167465-36-3
167465-36-3 结构式
基本信息
唑喹达三盐酸盐
ZOSUQUIDAR 三盐酸盐
P-糖蛋白抑制剂(唑喹达三盐酸盐)
化合物ZOSUQUIDAR 3HCL
(2R)-1-{4-[(1AR,6R,10BS)-1,1-二氟-1,1A,6,10B-四氢二苯并[A,E]环丙并[C]环庚烯-6-基]哌嗪-1-基}-3-(喹啉-5-基氧基)丙-2-醇三盐酸盐
D06387
LY335979
RS 33295-198
Zosuquidar 3HCl
Trihydrochloride
Zosuquidar TriHCl
Zosuquidar (LY335979
LY335979, RS 33295-198
RS-33295-198, ZOSUQUIDAR
常见问题列表
| Target | Value |
|
P-gp
(Cell-free assay) | 60 nM(Ki) |
LY335979 竞争性抑制[LY335979作用于表达P-gp的白血病细胞系，包括K562/HHT40, K562/HHT90, K562/DOX 和 HL60/DNR，显著恢复药物敏感性，且作用于携带活性P-gp的原发性AML细胞，增强蒽环类药物(Daunorubicin, Idarubicin, Mitoxantrone)和gemtuzumab ozogamicin 的毒性。 最新文献说明LY335979作用于ABCB1转导的细胞，完全抑制(Z)-endoxifen在顶端调控的运输。
Zosuquidar trihydrochloride is only moderately active as an inhibitor of P-gp at the blood-brain. An oral dose of 25 mg/kg of zosuquidar trihydrochloride increases the brain concentrations by about 2.5-fold at 1 h and 5-fold at 24 h after paclitaxel administrationbarrier. Zosuquidar enhances the brain uptake of nelfinavir in a dose-dependent manner. Brain tissue/plasma nelfinavir concentration ratios increase from 0.06±0.03 in the absence of zosuquidar administration and 0.09±0.02 between 2 and 6 h after a 2 mg/kg intravenous dose of zosuquidar to 0.85±0.19 after 6h and 1.58±0.67 after 20 mg/kg zosuquidar.