中文同义词:
(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;唑喹达盐酸盐;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
英文名称:
ZOSUQUIDAR TRIHYSROCHLORIDE
英文同义词:
Zosuquidar 3HCl;Zosuquidar trihydrochloride, >=98%;Trihydrochloride;Zosuquidar (LY335979) triHydrochloride;D06387;LY 335979; LY-335979; LY335979; D06387; RS33295198;;(αR)-4-[(1aα,6α,10bα)-1,1-Difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-α-[(5-quinolinyloxy)methyl]-1-piperazineethanol trihydrochloride;RS-33295-198; ZOSUQUIDAR; LY-335979
相关类别:
信号转导通路激酶抑制剂;膜转运/离子通道;离子通道;膜转运;小分子抑制剂，天然产物;细胞生物学试剂;Inhibitors;Aromatics;Chiral Reagents;Heterocycles;Intermediates Fine Chemicals;Pharmaceuticals
储存条件
Inert atmosphere,Room Temperature
生物活性
Zosuquidar 3HCl (LY335979, RS 33295-198, D06387) 是一种有效的P-glycoprotein介导的多药耐抗性的调节剂，无细胞试验中Ki为60 nM。Phase 3。
靶点
Target Value
P-gp
(Cell-free assay) 60 nM(Ki)
P-gp
(Cell-free assay)
60 nM(Ki)
体外研究
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。
体内研究
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.
