PF 4981517

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Cat.No. 4252 - PF 4981517 | C26H32N8 | CAS No. 1390637-82-7
Description: Selective CYP3A4 inhibitor
Chemical Name: (1-Methyl-3-[1-methyl-5-(4-methylphenyl)-1H-pyrazol-4-yl]-4-[(3S)-3-piperidin-1-ylpyrrolidin-1-yl]-1H-pyrazolo[3,4-d]pyrimidine)
Purity: ≥98% (HPLC)

Biological Activity

Potent and selective inhibitor of CYP3A4 (IC50 values are 0.03, 17 and 70 μM for CYP3A4, CYP3A5 and CYP3A7 respectively).

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 456.59
Formula C26H32N8
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1390637-82-7
PubChem ID 71315139
Smiles CN1N=C(C5=C(C6=CC=C(C)C=C6)N(C)N=C5)C2=C1N=CN=C2N3C[C@@H](N4CCCCC4)CC3

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 45.66 100
ethanol 9.13 20

Preparing Stock Solutions

The following data is based on the product molecular weight 456.59. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.19 mL 10.95 mL 21.9 mL
5 mM 0.44 mL 2.19 mL 4.38 mL
10 mM 0.22 mL 1.1 mL 2.19 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets

Safety Datasheet


References are publications that support the products' biological activity.

Walsky et al (2012) Selective mechanism-based inactivation of cytochrome P4503A4 by cyp3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of cytochrome P4503A4 versus P4503A5 in the metabolism of drugs. Am.Soc.Pharmacol.Exp.Ther. Epub ahead of print PMID:

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Keywords: pfizer PF4981517 selective inhibitors inhibits cyp3a4 cytochrome p4503A4 cyp3cide Cytochrome P450

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