ABX-1431

Catalog No.S8823

ABX-1431 Chemical Structure

Molecular Weight(MW): 507.39

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.

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Choose Selective Lipase Inhibitors

Biological Activity

Description 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 [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[1].

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[1]. 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[2].

Protocol

Cell Research:

[1]

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  • Cell lines: PC3 cells
  • Concentrations: 0.1-10 μM
  • Incubation Time: 30 min
  • Method:

    Human prostate cancer PC3 cells (ATCC, CRL-1435) are grown in F-12K medium supplemented with 10% fetal bovine serum at 37 °C with 5% CO2 to ∼80% confluency in 100 mm dishes. ABX-1431 is added to cells to give final concentration of 0.1-10 μM compound in serum free media. Cells are incubated with compound for 30 min at 37°C with 5% CO2. Cells are washed, harvested, and lysed by probe sonication. Cell lysates (2 mg/mL) are treated with JW912 (1 μM) and analyzed by SDS-PAGE and in-gel fluorescence scanning.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: male Sprague-Dawley rats
  • Formulation: 70% polyethylene glycol (PEG) 400 in hydroxypropyl-β-cylcodextran (HPBCD) in saline (IV formulation); 70% PEG 400 in 0.5% carboxymethylcellulose (CMC, w/v) in saline (PO formulation)
  • Dosages: 1 mg/kg
  • Administration: IV
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (197.08 mM)
Ethanol 100 mg/mL (197.08 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 507.39
Formula

C20H22F9N3O2

CAS No. 1446817-84-0
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID