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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Soluble in DMSO (25 mg/ml ), ethanol (25 mg/ml), chloroform, methanol, and water (partly miscible).
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Roy et alRoy et al. (PubMed ID 18497958) found that Astemizole, a human ether-a-go-go (hEAG) potassium channel inhibitor, blocked MCF-7 cell proliferation. -SCBT Publication Review
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