SC 57461A
(Synonyms: N-甲基-N-[3-[4-(苯甲基)苯氧基]丙基Β-丙氨酸盐酸盐) 目录号 : GC18011A potent, orally active inhibitor of LTA4 hydrolase
Cas No.:423169-68-0
Sample solution is provided at 25 µL, 10mM.
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.
Cas No. | 423169-68-0 | SDF | |
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 SMILES | CN(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°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.7482 mL | 13.7408 mL | 27.4816 mL |
5 mM | 0.5496 mL | 2.7482 mL | 5.4963 mL |
10 mM | 0.2748 mL | 1.3741 mL | 2.7482 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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