Home Metabolism Lipase inhibitor ABX-1431 For research use only.

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.

ABX-1431 Chemical Structure

ABX-1431 Chemical Structure

CAS: 1446817-84-0

Purity & Quality Control

Batch: S882301 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] false] Water] Insoluble] false Purity: 99.99%
99.99

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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
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].
Cell Research Cell lines PC3 cells
Concentrations 0.1-10 μM
Incubation Time 30 min
Method

Human prostate cancer PC3 cells 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.
In Vivo
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].
Animal Research Animal Models male Sprague-Dawley rats
Dosages 1 mg/kg
Administration IV
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03447756 Completed Post Herpetic Neuralgia|Diabetic Peripheral Neuropathy|Small Fiber Neuropathy|Post-Traumatic Neuralgia Abide Therapeutics October 2 2017 Phase 1
NCT03138421 Completed Neuromyelitis Optica Spectrum Disorder|Transverse Myelitis|Multiple Sclerosis|Longitudinally Extensive Transverse Myelitis Abide Therapeutics August 1 2017 Phase 1
NCT03058562 Completed Tourette Syndrome|Chronic Motor Tic Disorder Abide Therapeutics February 1 2017 Phase 1
NCT02929264 Completed Pain Abide Therapeutics|University of Oxford December 2016 Phase 1

Chemical lnformation & Solubility

Molecular Weight 507.39 Formula

C20H22F9N3O2
CAS No. 1446817-84-0 SDF --
Smiles C1CCN(C1)C2=C(C=CC(=C2)C(F)(F)F)CN3CCN(CC3)C(=O)OC(C(F)(F)F)C(F)(F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (197.08 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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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

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