|Related Categories||Approved Therapeutics/Drug Candidates, Cell Biology, Cell Signaling and Neuroscience, Drug Efflux Pumps, Modulators for MDR/TAP Transporters,|
|color||white to off-white|
|solubility||DMSO: >5 mg/mL|
Sold for research purposes under agreement from Pfizer Inc.
CP-100356 is a specific inhibitor of MDR1 (P-Gp), the protypical ABC transporter. The compound has low uM to nM potency for inhibiting several MDR-1 substrates (calcein-AM, digoxin) in transfected MDCKII cells. CP-100356 also inhibits prazosin transport in human breast cancer resistance protein (BCRP)-transfected MDCKII cells, suggesting that it acts as a dual inhibitor. CP-100356 does not inhibit multidrug resistance-associated protein 2 (MPR2 IC50 >15 mM).
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. Kalgutkar, A.S., et al. J. Pharm. Sci. 98, 4914-4927, (2009)
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