T9652 Sigma


Synonym: α-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol



Related Categories Application Index, Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Biochemicals and Reagents,
solubility   chloroform: soluble 250 mg plus 5 ml of solvent, clear to very slightly hazy, colorless to faintly yellow
  H2O: soluble 0.01 mg/mL at 30 °C
  1 M HCl: soluble 0.12 mg/mL at 30 °C
  hexane: soluble 0.34 mg/mL at 30 °C
  0.1 M tartaric acid: soluble 0.45 mg/mL
  0.1 M citric acid: soluble 1.1 mg/mL
  methanol: soluble 37.5 mg/mL at 30 °C
  ethanol: soluble in salt form 37.8 mg/mL at 30 °C
originator   Sanofi Aventis
storage temp.   2-8°C
Gene Information   human ... ABCB1(5243), CYP2C8(1558), CYP3A4(1576), HRH1(3269), IL4(3565), IL5(3567), KCNH1(3756), KCNH2(3757)
mouse ... Abcb1a(18671), Abcb1b(18669)
rat ... Hrh1(24448)


Biochem/physiol Actions

Terfenadine inhibits HERG (human ether-a-gogo-related gene) K+ channels. It also blocks the delayed rectifier potassium current (IK) of rat isolated ventricular myocytes with IC50 value of 5.96 μM.

Non-sedating second generation H1 histamine receptor antagonist. Mainly metabolized by Cyp3A4, 5, 7. Inhibits CYP2C8.


5, 25 g in poly bottle

Preparation Note

250 mg of Terfenadine dissolves in 5ml of chloroform to yield a clear, colorless solution. Terfenadine is also soluble at 30° C in 0.1 M citric acid (1.1 mg/ml), water (0.01 mg/ml), methanol (37.5 mg/ml), hexane (0.34 mg/ml), ethanol (37.8 mg/ml), 1 M hydrochloric acid (0.12 mg/ml), and 0.1 M tartaric acid (0.45 mg/ml).


Terfenadine has been used to study the role of histamine in itch related to proteinase-activated receptors (PARs) in mice. Terfenadine has also been used to block histamine receptor type 1 to study the pathogenesis of 2,4-dinitrobenzene sulfonic acid (DNBS)-induced ulcerative colitis in rats.

Features and Benefits

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This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.

This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by Sanofi Aventis. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Legal Information

LOPAC is a registered trademark of Sigma-Aldrich Co. LLC

Other Notes

Tandem Mass Spectrometry data independently generated by Scripps Center for Metabolomics is available to view or download in PDF. T9652.pdf Tested metabolites are featured on Scripps Center for Metabolomics METLIN Metabolite Database. To learn more, visit

Safety & Documentation

Safety Information

Hazard statements 
NONH for all modes of transport
WGK Germany 

Expore Enzymes, Proteins & Cofactors

Biomedical Applications
Protocols & Articles


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