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ABX-1431

Catalog No. T5353 CAS 1446817-84-0

Synonyms: Elcubragistat

ABX-1431 (Elcubragistat) is a selective and orally available CNS-penetrant monoacylglycerol lipase (MAGL/MGLL) inhibitor (IC50: 14 nM).

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ABX-1431, CAS 1446817-84-0

Pack Size	Availability	Price/USD
2 mg	In stock	$ 30.00
5 mg	In stock	$ 45.00
10 mg	In stock	$ 64.00
25 mg	In stock	$ 126.00
50 mg	In stock	$ 207.00
100 mg	In stock	$ 369.00
1 mL * 10 mM (in DMSO)	In stock	$ 45.00

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Purity: 99.8%

Purity: 99.27%

Biological Description

Chemical Properties

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Description	ABX-1431 (Elcubragistat) is a selective and orally available CNS-penetrant monoacylglycerol lipase (MAGL/MGLL) inhibitor (IC50: 14 nM).
Targets&IC50	MGLL (mouse):27 nM, MGLL (human):14 nM
In vitro	ABX-1431 was 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-minute inhibitor incubation time caused 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. In the cell-based assay, >100-fold selectivity for MGLL over ABHD6 (IC50 = 0.253 μM) and PLA2G7 (IC50 = 494 μM) was maintained.
In vivo	In vivo, ABX-1431 inhibits MGLL activity in rodent brain (ED50 = 0.5-1.4 mg/kg), increases brain 2-AG concentrations, and suppresses pain behavior in the rat formalin pain model.
Cell Research	Human prostate cancer PC3 cells were 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 was added to cells to give final concentration of 0.1–10 μM compound in serum free media. Cells were incubated with compound for 30 min at 37°C with 5% CO2. Cells were washed, harvested, and lysed by probe sonication. Cell lysates (2mg/mL) were treated with JW912 (1μM) and analyzed by SDS-PAGE and in-gel fluorescence scanning.
Animal Research	All animals were 6?8 weeks old at the time of study and weighed between 197-217 g. Animals (n = 3 per dosing route) were dosed with ABX-1431 at 1 mg/kg iv (in 70% polyethylene glycol (PEG) 400 in hydroxypropyl-?-cylcodextran (HPBCD) in saline) or 5 mg/kg po (in 70% PEG 400 in 0.5% carboxymethylcellulose (CMC, w/v) in saline). Animals were fasted overnight, and food withheld until 4 h post dose. Approximately 100 μL of blood were collected via a jugular vein catheter at 0.033, 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, and 24 h after intravenous and 0.25, 0.5, 1, 2, 4, 6, 8, and 24 h after oral administration. All blood samples were collected into tubes containing 400 μL acetonitrile to immediately inactivate blood esterase activity and frozen at ?80 °C. Samples were thawed and centrifuged (14,000 rpm for 5 min at 4 °C) and the supernatant transferred for LCMS analysis.

Synonyms	Elcubragistat
Molecular Weight	507.39
Formula	C20H22F9N3O2
CAS No.	1446817-84-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 10 mg/mL (19.71 mM)

DMSO: 100 mg/mL (197.08 mM)

H2O: Insoluble

References and Literature

1. Cisar JS, et al. Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders. J Med Chem. 2018 Oct 25;61(20):9062-9084.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Drug Repurposing Compound Library Inhibitor Library Anti-Obesity Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Target-Focused Phenotypic Screening Library Anti-Metabolism Disease Compound Library Metabolism Compound Library ReFRAME Related Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

ABX-1431 1446817-84-0 Metabolism Lipase ABX1431 inhibit Monoacylglycerol lipase MAGL Elcubragistat ABX 1431 Inhibitor inhibitor

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