货号 | 15040-100mg |
描述 | SKF 525A is a widely used, nonspecific cytochrome P (CYP)450 inhibitor that demonstrates 100% inhibition of the various CYP450 isoforms at 1-100 μM.1 It therefore potentiates the effects of many different drugs by inhibiting their metabolism (IC50 values in the μM range when tested using human liver microsomes).2 SKF 525A inhibits CYP450-dependent arachidonic acid conversion to active EET metabolites, antagonizing the recovery of functional calcium pools.3 It also acts as a noncompetitive inhibitor of acetylcholine nicotinic receptors (IC50 = 19 μM in mouse skeletal muscle).4,5 |
别名 | RP 5171;U 5446; |
供应商 | Cayman |
应用文献 | |
1.Franklin, M.R. and Hathaway, L.B. 2-Diethylaminoethyl-2,2-diphenylvalerate-HCl (SKF525A) revisited: Comparative cytochrome P450 inhibition in human liver microsomes by SKF525A, its metabolites, and SKF-acid and SKF-alcohol. Drug Metabolism and Disposition 36(12), 2539-2546 (2008). 2.Emoto, C.,Murase, S.,Sawada, Y., et al. In vitro inhibitory effect of 1-aminobenzotriazole on drug oxidations in human liver microsomes: A comparison with SKF-525A. Drug Metab.Pharmacokinet. 20(5), 351-357 (2005). 3.Graber, M.N.,Alfonso, A. and Gill, D.L. Recovery of Ca2+ pools and growth in Ca2+ pool-depleted cells is mediated by specific epoxyeicosatrienoic acids derived from arachidonic acid. The Journal of Biological Chemisty 272, 29546-29553 (1997). 4.Kagota, S.,Yamaguchi, Y.,Nakamura, K., et al. Characterization of nitric oxide- and prostaglandin-independent relaxation in response to acetylcholine in rabbit renal artery. Clinical and Experimental Pharmacology and Physiology 26, 790-796 (1999). 5.Spitzmaul, G.,Gumilar, F.,Dilger, J.P., et al. The local anaesthetics proadifen and adiphenine inhibit nicotinic receptors by different molecular mechanisms. British Journal of Pharmacology 157(5), 804-817 (2009). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 390 |
分子式 | C23H31NO2 • HCl |
CAS号 | 62-68-0 |
稳定性 | ≥ 2 years |
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