唑喹达三盐酸盐
中文名称 | 唑喹达三盐酸盐 |
---|---|
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;LY 335979; LY-335979; LY335979; D06387; RS33295198; ZOSUQUIDAR HCL; ZOSUQUIDAR 3HCL; ZOSUQUIDAR TRIHYDROCHLORIDE;(R)-1-(4-((1AR,6R,10BS)-1,1-二氟-1,1A,6,10B-四氢二苯并[A,E]环丙烷[C][7]轮烯-6-基)哌嗪-1-基)-3-(喹啉-5-基氧基)丙-2-醇三盐酸盐 |
英文名称 | ZOSUQUIDAR TRIHYSROCHLORIDE |
英文同义词 | Zosuquidar 3HCl;Zosuquidar trihydrochloride, >=98%;RS 33295-198;LY335979 (Zosuquidar 3HCl);ZOSUQUIDAR TRIHYSROCHLORIDE;LY335979, RS 33295-198;Zosuquidar Trihydrochloride;[6(R)-(1aα,6α,10bα)]-4-(1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl)-α-[(5-quinolinyloxy)Methyl]-piperazineethanol trihydrochloride, (2R)-anti-5-{3-[4-(10,11-difluoroMethanodibenzosuber-5-yl)piperazin-1-yl]-2-hydroxypropoxy |
CAS号 | 167465-36-3 |
分子式 | C32H32ClF2N3O2 |
分子量 | 564.07 |
EINECS号 | |
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 |
Mol文件 | 167465-36-3.mol |
结构式 |
唑喹达三盐酸盐 性质
熔点 | 172-176°C |
---|---|
储存条件 | Inert atmosphere,Room Temperature |
溶解度 | 可溶于甲醇(轻微)、水(轻微、超声处理) |
形态 | 固体 |
颜色 | 淡黄色至浅黄色 |
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/08/19 | S1481 | 唑喹达三盐酸盐 Zosuquidar (LY335979) 3HCl | 167465-36-3 | 5mg | 1398.44元 |
2024/08/19 | S1481 | 唑喹达三盐酸盐 Zosuquidar (LY335979) 3HCl | 167465-36-3 | 10mM(1mL in DMSO) | 1970元 |