Terfenadine

Name: Terfenadine
Brand: Tocris Bioscience
SKU: 3948
Rating: 5 (1 reviews)

Tocris Bioscience a Bio-Techne Brand

Catalog # 3948

Citations (3)

(1)

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Key Product Details

Description:	H₁ antagonist. Also K_V11.1 (hERG) and K_ir6 (K_ATP) channel blocker
Chemical Name:	α-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol
Purity:	≥98% (HPLC)
Molecular Weight:	471.67

View Full Technical Details for Terfenadine

Biological Activity for Terfenadine

Terfenadine is a histamine H₁ receptor antagonist. Also blocks K_V11.1 (hERG) and K_ir6 (K_ATP) channels (IC₅₀ values are 204 nM and 1.2 μM respectively). Inhibits the delayed rectifier K⁺ current (I_Kr) 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 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	10.60 mL	21.20 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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References for Terfenadine

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

Stork State dependent dissociation of HERG channel inhibitors. Br.J.Pharmacol. 2007 PMID: 17592502
Crumb Loratadine blockade of K⁺ channels in human heart: comparison with terfenadine under physiological conditions. J.Pharmacol.Exp.Ther. 2000 PMID: 10604956
Zunkler Mechanism of terfenadine block of ATP-sensitive K⁺ channels. Br.J.Pharmacol. 2000 PMID: 10928959

Citations for Terfenadine (3)

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Citations are publications that use Bio-Techne products. Selected citations for Terfenadine include:

Pérez-G?mez et al. (2018) A phenotypic Caenorhabditis elegans screen identifies a selective suppressor of antipsychotic-induced hyperphagia. Nat Commun. 9:5272
PMID: 30532051
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
Francis et al. (2012) Inhibition of histidine decarboxylase ablates the autocrine tumorigenic effects of histamine in human cholangiocarcinoma. Gut. 61:753
PMID: 21873469

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Customer Reviews for Terfenadine (1)

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Terfenadine was used to assess its action on BK channels

Name: Anonymous

Species: Human

Assay Type: In Vitro

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.

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Product Documents for Terfenadine

COA

Certificate of Analysis

To download a Certificate of Analysis, please select a batch below.