Terfenadine CAS: 50679-08-8
MF: C32H41NO2
MW: 471.67
A histamine H1-receptor antagonist, which blocks HERG and KIR6 channels.

Terfenadine (CAS 50679-08-8)

Terfenadine | CAS 50679-08-8 is rated 5.0 out of 5 by 1.
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Alternate Names: α-[4-(1,1-Dmethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol
Application: Terfenadine is a histamine H1-receptor antagonist, which blocks HERG and KIR6 channels
CAS Number: 50679-08-8
Molecular Weight: 471.67
Molecular Formula: C32H41NO2
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).

Terfenadine is a histamine H1-receptor antagonist, which blocks HERG and KIR6 (KATP) channels. The IC values for Terfenadines inhibitory activity against these channels is 204nM for HERG and 1.2µM for KIR6 (KATP). Studies show that Terfenadine inhibits the delayed rectifier K+ in ventricular myocytes. Terfenadine is converted into its more active form, terfenadine carboxylate by the enzyme CYP3A4. Terfenadine is an inhibitor of CYP2C8.


References

1. Zünkler, B.J., et al. 2000. Br. J. Pharmacol. 130: 1571-1574. PMID: 10928959
2. Crumb, W.J., 2000. J. Pharmacol. Exp. Ther. 292: 261-264. PMID: 10604956

Physical State :
Solid
Solubility :
Soluble in chloroform, DMSO (100 nM), ethanol (25 nM), and water (0.001 g/100 ml) at 30° C.
Storage :
Store at 4° C
Melting Point :
146.5-148.5° C
Boiling Point :
~626.8° C at 760 mmHg (Predicted)
Density :
~1.1 g/cm3 (Predicted)
Refractive Index :
n20D 1.58 (Predicted)
IC50 :
HERG: IC50 = 50 nM (human); Histamine H1 receptor: IC50 = 94 nM (human); Alpha-1a adrenergic receptor: IC50 = 2340 nM (human); Cytochrome P450 3A4: IC50 = 320 nM (human); P-glycoprotein 1: IC50 = 1400 nM (human)
Ki Data :
Histamine H1 receptor: Ki= 40 nM (human); HERG: Ki= 320 nM (human)
pK Values :
pKa: 13.32, pKb: 9.42
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
2
RTECS :
TM4969000
PubChem CID :
5405
Merck Index :
14: 9163
MDL Number :
MFCD00079622
EC Number :
256-710-8
SMILES :
CC(C)(C)C1=CC=C(C=C1)C(CCCN2CCC(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O)O

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Crumb (PubMed ID 10604956) found that the Crumb (PubMed ID 10604956) found that the antihistamines loratadine and terfenadine show similar human cardiac K(+) channel-blocking effects that can lead to arrhythmias in the human heart. -SCBT Publication Review
Date published: 2015-02-09
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