Astemizole
Cat. No.：YN320605
CAS No. ：68844-77-9
| 产品名称: | Astemizole |
| CAS No.: | 68844-77-9 |
| Chemical Name: | 1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine |
| Synonyms: | R 43512 |
| 分子量: | 458.57 |
| 分子式: | C₂₈H₃₁FN₄O |
| SMILES: | COC1=CC=C(CCN2CCC(NC3=NC4=CC=CC=C4N3CC5=CC=C(F)C=C5)CC2)C=C1 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Astemizole (R 43512) 是一个长效的二代抗组胺药物，是常用的抗过敏药物，是组胺 H1 受体 (histamine H1-receptor) 的拮抗剂，IC50值为 4 nM。Astemizole 同时还具有hERG K+通道的阻断活性，IC50值为 0.9 nM。Astemizole 还具有抗胆碱能和止痒作用。 |
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Du, L.P., Tsai, K.C., Li, M.Y., et al.The pharmacophore hypotheses of IKr potassium channel blockers: Novel class III antiarrhythmic agentsBioorg. Med. Chem. Lett.14(18),4771-4777(2004)
Ficker, E., Obejero-Paz, C.A., Zhao, S., et al.The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutationsJ. Biol. Chem.277(7),4989-4998(2002)
García-Quiroz, J., García-Becerra, R., Santos-Martínez, N., et al.In vivo dual targeting of the oncogenic Ether-à-go-go-1 potassium channel by calcitriol and astemizole results in enhanced antineoplastic effects in breast tumorsBMC Cancer14,2-10(2014)
