R&D Systems Inc. Tocris Bioscience Boston Biochem

Astemizole

Cat. No. 3489

Astemizole C28H31FN4O [68844-77-9]

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Alternative Name: Hismanal

Chemical Name: 1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine

Biological Activity

Orally active, potent histamine H1 antagonist (IC50 = 4 nM) that displays 20-fold, > 250-fold and > 250-fold selectivity over 5-HT, dopamine and muscarinic acetylcholine receptors respectively. Exhibits antimalarial activity in multidrug resistant strains in vitro (IC50 = 227 - 734 nM). Also potent KV11.1 (hERG) channel blocker (IC50 = 0.9 nM) that displays cardiotoxicity in vivo.

Technical Data

M.Wt:
458.57
Formula:
C28H31FN4O
Solubility:
Soluble to 100 mM in DMSO and to 25 mM in ethanol
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
68844-77-9

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

Laduron et al (1981) In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole. Mol.Pharmacol. 21 294.

Cavalli et al (2002) Towards a pharmacophore for drugs inducing the long QT syndrome: Insights from a CoMFA study of hERG K+ channel blockers. J.Med.Chem. 45 3844. PMID: 12190308.

Chong et al (2006) A clinical drug library screen identifies astemizole as an antimalarial agent. Nat.Chem.Biol. 2 415. PMID: 16816845.

If you know of a relevant citation for this product please let us know.

Keywords: Astemizole, supplier, Potent, hERG, K+, channel, blockers, histamine, H1, antagonists, histaminergic, Orally, active, potent, Potassium, KV, Channels, Human, Ether-A-Go-Go, Gene, voltage-gated, voltage-dependent, Receptors, Histamine, KV11.1

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