A P-glycoprotein inhibitor
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CP 100,356 (hydrochloride)

Item No. 32853

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-N-[2-(3,4-dimethoxyphenyl)ethyl]-6,7-dimethoxy-2-quinazolinamine, monohydrochloride
CAS Number
142715-48-8
Molecular Formula
C31H36N4O6 • HCl
Formula Weight
597.1
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 40 mg/ml
SMILES
COC1=CC2=C(N3CCC4=CC(OC)=C(C=C4C3)OC)N=C(NCCC5=CC=C(C(OC)=C5)OC)N=C2C=C1OC.Cl
InChi Code
InChI=1S/C31H36N4O6.ClH/c1-36-24-8-7-19(13-25(24)37-2)9-11-32-31-33-23-17-29(41-6)28(40-5)16-22(23)30(34-31)35-12-10-20-14-26(38-3)27(39-4)15-21(20)18-35;/h7-8,13-17H,9-12,18H2,1-6H3,(H,32,33,34);1H
InChi Key
WWCHXVYTCMPAMV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $69

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    5 mg

    $149

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    10 mg

    $256

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    Product Description

    CP 100,356 is an inhibitor of P-glycoprotein (P-gp; IC50 = 0.5 µM for inhibition of calcein AM transport in MDCKII monolayers).1 It is selective for P-gp over multidrug resistance-associated protein 2 (MRP2) at 15 µM, as well as the cytochrome P450 (CYP) isoforms CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 (IC50s = >50 µM for all) and organic anion transporter 1B1 (OATP1B1; IC50 = ~66 µM), but does inhibit breast cancer resistance protein (BCRP; IC50 = 1.5 µM). CP 100,356 (24 mg/kg), when administered in combination with prazosin (Item No. 15023), increases the rate of prazosin clearance in rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kalgutkar, A.S., Frederick, K.S., Chupka, J., 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. 98(12), 4914-4927 (2009).