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CP-100356 hydrochloride

CAS No. 142715-48-8

CP-100356 hydrochloride( —— )

Catalog No. M33840 CAS No. 142715-48-8

CP-100356 hydrochloride is an orally active, low micromolar dual inhibitor of MDR1 (P-gp) and BCRP, a nucleotide-derived substrate analogue that inhibits MDR1-mediated Calcein-AM and BCRP-mediated Prazosin transporters.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    CP-100356 hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    CP-100356 hydrochloride is an orally active, low micromolar dual inhibitor of MDR1 (P-gp) and BCRP, a nucleotide-derived substrate analogue that inhibits MDR1-mediated Calcein-AM and BCRP-mediated Prazosin transporters.
  • Description
    CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 μM for inhibitingMDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=～66 μM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 μM).
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Membrane Transporter/Ion Channel
  • Target
    BCRP
  • Recptor
    BCRP
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    142715-48-8
  • Formula Weight
    597.1
  • Molecular Formula
    C31H37ClN4O6
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 11.36 mg/mL (19.03 mM; Ultrasonic (<60°C)
  • SMILES
    Cl.COc1ccc(CCNc2nc(N3CCc4cc(OC)c(OC)cc4C3)c3cc(OC)c(OC)cc3n2)cc1OC
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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.?
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