CP 100356 hydrochloride
Cat. No. 4193
Chemical Name: 4-(3,4-Dihydro-6,7-dimethoxy-2(1H)-
Biological ActivityHigh affinity P-glycoprotein (P-gp) inhibitor (Ki values are 58 and 94 nM for mouse Pgp1a and Pgp1b isoforms). Inhibits calcein-AM uptake in MDR1-transfected MDCKII cells (IC50 = 0.5 μM) and prazosin transport in BCRP-transfected MDCKII cells (IC50 = 1.5 μM). Displays weak or no inhibitory activity against MRP1, OATP1B1 and several major human P450 enzymes (IC50 > 50 μM).
Licensing InformationSold for research purposes under agreement from Pfizer Inc.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Kalgutkar et al (2009) 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 4914. PMID: 19373887.
Taylor et al (1999) The equilibrium and kinetic drug binding properties of the mouse P-gp1a and P-gp1b P-glycoproteins are similar. Br.J.Cancer 81 783. PMID: 10555746.
Wandel et al (1999) P-glycoprotein and cytochrome P-450 3A inhibition: dissociation of inhibitory potencies. Cancer Res. 59 3944. PMID: 10463589.
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Citations are publications that use Tocris products. Selected citations for CP 100356 hydrochloride include:
Sheehy et al (2015) Calcium and P-glycoprotein independent synergism between schweinfurthins and verapamil. Acta Neuropathol Commun 16 1259. PMID: 26046259.
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