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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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