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YZ剂描述： 产品名称：Zosuquidar (LY335979) triHydrochloride 产品别名：唑喹达三盐酸盐 英文别名：Zosuquidar trihydrochloride;;RS 33295-198 trihydrochloride;LY-335979 trihydrochloride 靶点：P-gp CAS：167465-36-3 纯度：>98% 外观：见爱必信官网 保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months. 描述： Zosuquidar (LY335979) 3HCl是一种有效的P-glycoprotein（P-糖蛋白）介导的多药耐抗性的调节剂，Ki为60 nM。LY335979 竞争性YZ[3H]vinblastine与P-gp的平衡结合，Ki为 60 nM，通过阻断CEM/VLB100质膜中P-gp的[3H]azidopine的光亲和标记。LY335979 浓度为0.1 μM时，单独给药对药物敏感的MDR细胞系，具有细胞毒性，IC50为6 μM-16 μM，且浓度为 0.5 μM时，完全扭转对 MDR 细胞P388/ADR, MCF7/ADR, 2780AD, 或 UCLA-P3.003VLB溶瘤细胞抗性(Vinblastine, Doxorubicin, 或 Etoposide)。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。 溶解性：DMSO ：31.9 mg/mL (50 mM) 体外研究： LY335979 competitively inhibits equilibrium binding of vinblastine to Pgp by blocking azidopine photoaffinity labeling of the Pgp in CEM/VLB100 plasma membranes. LY335979 alone shows the cytotoxicity to drug-sensitive and MDR cell lines with IC50 ranging from 6 μM-16 μM and produces its ability to completely reverse the resistance of the oncolytics (vinblastine, doxorubicin, or etoposide) to the MDR cell lines P388/ADR, MCF7/ADR, 2780AD, or UCLA-P3.003VLB at concentration of 0.1 and 0.5 μM. LY335979 significantly restores drug sensitivity in P-gp-expressing leukemia cell lines including K562/HHT40, K562/HHT90, K562/DOX and HL60/DNR, and enhances the cytotoxicity of anthracyclines (daunorubicin, idarubicin, mitoxantrone) and gemtuzumab ozogamicin (Mylotarg) in primary AML blasts with active P-gp. A latest paper indicates that LY335979 completely inhibits apically directed transport of (Z)-endoxifen in the ABCB1-transduced cells. 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. 产品信息订购：
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