CP 100356 hydrochloride

Key Product Details

Product Description

CP 100356 hydrochloride is a high affinity P-glycoprotein (P-gp) inhibitor (K_i 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 Information

Sold for research purposes under agreement from Pfizer Inc.

Product Specifications for CP 100356 hydrochloride

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for CP 100356 hydrochloride

The following data is based on the product molecular weight 597.10.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	8.37 mL	41.87 mL	83.74 mL
1 mM	1.67 mL	8.37 mL	16.75 mL
2 mM	0.84 mL	4.19 mL	8.37 mL
10 mM	0.17 mL	0.84 mL	1.67 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Wandel P-glycoprotein and cytochrome P-450 3A inhibition: dissociation of inhibitory potencies. Cancer Res. 1999 PMID: 10463589
• Kalgutkar 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 J.Pharm.Sci. 2009 PMID: 19373887
• Taylor The equilibrium and kinetic drug binding properties of the mouse P-gp1a and P-gp1b P-glycoproteins are similar. Br.J.Cancer 1999 PMID: 10555746

Product Documents for CP 100356 hydrochloride