1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. CYP3cide

CYP3cide (Synonyms: PF-4981517)

Cat. No.: HY-18642
Handling Instructions

CYP3cide (PF-4981517) is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC50 values for Midazolam 1’-hydroxylase activity are 0.03 μM, 17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. CYP3cide can be used to distinguish the contributions of CYP3A4 versus CYP3A5 on drug metabolism.

For research use only. We do not sell to patients.

CYP3cide Chemical Structure

CYP3cide Chemical Structure

CAS No. : 1390637-82-7

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Description

CYP3cide (PF-4981517) is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC50 values for Midazolam 1’-hydroxylase activity are 0.03 μM, 17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. CYP3cide can be used to distinguish the contributions of CYP3A4 versus CYP3A5 on drug metabolism[1].

IC50 & Target[1]

CYP3A4

30 nM (EC50)

CYP3A5

17 μM (EC50)

CYP3A7

71 μM (EC50)

In Vitro

When investigating the inhibitory properties of CYP3cide, an extreme metabolic inactivation efficiency (kinact/KI) of 3300 to 3800 ml • min-1 • μmol-1 is observed using human liver microsomes from donors of nonfunctioning CYP3A5 (CYP3A5 *3/*3). This observed efficiency equated to an apparent KI between 420 and 480 nM with a maximal inactivation rate (kinact) equal to 1.6 min-1. When CYP3cide is tested at a concentration and preincubation time to completely inhibit CYP3A4 in a library of genotyped polymorphic CYP3A5 microsomes, the correlation of the remaining midazolam 1'-hydroxylase activity to CYP3A5 abundance is significant[1].

Molecular Weight

456.59

Formula

C₂₆H₃₂N₈

CAS No.

1390637-82-7

SMILES

CC1=CC=C(C2=C(C3=NN(C)C4=NC=NC(N5C[[email protected]@H](N6CCCCC6)CC5)=C43)C=NN2C)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

CYP3cidePF-4981517PF4981517PF 4981517Cytochrome P450CYPsCYP3A4Midazolam1’-hydroxylasemetabolismCYP3A5Inhibitorinhibitorinhibit

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CYP3cide
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HY-18642
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