P-gp inhibitor 3 是一种高效的 P 糖蛋白 (P-gp) 抑制剂。P-gp inhibitor 3 通过激活 P-gp ATP 酶来抑制 P-gp 的外排功能。P-gp inhibitor 3 具有较强的多重耐药性 (MDR) 逆转能力，能增强紫杉醇抗肿瘤活性。
| 生物活性 | P-gp inhibitor 3 is an effectiveP-glycoprotein(P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel[1]. |
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体外研究
(In Vitro) | P-gp inhibitor 3 (compound 16) (10 μM; 72 hours) has appreciable cytotoxicity in KBV cancer cells, with relatively stronger MDR reversal ability[1].
P-gp inhibitor 3 (2.5, 5, 10 μM ; 3 hours) reverses tumor MDR by inhibiting the efflux function of P-gp[1].
P-gp inhibitor 3 (0.25, 0.5, 1 mM; 5 minutes) can significantly increase ATP consumption in a concentration-dependent manner (p<0.01)[1].
P-gp inhibitor 3 (10 μM; 24 hours) inducesapoptosisin KBV cells in the G2/M phase[1].
Cell Cytotoxicity Assay | Cell Line: | KBV cells[1] | | Concentration: | 10 μM | | Incubation Time: | 72 hours | | Result: | Showed appreciable cytotoxicity in KBV cancer cells, and exhibited relatively stronger MDR reversal ability. |
Cell Cycle Analysis | Cell Line: | KBV cells[1] | | Concentration: | 10 μM | | Incubation Time: | 24 hours | | Result: | Induced apoptosis in KBV cells in the G2/M phase. |
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体内研究
(In Vivo) | P-gp inhibitor 3 (10 mg/kg; i.p., once a day, for 1 to 18 days) significantly enhances the anti-tumor activity of paclitaxel and the tumor suppression rate is 56.24%[1].
| Animal Model: | Nude mice xenograft tumor model (6-8 weeks old, BALB/c, male)[1] | | Dosage: | 10 mg/kg for P-gp inhibitor 3; 30 mg/kg for paclitaxel | | Administration: | i.p.; once a day (P-gp inhibitor 3), once every three days (paclitaxel); for 1 to 18 days | | Result: | Significantly enhanced the anti-tumor activity of paclitaxel and the tumor suppression rate was 56.24%. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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