Astemizole

Astemizole is a non-sedating antihistamine that antagonizes the histamine H1 receptor with a Ki value of 4.4 nM. It is considerably less potent at muscarinic acetylcholine receptors (Ki = 2.4 µM). Astemizole is also a potent blocker of ether-a-go-go-related gene (ERG) potassium channels (IC50 = ~1 nM) that has been used to study long QT syndrome type 2. Furthermore, because it can target oncogenic ERG1 and ERG potassium channels, astemizole has been explored as a potential antineoplastic agent for decreasing proliferation of various cancer cells.Formal Name: 1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine. CAS Number: 68844-77-9. Synonyms: NSC 329963. Molecular Formula: C28H31FN4O. Formula Weight: 458.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 20 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml, Ethanol: 5 mg/ml. lambdamax: 215, 250, 285 nm. SMILES: COC1=CC=C(CCN2CCC(NC3=NC4=C(C=CC=C4)N3CC5=CC=C(F)C=C5)CC2)C=C1. InChi Code: InChI=1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31). InChi Key: GXDALQBWZGODGZ-UHFFFAOYSA-N.