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SC 57461A
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SC 57461A图片
CAS NO:423169-68-0
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
SC 57461A 是一种有效的、具有口服活性的、非肽类和选择性的白三烯 A4 (LTA4) 水解酶抑制剂,对重组人、小鼠和大鼠 LTA4 水解酶的 IC50 分别为 2.5 nM、3 nM 和 23 nM。
Cas No.423169-68-0
别名N-甲基-N-[3-[4-(苯甲基)苯氧基]丙基Β-丙氨酸盐酸盐
化学名3-[3-(4-benzylphenoxy)propyl-methylamino]propanoic acid;hydrochloride
Canonical SMILESCN(CCCOC1=CC=C(C=C1)CC2=CC=CC=C2)CCC(=O)O.Cl
分子式C20H25NO3.HCl
分子量363.88
溶解度≥ 36.4mg/mL in DMSO
储存条件Desiccate at 4℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].
References:
[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.