MW:636.99
溶解性:DSMO 127 mg/mL Water 23 mg/mL Ethanol <1 mg/ml
纯度:>99%
描述:
As a selective inhibitor of P-gp, LY335979 can potently inhibit P-gp with Ki of 59 nM, but does not modulate MRP-mediated resistance by MRP1 (ABCC1) and MRP2 (ABCC2). LY335979 is 500-1500 times more potent than cyclosporin A or verapamil in restoring Pgp substrate accumulation in the MDR cell line HL60/VCR. LY335979 could effectively block Pgp function on isolated CD56(+) lymphocytes and CD56(+) lymphocytes in whole blood with IC50 of 1.2 nM and 174 nM.
参考文献:
[1] Dantzig, A. H., K. L. Law, et al. (2001). "Reversal of multidrug resistance by the P-glycoprotein modulator, LY335979, from the bench to the clinic." Curr Med Chem 8(1): 39-50.
[2] Green, L. J., P. Marder, et al. (2001). "Modulation by LY335979 of P-glycoprotein function in multidrug-resistant cell lines and human natural killer cells." Biochem Pharmacol 61(11): 1393-1399.
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