货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T96122-1ml促销	10mM in DMSO	￥720.00 ￥648.00 T96122-1ml ￥648.00 现货	5 5	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T96122-1ml促销

10mM in DMSO

￥720.00 ￥648.00

产品描述：

脂肪氧化酶抑制剂;Lipoxygenase Inhibitors;;InformationML355 ML355 is a potent and selective inhibitor of human 12-Lipoxygenase with an IC50 of 290 nM and shows excellent selectivity over related lipoxygenases and cyclooxygenases.Targets12-LOXIn vitroML355 displays nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases.In vivoIn vivo PK studies where ML355 is administered as a solution via IV (3mpk) and PO (30mpk) demonstrated that ML355 is orally bioavailable (%F = 20) with good half-life (T1/2 = 2.9 hours). At 30 mpk dosing, ML355 achieves a Cmax of over 135 times the in vitro IC50 and remains over IC50 value for over 12 hours. The compound has low clearance (3.4 mL/min/kg) and good overall exposure (AUCinf) of 38 µM. Although, the volume of distribution (VD) observed is low (0.55 L/kg), the rest of the PK profiling results suggest a reasonable distribution between tissue and blood.

体内研究：

ML355（1.88-30 mg/kg；i.g.；每天 2 次，连续两天）与 WT 对照相比在较高剂量下强烈抑制了小鼠的血栓形成。

参考文献：

1. Luci DK, et al. Synthesis and structure-activity relationship studies of 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase. J Med Chem. 2014 Jan 23;57(2):495-506.
2. Zhang XJ, et al. An ALOX12-12-HETE-GPR31 signaling axis is a key mediator of hepatic ischemia-reperfusion injury. Nat Med. 2018 Jan;24(1):73-83.
3. Adili R, et al. First Selective 12-LOX Inhibitor, ML355, Impairs Thrombus Formation and Vessel Occlusion In Vivo With Minimal Effects on Hemostasis. Arterioscler Thromb Vasc Biol. 2017 Oct;37(10):1828-1839.

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.265 ml	11.325 ml	22.649 ml
5 mM	0.453 ml	2.265 ml	4.53 ml
10 mM	0.226 ml	1.132 ml	2.265 ml
50 mM	0.045 ml	0.226 ml	0.453 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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