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Submit ReviewTerfenadine
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)
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 |
| InChI Key | GUGOEEXESWIERI-UHFFFAOYSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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 |
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Product Datasheets for Terfenadine
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.
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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:
Francis et al (2012) Inhibition of histidine decarboxylase ablates the autocrine tumorigenic effects of histamine in human cholangiocarcinoma. Gut 61 753 PMID: 21873469
Rui et al (2020) Antihistamine Drug Ebastine Inhibits Cancer Growth by Targeting Polycomb Group Protein EZH2. Mol Cancer Ther 19 2023-2033 PMID: 32855270
Pérez-Gómez et al (2018) A phenotypic Caenorhabditis elegans screen identifies a selective suppressor of antipsychotic-induced hyperphagia. Nat Commun 9 5272 PMID: 30532051
Masafumi et al (2021) Cardioluminescence in Transgenic Zebrafish Larvae: A Calcium Imaging Tool to Study Drug Effects and Pathological Modeling. Biomedicines 9 PMID: 34680411
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
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.)
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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.
Literature in this Area
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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.