Astemizole

H1-receptor antagonist

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Catalog No. A13899

Availability:Stock in USAIn stock

Product Name Catalog No. Price Qty
Astemizole 100mg A13899-100
$140.00
Astemizole 500mg A13899-500
$420.00

Products are for laboratory research use only. Not for human use. We do not sell to patients.

Quick Overview

Astemizole is a potent antihistamine (H1-receptor antagonist, IC50 = 4 nM) that displays selectivity over dopamine, 5-HT, and muscarinic acetylcholine receptors. This compound has shown potent hERG K+ channel blocking activity (IC50 = 0.9 nM), antimalarial activity in multidrug resistant strains in vitro (IC50 = 227 - 734 nM), and has been used as a chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels.

Astemizole

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Chemical Information

Catalog Num A13899
Actions Antagonist
M. Wt 458.57
Formula C28H31FN4O
Solubility DMSO
Purity >98%
Storage at -20°C 2 years
CAS No. 68844-77-9
Synonyms Astemisan, Hismanal, Histamen, Paralergim
SMILES code COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F
Chemical Name 1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine

Biological Activity

Description
Astemizole is a potent antihistamine (H1-receptor antagonist, IC50 = 4 nM) that displays selectivity over dopamine, 5-HT, and muscarinic acetylcholine receptors. This compound has shown potent hERG K+ channel blocking activity (IC50 = 0.9 nM), antimalarial activity in multidrug resistant strains in vitro (IC50 = 227 - 734 nM), and has been used as a chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels.

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