Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.9709 mL	9.8544 mL	19.7087 mL
5 mM	0.3942 mL	1.9709 mL	3.9417 mL
10 mM	0.1971 mL	0.9854 mL	1.9709 mL
50 mM	0.0394 mL	0.1971 mL	0.3942 mL

Description

ABX-1431 is a highly potent, selective, and CNS-penetrant inhibitor with IC50 values of 14 nM and 27 nM for hMGLL and mMGLL respectively.

Targets

hMGLL ^[1]	mMGLL ^[1]
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.

References

[1] Cisar JS, et al. J Med Chem. 2018, 61(20):9062-9084.
[2] Ming Jiang, et al. J Med Chem. 2018, 61(20): 9059–9061.

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[CAS NO. 1446817-84-0]??ABX-1431

PRODUCTS SPECIFICATIONS [1446817-84-0]

DESCRIPTION [1446817-84-0]

Overview

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Description

Targets

In vitro

References