aladdin 阿拉丁 A414203 ABX-1431 1446817-84-0 98%

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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