货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
Y65375-1mg	98%	￥1650.00 Y65375-1mg ￥1650.00 2-4周	0 货期：2-4周	-	-	-	-
Y65375-200mg	98%	￥15800.00 Y65375-200mg ￥15800.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

Y65375-1mg

98%

￥1650.00

货期：2-4周

Y65375-200mg

98%

￥15800.00

货期：3-5天

靶点：

IC50: 4.2 nM (FLAP)

体内研究：

AM 103 has high bioavailability (64%), low clearance (2.9 mL/min/kg), low volume of distribution (0.41 L/kg), and a long i.v. half-life (5.2 h) in dogs. AM 103 (10 mg/kg q.i.d.) inhibits the increase in CysLTs and EPO by approximately 60%, and IL-5 levels are reduced to the concentrations obtained following saline treatment alone in mice. AM103 (1 mg/kg, p.o.) displays >50% inhibition for up to 6 h with a calculated EC50 of appr 60 nM, in a rat ex vivo whole-blood calcium ionophore-induced LTB4 assay. AM 103 inhibits LTB4 and cysteinyl leukotriene (CysLT) production with ED50 values of 0.8 and 1 mg/kg, respectively, when rat lung is challenged in vivo with calcium ionophore. In this model, the EC50 derived from plasma AM103 is appr 330 nM for inhibition of both LTB4 and CysLT. In a model of chronic lung inflammation using ovalbumin-primed and challenged BALB/c mice, AM103 reduces the concentrations of eosinophil peroxidase, CysLTs, and interleukin-5 in the bronchoalveolar lavage fluid. Finally, AM 103 increases survival time in mice exposed to a lethal intravenous injection of platelet-activating factor.

参考文献：

1. Hutchinson JH, et al. 5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103). J Med Chem. 2009 Oct 8;52(19):5803
2. Lorrain DS, et al. Pharmacological characterization of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103), a novel selective 5-lipoxygenase-activating protein inhibitor

溶解性：

DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.578 ml	7.889 ml	15.778 ml
5 mM	0.316 ml	1.578 ml	3.156 ml
10 mM	0.158 ml	0.789 ml	1.578 ml
50 mM	0.032 ml	0.158 ml	0.316 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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