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

CYP3cide  (Synonyms: PF-4981517)

Cat. No.: HY-18642 Purity: 99.46%
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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 agent metabolism.

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CYP3cide Chemical Structure

CYP3cide Chemical Structure

CAS No. : 1390637-82-7

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Based on 1 publication(s) in Google Scholar

CYP3cide Related Antibodies

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP3A4 CYP17A1

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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 agent 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CYP3cide Related Antibodies
Molecular Weight

456.59

Formula

C26H32N8
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (109.51 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1901 mL 10.9507 mL 21.9015 mL
5 mM 0.4380 mL 2.1901 mL 4.3803 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Volume (start)

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C2

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V2

In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1901 mL 10.9507 mL 21.9015 mL 54.7537 mL
5 mM 0.4380 mL 2.1901 mL 4.3803 mL 10.9507 mL
10 mM 0.2190 mL 1.0951 mL 2.1901 mL 5.4754 mL
15 mM 0.1460 mL 0.7300 mL 1.4601 mL 3.6502 mL
20 mM 0.1095 mL 0.5475 mL 1.0951 mL 2.7377 mL
25 mM 0.0876 mL 0.4380 mL 0.8761 mL 2.1901 mL
30 mM 0.0730 mL 0.3650 mL 0.7300 mL 1.8251 mL
40 mM 0.0548 mL 0.2738 mL 0.5475 mL 1.3688 mL
50 mM 0.0438 mL 0.2190 mL 0.4380 mL 1.0951 mL
60 mM 0.0365 mL 0.1825 mL 0.3650 mL 0.9126 mL
80 mM 0.0274 mL 0.1369 mL 0.2738 mL 0.6844 mL
100 mM 0.0219 mL 0.1095 mL 0.2190 mL 0.5475 mL
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CYP3cide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CYP3cide1390637-82-7PF-4981517PF4981517PF 4981517Cytochrome P450CYPsCYP3A4Midazolam1’-hydroxylasemetabolismCYP3A5Inhibitorinhibitorinhibit

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