货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T88375-1ml	10mM in DMSO	￥500.00 T88375-1ml ￥500.00 现货	6 6	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T88375-1ml

10mM in DMSO

￥500.00

产品描述：

脂肪酶抑制剂;Lipase Inhibitors;;InformationABX-1431 ABX-1431 is a highly potent, selective, and CNS-penetrant Monoacylglycerol lipase (MGLL) inhibitor with IC50 values of 14 nM and 27 nM for hMGLL and mMGLL respectively.TargetshMGLL ; mMGLL 14 nM; 27 nMIn vitroABX-1431 is a potent human MGLL inhibitor (average IC50 = 0.014 μM) with >100-fold selectivity against ABHD6 and >200-fold selectivity against PLA2G7. Treatment of intact human PC3 cells with ABX-1431 following a 30 min inhibitor incubation time causes concentration dependent inhibition of MGLL activity with an IC50 value of 0.0022 μM, which is ∼6-fold more potent than that observed in vitro. ABX-1431 inhibits MGLL via carbamoylation of the catalytic nucleophile Ser122.In vivoPharmacokinetic analysis in rats and dogs of ABX-1431 indicate low to moderate systemic clearance, moderate volume of distribution, and high oral bioavailability (64% in rat, 57% in dog). While ABX-1431 is stable in human and dog plasma, it is not stable in rat plasma. ABX-1431 is a potent and selective inhibitor of MGLL in mouse and rat brain in vivo. ABX-1431 inhibits MGLL activity with an ED50 of 0.5-1.4 mg/kg (po) and dose-dependently increases brain 2-AG levels in mouse brain. A rat inflammatory pain model is used to assess the pharmacodynamics effect. ABX-1431 demonstrates potent antinociceptive effects in a formalin paw test at a dose that produced near complete MGLL inhibition and maximal elevation of 2-AG.Cell Research(from reference)Cell lines：PC3 cells Concentrations：0.1-10 μM Incubation Time：30 min

靶点：

IC50: 14 nM (human MGLL)

体内研究：

Elcubragistat (ABX-1431) 可抑制啮齿动物脑中的 MGLL 活性（ED50=0.5-1.4 mg/kg），增加脑中 2-AG 浓度，并抑制大鼠福尔马林疼痛模型中的疼痛行为。

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	1.971 ml	9.854 ml	19.709 ml
5 mM	0.394 ml	1.971 ml	3.942 ml
10 mM	0.197 ml	0.985 ml	1.971 ml
50 mM	0.039 ml	0.197 ml	0.394 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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