167465-36-3
167465-36-3 結(jié)構(gòu)式
基本信息
唑喹達(dá)三鹽酸鹽
ZOSUQUIDAR 三鹽酸鹽
P-糖蛋白抑制劑(唑喹達(dá)三鹽酸鹽)
化合物ZOSUQUIDAR 3HCL
(2R)-1-{4-[(1AR,6R,10BS)-1,1-二氟-1,1A,6,10B-四氫二苯并[A,E]環(huán)丙并[C]環(huán)庚烯-6-基]哌嗪-1-基}-3-(喹啉-5-基氧基)丙-2-醇三鹽酸鹽
D06387
LY335979
RS 33295-198
Zosuquidar 3HCl
Trihydrochloride
Zosuquidar TriHCl
Zosuquidar (LY335979
LY335979, RS 33295-198
RS-33295-198, ZOSUQUIDAR
物理化學(xué)性質(zhì)
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
| 2024/11/08 | S1481 | 唑喹達(dá)三鹽酸鹽 Zosuquidar (LY335979) 3HCl | 167465-36-3 | 5mg | 1398.44元 |
| 2024/11/08 | S1481 | 唑喹達(dá)三鹽酸鹽 Zosuquidar (LY335979) 3HCl | 167465-36-3 | 10mM(1mL in DMSO) | 1970元 |
| 2024/11/08 | HY-50671 | 唑喹達(dá)三鹽酸鹽 Zosuquidar trihydrochloride | 167465-36-3 | 5mg | 900元 |
常見問題列表
| Target | Value |
|
P-gp
(Cell-free assay) | 60 nM(Ki) |
LY335979 競爭性抑制[LY335979作用于表達(dá)P-gp的白血病細(xì)胞系，包括K562/HHT40, K562/HHT90, K562/DOX 和 HL60/DNR，顯著恢復(fù)藥物敏感性，且作用于攜帶活性P-gp的原發(fā)性AML細(xì)胞，增強(qiáng)蒽環(huán)類藥物(Daunorubicin, Idarubicin, Mitoxantrone)和gemtuzumab ozogamicin 的毒性。 最新文獻(xiàn)說明LY335979作用于ABCB1轉(zhuǎn)導(dǎo)的細(xì)胞，完全抑制(Z)-endoxifen在頂端調(diào)控的運(yùn)輸。
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.