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.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 471.67. Batch specific molecular weights may vary from batch to batch due to solvent 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|
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
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
2 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
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
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Literature in this Area
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