CP 100356 hydrochloride
Tocris Bioscience, part of Bio-Techne | Catalog # 4193
P-gp inhibitor
Product Description
CP 100356 hydrochloride is a high 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 Information
Sold for research purposes under agreement from Pfizer Inc.Product Specifications
Molecular Weight
597.10
Formula
C31H36N4O6.HCl
Storage
Desiccate at RT
Purity
≥98% (HPLC)
Chemical Name
4-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-N-2[2-(3,4-dimethoxyphenyl)ethyl]-6,7-dimethoxy-2-quinazolinamine hydrochloride
CAS Number
142715-48-8
PubChem ID
71312025
InChI Key
WWCHXVYTCMPAMV-UHFFFAOYSA-N
SMILES
COC2=CC1=C(N3CCC(C=C(OC)C(OC)=C5)=C5C3)N=C(NCCC4=CC=C(OC)C(OC)=C4)N=C1C=C2OC.Cl
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 11.94 | 20 |
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
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 Specific Notices for CP 100356 hydrochloride
For research use only
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