Astemizole

• Supplier: Tocris Bioscience
• Catalog: 4092
• Prices: $75.00
• Sizes: 50 mg
• Function Type: Antagonist
• Cas Number: 68844-77-9
• Chemical Name: 1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine
• Formula: C28H31FN4O
• Molecular Weight: 458.57
• Purity: >99 %
• Description: Orally active, potent histamine H 1 antagonist (IC 50 = 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 (IC 50 = 227 - 734 nM). Also potent K V 11.1 (hERG) channel blocker (IC 50 = 0.9 nM) that displays cardiotoxicity in vivo .

Product References

Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a - Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a

Cavalli A, Poluzzi E, De Ponti F, Recanatini M. J Med Chem. 2002 Aug 29;45(18):3844-53.

A clinical drug library screen identifies astemizole as an antimalarial agent. - A clinical drug library screen identifies astemizole as an antimalarial agent.

Chong CR, Chen X, Shi L, Liu JO, Sullivan DJ Jr. Nat Chem Biol. 2006 Aug;2(8):415-6. Epub 2006 Jul 2.