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 inhibiting MDR1-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).
Product information
CAS Number: 142715-48-8
Molecular Weight: 597.10
Formula: C31H37ClN4O6
Chemical Name: 4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)-N-[2-(3,4-dimethoxyphenyl)ethyl]-6,7-dimethoxyquinazolin-2-amine hydrochloride
Smiles: Cl.COC1C=C(CCNC2=NC(=C3C=C(OC)C(=CC3=N2)OC)N2CC3C=C(OC)C(=CC=3CC2)OC)C=CC=1OC
InChiKey: WWCHXVYTCMPAMV-UHFFFAOYSA-N
InChi: 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
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 44 mg/mL (73.69 mM; Need ultrasonic and warming).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
CP-100356 (0.1-15 µM; pretreated for 30 min) inhibits acetoxymethyl Calcein (Calcein-AM) uptake and and Digoxin transport in human MDR1-transfected MDCKII cells, with IC50s of 0.50 µM and 1.2 µM, respectively. CP-100356 decreases the BCRP-mediated transport of Prazosin in MDCKII cells, with an IC50 of 1.5 µM. CP-100356 (0.064-200 µM; 5 min) inhibits OATP1B1-mediated uptake of Estradiol 17β-D-Glucuronide, with an IC50 of ~66 µM. CP-100356 (0-50 µM; 10-30 min) is devoid of inhibition (IC50>50 µM) against the catalytic activity of the individual P450 enzymes including P4503A4 in the competitive inhibition study.
In Vivo:
CP-100356 (6-24 mg/kg; p.o.) increases the systemic exposure of Fexofenadine (36- and 80-fold increase in Cmax and AUC at the dose of 24 mg/kg) in rats.
Products are for research use only. Not for human use.
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