Terfenadine

Pricing Availability Delivery Time Qty
Cat.No. 3948 - Terfenadine | C32H41NO2 | CAS No. 50679-08-8
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)
Datasheet
Citations (2)
Literature

Biological Activity

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

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

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

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.

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

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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:


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View Related Products by Product Action

View all Histamine H1 Receptor Antagonists

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2 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

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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