Cat No.
CEI-0254
Description
LY335979 can potently inhibit P-gp with Ki of 59 nM.
Alias
RS-33295-198
Synonyms
RS-33295-198
CAS No.
167465-36-3
Targets
P-gp
Chemical Name
1-Piperazineethanol, 4-[(1aalpha,6alpha,10balpha)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-alpha-[(5-quinolinyloxy)methyl]-,trihydrochloride
M.Wt
636.99
Purity
>99%
Solubility
DMSO 127 mg/mL Water 23 mg/mL Ethanol
Storage
2 years at -20centigrade Powder
In vitro
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.
