CP-100356

CP-100356 is an orally active dual MDR1 (P-gp) /BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 is also a weak inhibitor of OATP1B1 (IC50 = ∼66 µM) . CP-100356 is devoid of inhibition against MRP2 and major human P450 enzymes (IC50 > 15 µM) [1].

Product Specifications

CAS Number

[142716-85-6]

UNSPSC

12352005

Target

BCRP; P-glycoprotein

Related Pathways

Membrane Transporter/Ion Channel

Field of Research

Metabolic Disease

Smiles

COC1=CC2=NC(NCCC3=CC=C(C(OC)=C3)OC)=NC(N4CC5=C(CC4)C=C(C(OC)=C5)OC)=C2C=C1OC

Molecular Formula

C31H36N4O6

Molecular Weight

560.64

References & Citations

[1]Kalgutkar AS, et, al. N- (3,4-dimethoxyphenethyl) -4- (6,7-dimethoxy-3,4-dihydroisoquinolin-2[1H]-yl) -6,7-dimethoxyquinazolin-2-amine (CP-100,356) as a "chemical knock-out equivalent" to assess the impact of efflux transporters on oral drug absorption in the rat. J Pharm Sci. 2009 Dec;98 (12) :4914-27.