P-gp inhibitor 1

Research use only, not for human use.

P-gp inhibitor 1 inhibits reversing P-glycoprotein-mediated multidrug resistance with an EC50 of 57.9 nM (K562/A02 cells).

P-gp inhibitor 1 inhibits reversing P-glycoprotein-mediated multidrug resistance with an EC50 of 57.9 nM (K562/A02 cells).(In Vitro):In K562/A02 MDR cells, P-gp inhibitor 1 (0.1, 1, 5 μM, 1 h) boosts the potency of other MDR-related cytotoxic agents with different structures, increases the accumulation of DOX, blocks Pgp-mediated Rh123 efflux, and suppresses P-gp ATPase activity.

P-gp inhibitor 1 (12k) possesses high potency (EC50=57.9±3.5 nM), low cytotoxicity, and long duration of activity in reversing doxorubicin (DOX) resistance in K562/A02 cells (1 μM, 80 minutes). P-gp inhibitor 1 also boosts the potency of other MDR-related cytotoxic agents with different structures, increases accumulation of DOX, blocks Pgp-mediated Rh123 efflux, and suppresses P-gp ATPase activity in K562/A02 MDR cells (0.1, 1, 5 μM, 1 hour). Western Blot Analysis Cell Line:K562/A02 cell Concentration:0.1, 0.5, or 2.0 μM Incubation Time:72 hours Result:MDR reversal by 12k was not caused by a decreased protein expression but instead most likely due to direct inhibition of P-gp efflux.

——

——

Others

Other Targets

Histamine Receptor

——

——

2050747-49-2

517.633

C32H31N5O2

>98% (HPLC)

In Vitro:?DMSO : 16.67 mg/mL (32.21 mM)

COc1cc2CCN(CCc3ccc(Nc4nc(nc5ccccc45)-c4ccncc4)cc3)Cc2cc1OC

——

(-20℃)

With Ice Pack

≥ 2 years