CP-100356

• Description:

  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].

• 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

• CAS Number:

  142716-85-6