T9652 Sigma-Aldrich


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,
Quality Level   200
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
SMILES string   CC(C)(C)c1ccc(cc1)C(O)CCCN2CCC(CC2)C(O)(c3ccccc3)c4ccccc4
InChI   1S/C32H41NO2/c1-31(2,3)26-18-16-25(17-19-26)30(34)15-10-22-33-23-20-29(21-24-33)32(35,27-11-6-4-7-12-27)28-13-8-5-9-14-28/h4-9,11-14,16-19,29-30,34-35H,10,15,20-24H2,1-3H3
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)



Terfenadine has been used as a positive control in electrophysiology recordings. It has also been used as a constituent of internal standard solution in liquid chromatography-mass spectrometry (LC-MS).

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.


5, 25 g in poly bottle

Biochem/physiol Actions

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

Terfenadine acts a potential anti-histamine and is used in the treatment of allergic rhinitis and chronic urticaria.

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.

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).

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

Legal Information

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

Safety & Documentation

Safety Information

Hazard statements 
Precautionary statements 
NONH for all modes of transport
WGK Germany 
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable


Certificate of Analysis (COA)

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Certificate of Origin (COO)

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Protocols & Articles


Discover Bioactive Small Molecules for ADME/Tox

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HPLC Analysis of Terfenadine Enantiomers on Astec® Cellulose DMP

From our library of Articles, Sigma-Aldrich presents HPLC Analysis of Terfenadine Enantiomers on Astec® Cellulose DMP
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