PF-4981517

製品コードS2921 バッチS292150

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
* <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) is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.
in vitro	PF-4981517 (CYP3cide) is a potent, efficient, and specific time-dependent inactivator of human CYP3A4. PF-4981517 is tested as a reversible inhibitor of several human cytochrome P450 activities in pooled HLMs. PF-4981517 is selective for CYP3A4 with IC50 of 0.03 μM, 17 μM and 70 μM for CYP3A4, 3A5, and 3A7, respectively. PF-4981517 is a mechanism-based inactivator. PF-4981517 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). PF-4981517 is useful to investigators seeking to delineate the relative contribution of CYP3A4 versus CYP3A5 in the metabolism of compounds cleared by CYP3A. ^[1]

製品説明

PF-4981517 (CYP3cide, PF-04981517) is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.

in vitro

PF-4981517 (CYP3cide) is a potent, efficient, and specific time-dependent inactivator of human CYP3A4. PF-4981517 is tested as a reversible inhibitor of several human cytochrome P450 activities in pooled HLMs. PF-4981517 is selective for CYP3A4 with IC50 of 0.03 μM, 17 μM and 70 μM for CYP3A4, 3A5, and 3A7, respectively. PF-4981517 is a mechanism-based inactivator. PF-4981517 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). PF-4981517 is useful to investigators seeking to delineate the relative contribution of CYP3A4 versus CYP3A5 in the metabolism of compounds cleared by CYP3A. ^[1]

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 CYP3cide at concentrations of 0, 0.32, 1, 3.2, 10, 32, and 100 μM. Stock solutions of CYP3cide are prepared in 50:50 acetonitrile/water. Kinetic constants are estimated using the SigmaPlot version 12 curve-fitting software.

参考

[1] Walsky RL, et al. Drug Metab Dispos, 2012, 40(9), 1686-1697.

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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