PF-4981517

製品コードS2921 バッチS292150

印刷

化学情報

Synonyms

CYP3cide, PF-04981517

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₆H₃₂N₈

分子量

456.59

CAS No.

1390637-82-7

Solubility (25°C)*

体外

DMSO

91 mg/mL (199.3 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.55mg/ml (9.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 91 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.65mg/ml (1.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	PF-4981517（CYP3cide、PF-04981517）は、CYP3A4（P450）の強力かつ選択的阻害剤であり、IC50は0.03 μMで、CYP3A5およびCYP3A7に対して500倍以上の選択性を示します。
in vitro	PF-4981517 (CYP3cide) is a potent, efficient, and specific time-dependent inactivator of human CYP3A4. This compound is tested as a reversible inhibitor of several human cytochrome P450 activities in pooled HLMs. It is selective for CYP3A4 with IC50 of 0.03 μM, 17 μM and 70 μM for CYP3A4, 3A5, and 3A7, respectively. This chemical is a mechanism-based inactivator. It serves as an important in vitro tool, which when used side-by-side with ketoconazole to inhibit all CYP3A activity will permit distinction between the contribution of CYP3A4 to CYP3A5 (as well as CYP3A7 and maybe CYP3A43). This compound is useful to investigators seeking to delineate the relative contribution of CYP3A4 versus CYP3A5 in the metabolism of compounds cleared by CYP3A.

製品説明

PF-4981517（CYP3cide、PF-04981517）は、CYP3A4（P450）の強力かつ選択的阻害剤であり、IC50は0.03 μMで、CYP3A5およびCYP3A7に対して500倍以上の選択性を示します。

in vitro

PF-4981517 (CYP3cide) is a potent, efficient, and specific time-dependent inactivator of human CYP3A4. This compound is tested as a reversible inhibitor of several human cytochrome P450 activities in pooled HLMs. It is selective for CYP3A4 with IC50 of 0.03 μM, 17 μM and 70 μM for CYP3A4, 3A5, and 3A7, respectively. This chemical is a mechanism-based inactivator. It serves as an important in vitro tool, which when used side-by-side with ketoconazole to inhibit all CYP3A activity will permit distinction between the contribution of CYP3A4 to CYP3A5 (as well as CYP3A7 and maybe CYP3A43). This compound is useful to investigators seeking to delineate the relative contribution of CYP3A4 versus CYP3A5 in the metabolism of compounds cleared by CYP3A.

プロトコル(参考用のみ)

キナーゼアッセイ	Reversible Inhibition and Selectivity of PF-4981517
キナーゼアッセイ	The enzyme source of reactions is either pooled HLM, rCYP3A4, rCYP3A5, or rCYP3A7 with POR and cytochrome b5. For the recombinant enzymes, the P450/oxdioreductase/b5 ratio is calculated to be 1:5:7, 1:13:7, and 1:3:2, respectively. The P450 and POR concentrations are experimentally derived by the vendor and noted from the product specifications sheet. The cytochrome b5 concentration is calculated using an assumed specific activity of 3200 nmol of reduced cytochrome c min⁻¹ per nmol of reductase and applying it to the reduced cytochrome c rate. The ratio of all three enzymes is stated using the reported P450 concentration as the denominator. P450 isoform-specific substrates testing is conducted at an experimentally derived KM value to establish IC50 values; thus, the observed results are never more than 2-fold from the Ki. All IC50 determinations are repeated in duplicate. Incubation mixtures typically contained this compound at concentrations of 0, 0.32, 1, 3.2, 10, 32, and 100 μM. Stock solutions of this compound are prepared in 50:50 acetonitrile/water. Kinetic constants are estimated using the SigmaPlot version 12 curve-fitting software.

参考

https://pubmed.ncbi.nlm.nih.gov/22645092/

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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