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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Purity: ≥98%
PF-4981517 (also named as PF 04981517; PF04981517, CYP-3cide, PF 4981517; PF4981517) is a specific and time-dependent inactivator of human CYP3A4 (P450) with IC50 of 0.03 μM, it exhibits >500-fold selectivity for inhibiting CYP3A4 over CYP3A5 and CYP3A7 and a time-dependent inactivation of human CYP3A4.
ln Vitro |
Using human liver microsomes from donors with nonfunctioning CYP3A5 (CYP3A5 *3/*3), an extraordinary metabolic inactivation efficiency (kinact/KI) of 3300 to 3800 ml • min-1 • μmol-1 is observed when examining the inhibitory characteristics of CYP3cide. This efficiency was found to correspond to an apparent KI of 420–480 nM and a maximal inactivation rate (kinact) of 1.6 min-1. The connection between CYP3A5 abundance and the remaining midazolam 1'-hydroxylase activity is strong when CYP3cide is assessed in a library of genotyped polymorphic CYP3A5 microsomes at a concentration and preincubation period that totally inhibits CYP3A4[1].
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ln Vivo |
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Animal Protocol |
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References |
[1]. Robert L Walsky, et al. Selective mechanism-based inactivation of CYP3A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of CYP3A4 versus CYP3A5 in the metabolism of drugs. Drug Metab Dispos. 2012 Sep;40(9):1686-97.
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Molecular Formula |
C26H32N8
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Molecular Weight |
456.59
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CAS # |
1390637-82-7
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Related CAS # |
1390637-82-7;
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CC1=CC=C(C=C1)C2=C(C=NN2C)C3=NN(C)C4=C3C(=NC=N4)N5CC[C@@H](C5)N6CCCCC6
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 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 | |
10 mM | 0.2190 mL | 1.0951 mL | 2.1901 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.