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PF-4981517

Name: PF-4981517
Brand: TargetMol
SKU: T21548
Price: 42 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. T21548Cas No. 1390637-82-7

Alias CYP3cide

PF-4981517 (CYP3cide) is a efficient, specific and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC 50 values for CYP3A activity are 0.03 μM,17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. PF-4981517 is able to be used to distinguish the contributions of CYP3A4 versus CYP3A5 on drug Metabolism.

PF-4981517

🥰Excellent

Purity: 99.83%

Catalog No. T21548Alias CYP3cideCas No. 1390637-82-7

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$42	In Stock	In Stock
5 mg	$98	In Stock	In Stock
10 mg	$156	In Stock	In Stock
25 mg	$313	In Stock	In Stock
50 mg	$503	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$98	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Purity:99.83%

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	PF-4981517 (CYP3cide) is a efficient, specific and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC 50 values for CYP3A activity are 0.03 μM,17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. PF-4981517 is able to be used to distinguish the contributions of CYP3A4 versus CYP3A5 on drug Metabolism.
Targets&IC50	CYP3A7:71 μM (EC50), CYP3A5:17 μM (EC50), CYP3A4:30 nM (EC50)
In vitro	When investigating the inhibition of PF-4981517, an extreme metabolic inactivation efficiency (k inact /K I ) of 3300 to 3800 ml min -1 μmol -1 is observed in 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 PF-4981517 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 CYP3A activity to CYP3A5 abundance is significant.
Synonyms	CYP3cide

Chemical Properties

Molecular Weight	456.59
Formula	C₂₆H₃₂N₈
Cas No.	1390637-82-7
Smiles	Cc1ccc(cc1)-c1c(cnn1C)-c1nn(C)c2ncnc(N3CC[C@@H](C3)N3CCCCC3)c12
Relative Density.	1.34 g/cm3 (Predicted)
Color	Yellow
Appearance	Solid

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 40 mg/mL (87.61 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 4 mg/mL (8.76 mM), Sonication is recommeded.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1901 mL	10.9507 mL	21.9015 mL	109.5074 mL
5 mM	0.4380 mL	2.1901 mL	4.3803 mL	21.9015 mL
10 mM	0.2190 mL	1.0951 mL	2.1901 mL	10.9507 mL
20 mM	0.1095 mL	0.5475 mL	1.0951 mL	5.4754 mL
50 mM	0.0438 mL	0.2190 mL	0.4380 mL	2.1901 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc