemical Structure

CAS No. : 50679-08-8

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10 mM * 1 mL in DMSO
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Based on 2 publication(s) in Google Scholar

Terfenadine Related Antibodies

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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

 

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.

Terfenadine Related Antibodies

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.
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 : 0.67 mg/mL (1.42 mM; Need ultrasonic)

*"≥" 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
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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(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%

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

Handling Instructions (2659 KB)
References

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
H2O / DMSO 1 mM 2.1201 mL 10.6006 mL 21.2013 mL 53.0032 mL
DMSO 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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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