中文名：ABX-1431
英文名：ABX-1431
纯度：Moligand™，≥98%
货号：A414203
Cas号：1446817-84-0
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
ABX-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.
Targets
hMGLL ; mMGLL 14 nM; 27 nM
In vitro
ABX-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 vivo
Pharmacokinetic 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
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关键字： 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate ; BS-15747 ; BDBM180052 ; 1-Piperazinecarboxylic acid, 4-((2-(1-pyrrolidinyl)-4-(trifluoromethyl)phenyl)methyl)-2,2,2-trifluoro-1-(trifluoromethyl)
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