| 货号 | 10108-1mg |
| 描述 | Leukotriene A4(LTA4) hydrolase/aminopeptidase is a bifunctional zinc metalloenzyme that both catalyzes the synthesis of LTB4 (Item No. 20110) from LTA4 and cleaves the chemotactic peptide Pro-Gly-Pro.1,2 SC-57461A is a potent, orally active inhibitor of LTA4 hydrolase that blocks ionophore-stimulated LTB4 synthesis in whole blood (IC50 = 49 nM).3,4 It blocks both the hydrolase and aminopeptidase activity in vitro.4 SC-57461A is without effect against other enzymes of the arachidonic acid cascade, including 5-lipoxygenase, LTC4 synthase, COX-1, and COX-2. In a rat model of ionophore-induced peritoneal eicosanoid production, SC-57461A inhibits LTB4 biosynthesis without affecting LTC4 (Item No. 20210) or 6-keto prostaglandin F1α production (Item No. 15210).5 Oral or topical pretreatment with SC-57461A before challenge with arachidonic acid blocks ear edema in mice.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Haeggström, J.Z. Leukotriene A4 hydrolase/aminopeptidase, the gatekeeper of chemotactic leukotriene B4 biosynthesis. The Journal of Biological Chemisty 279(49), 50639-50642 (2004). 2.Snelgrove, R.J.,Jackson, P.L.,Hardison, M.T., et al. A critical role for LTA4H in limiting chronic pulmonary neutrophilic inflammation. Science 330, 90-94 (2010). 3.Penning, T.D.,Russel, M.A.,Chen, B.B., et al. Synthesis of potent leukotriene A(4) hydrolase inhibitors. Identification of 3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic acid. Journal of Medicinal Chemistry 45(16), 3482-3490 (2016). 4.Askonas, L.J.,Kachur, J.F.,Villani-Price, D., et al. Pharmacological characterization of SC-57461A (3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic acid HCl), a potent and selective inhibitor of leukotriene A4 hydrolase I: In vivo studies. Journal of Pharmacology and Experimental Therapeutics 300(2), 577-582 (2002). 5.Kachur, J.F.,Askonas, L.J.,Villani-Price, D., et al. Pharmacological characterization of SC-57461A (3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic acid HCl), a potent and selective inhibitor of leukotriene A4 hydrolase II: In vivo studies. Journal of Pharmacology and Experimental Therapeutics 300(2), 583-587 (2002). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 363.9 |
| 分子式 | C20H25NO3 • HCl |
| CAS号 | 423169-68-0 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |