Pricing Availability   Qty
Description: H1 antagonist. Also KV11.1 (hERG) and Kir6 (KATP) channel blocker
Chemical Name: α-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol
Purity: ≥98% (HPLC)
Citations (5)
Reviews (1)
Literature (1)

Biological Activity for Terfenadine

Terfenadine is a histamine H1 receptor antagonist. Also blocks KV11.1 (hERG) and Kir6 (KATP) channels (IC50 values are 204 nM and 1.2 μM respectively). Inhibits the delayed rectifier K+ current (IKr) in guinea pig ventricular myocytes (IC50 = 50 nM). Activity prolongs QT and induces Torsades de pointes (TdP); cardiotoxic in vivo.

Compound Libraries for Terfenadine

Terfenadine is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Terfenadine

M. Wt 471.67
Formula C32H41NO2
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 50679-08-8
PubChem ID 5405
Smiles OC(C3=CC=CC=C3)(C4=CC=CC=C4)C1CCN(CCCC(O)C2=CC=C(C(C)(C)C)C=C2)CC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Terfenadine

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 47.17 100
ethanol 11.79 25

Preparing Stock Solutions for Terfenadine

The following data is based on the product molecular weight 471.67. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.12 mL 10.6 mL 21.2 mL
5 mM 0.42 mL 2.12 mL 4.24 mL
10 mM 0.21 mL 1.06 mL 2.12 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.


Dilution Calculator

Calculate the dilution required to prepare a stock solution.

References for Terfenadine

References are publications that support the biological activity of the product.

Crumb (2000) Loratadine blockade of K+ channels in human heart: comparison with terfenadine under physiological conditions. J.Pharmacol.Exp.Ther. 292 261 PMID: 10604956

Zunkler et al (2000) Mechanism of terfenadine block of ATP-sensitive K+ channels. Br.J.Pharmacol. 130 1571 PMID: 10928959

Stork et al (2007) State dependent dissociation of HERG channel inhibitors. Br.J.Pharmacol. 151 136 PMID: 17592502

If you know of a relevant reference for Terfenadine, please let us know.

View Related Products by Product Action

View all Histamine H1 Receptor Antagonists

Keywords: Terfenadine, Terfenadine supplier, hERG, Human, Ether-A-Go-Go, Gene, KV11.1, KIR6, K+, channel, blockers, histamine, H1, antagonists, histaminergic, Potassium, KV, KATP, Channels, voltage-gated, voltage-dependent, Receptors, a-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol, Voltage-Gated, Histamine, Inward, rectifier, 3948, Tocris Bioscience

5 Citations for Terfenadine

Citations are publications that use Tocris products. Selected citations for Terfenadine include:

Klingerman et al (2014) Second-generation antipsychotics cause a rapid switch to fat oxidation that is required for survival in C57BL/6J mice. Schizophr Bull 40 327 PMID: 23328157

Pérez-Gómez et al (2018) A phenotypic Caenorhabditis elegans screen identifies a selective suppressor of antipsychotic-induced hyperphagia. Nat Commun 9 5272 PMID: 30532051

Rui et al (2020) Antihistamine Drug Ebastine Inhibits Cancer Growth by Targeting Polycomb Group Protein EZH2. Mol Cancer Ther 19 2023-2033 PMID: 32855270

Francis et al (2012) Inhibition of histidine decarboxylase ablates the autocrine tumorigenic effects of histamine in human cholangiocarcinoma. Gut 61 753 PMID: 21873469

Do you know of a great paper that uses Terfenadine from Tocris? Please let us know.

Reviews for Terfenadine

Average Rating: 5 (Based on 1 Review.)

5 Star
4 Star
3 Star
2 Star
1 Star

Have you used Terfenadine?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Filter by:

Terfenadine was used to assess its action on BK channels.
By Anonymous on 12/03/2018
Assay Type: In Vitro
Species: Human

Terfenadine was used to assess its action on BK channels, which are Calcium activated voltage-gated potassium channels that conduct large amounts of potassium ions (K+) across the cell membrane. Results were reliable and reproducible.

review image

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Histamine Receptors Scientific Review

Histamine Receptors Scientific Review

Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.