LTA4 hydrolase inhibitor,potent and selective
CAS：423169-68-0
分子式：C20H25NO3.HCl
分子量：363.88
纯度：98%
存储：Store at -20°C

Background:

SC-57461A is a selective inhibitor of human recombinant LTB4 with IC50 value of 49 nM [1].
LTB4 (leukotriene B (4)) is a leukotriene and plays an important role in inflammation. LTB4 functions through interacting with the specific cell-surface receptors BLTR1 and BLTR2 [2].
SC-57461A is a potent LTB4 inhibitor and has a more potent activity than the reported LTA4 inhibitor RP64966. When tested with PMN cells, administration of SC-57461A significantly inhibited the synthesis of LT that induced by fMLP and PAF by acting on LTB4-BLTR1 interaction [3].
In fasted CD rat model of calcium ionophore A23187-induced eicosanoid production, oral administration of SC-57461A showed effective inhibition on LTB4 with ED50 value of 0.3-1.0 mg/kg. When tested with AA-induced edema on the ear, oral administration of SC-57461A resulted in markedly inhibition of edema at doses of 0.8, 4 and 20 mg/kg [1].
It is also been reported that SC-57461A inhibited LTB4A with Ki values of 23 nM and 27 nM for epoxide hydrolase and aminopeptidase, respectively [1].
参考文献:
[1].    Kachur, J.F., 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 A(4) hydrolase II: in vivo studies. J Pharmacol Exp Ther, 2002. 300(2): p. 583-7.
[2].    Filgueiras, L.R., et al., Leukotriene B4-mediated sterile inflammation promotes susceptibility to sepsis in a mouse model of type 1 diabetes. Sci Signal, 2015. 8(361): p. ra10.
[3].    Grenier, S., et al., Arachidonic acid activates phospholipase D in human neutrophils; essential role of endogenous leukotriene B4 and inhibition by adenosine A2A receptor engagement. J Leukoc Biol, 2003. 73(4): p. 530-9.