Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
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.
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.
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 |
Reconstitution Calculator
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:
Keywords: Terfenadine, supplier, hERG, Human, Ether-A-Go-Go, Gene, KV11.1, KIR6, K+, channel, blockers, histamine, H1, antagonists, histaminergic, Potassium, KV, KATP, Channels, voltage-gated, voltage-dependent, Receptors, a-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol, Voltage-Gated, Potassium, Channels, Histamine, H1, Receptors, Inward, rectifier, Potassium, Channels, Histamine, H1, Receptors, Tocris Bioscience