| 货号 | 3489/50 |
| 别名 | 1-[(4-Fluorophenyl)methyl]-N-[1-[2- |
| 供应商 | Tocris |
| 生物活性 | 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. |
| 运输条件 | Blue Ice |
| 存放说明 | 4℃ |
| 纯度 | >99 % |
| 计算分子量 | 458.57 |
| 分子式 | C28H31FN4O |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO and to 25 mM in ethanol |
| CAS号 | 68844-77-9 |
| 参考文献 | Chonget al (2006) A clinical drug library screen identifies astemizole as an antimalarial agent. Nat.Chem.Biol. 2 415. PMID: 16816845. Cavalliet 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. Laduronet al(1981)In vitroandin vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole. Mol.Pharmacol. 21294. |