| 货号 | 21533-1mg |
| 描述 | Zosuquidar is a modulator of P-glycoprotein (P-gp; Ki = 59 nM).1 It restores the sensitivity of P-gp-expressing cancer cells to vinblastine (Item No. 11762), doxorubicin (Item No. 15007), etoposide (Item No. 12092), and paclitaxel (Item No. 10461) when used at 0.1 µM.1 It less potently inhibits cytochrome P450 (CYP) isoforms CYP3A, CYP2D6, and CYP2C9 (Kis = 3.8, 25, and 12 µM, respectively).2 Zosuquidar does not modulate multidrug resistance-associated protein 1 (MRP-1). Zosuquidar significantly enhances the efficacy of chemotherapeutics in mice implanted with P-gp-expressing tumors.1 Through its effects on P-gp, zosuquidar enhances the distribution of P-gp substrates through the blood-brain barrier into the brain.3,4 |
| 别名 | LY335979;RS 33295-198; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Dantzig, A.H.,Shepard, R.L.,Cao, J., et al. Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res. 56(18), 4171-4179 (1996). 2.Dantzig, A.H.,Shepard, R.L.,Law, K.L., et al. Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities. J. Pharmacol. Exp. Ther. 290(2), 854-862 (1999). 3.Choo, E.F.,Leake, B.,Wandel, C., et al. Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes. Drug Metab. Dispos. 28(6), 655-660 (2000). 4.Liu, F.,Wang, X.,Li, Z., et al. P-Glycoprotein (ABCB1) limits the brain distribution of YQA-14, a novel dopamine D3 receptor antagonist. Chem. Pharm. Bull. (Tokyo) 63(7), 512-518 (2015). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 637 |
| 分子式 | C32H31F2N3O2 • 3HCl |
| CAS号 | 167465-36-3 |
| 稳定性 | ≥ 2 years |
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