Elcubragistat (Synonyms: ABX-1431)

Name: Elcubragistat
Brand: MedChemExpress
SKU: HY-117632
Rating: 4.5 (1 reviews)

Cat. No.: HY-117632 Purity: 99.96%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Elcubragistat (ABX-1431) is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC₅₀ of 14 nM.

For research use only. We do not sell to patients.

Elcubragistat Chemical Structure

CAS No. : 1446817-84-0

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 53	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 83	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 275	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE Elcubragistat

•Nat Commun. 2022 Feb 25;13(1):1058. [Abstract]

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Biological Activity
Protocol
Purity & Documentation
References
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Description

Elcubragistat (ABX-1431) is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC₅₀ of 14 nM.

IC₅₀ & Target

IC50: 14 nM (human MGLL)^[1]

In Vitro

Elcubragistat (ABX-1431) is a potent human MGLL inhibitor (IC₅₀=0.014 µM) with >100-fold selectivity against ABHD6 and >200-fold selectivity against PLA2G7. Elcubragistat inhibits human PC3 cells with an IC₅₀ of 0.0022 µM. In the cell-based assay, >100-fold selectivity for MGLL over ABHD6 (IC₅₀=0.253 µM) and PLA2G7 (IC₅₀=494 µM) is maintained^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Elcubragistat (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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

507.39

Formula

C₂₀H₂₂F₉N₃O₂

CAS No.

1446817-84-0

Appearance

Solid

Color

White to light yellow

SMILES

O=C(N1CCN(CC2=CC=C(C(F)(F)F)C=C2N3CCCC3)CC1)OC(C(F)(F)F)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (492.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.10 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.96%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (247 KB) HNMR (202 KB) LCMS (139 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

Cell Assay ^[1]	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 for 30 min. Cells are washed, harvested, and lysed by probe sonication. Cell lysates (2mg/mL) are treated with JW912 (1µM) and analyzed by SDS-PAGE and in-gel fluorescence scanning^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Rats^[1] Elcubragistat is administered in a volume of 5 mL/kg. Male ICR mice or male Sprague Dawley rats 6 to 12 weeks are administered single oral doses of Elcubragistat (0.5-32 mg/kg for mice and 0.03-10 mg/kg for rats). Four hours after Elcubragistat administration, animals are anesthetized. Following blood collection, animals are killed by decapitation and brains are removed, hemisected and frozen in liquid nitrogen for analysis^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9709 mL	9.8544 mL	19.7087 mL	49.2718 mL
	5 mM	0.3942 mL	1.9709 mL	3.9417 mL	9.8544 mL
	10 mM	0.1971 mL	0.9854 mL	1.9709 mL	4.9272 mL
	15 mM	0.1314 mL	0.6570 mL	1.3139 mL	3.2848 mL
	20 mM	0.0985 mL	0.4927 mL	0.9854 mL	2.4636 mL
	25 mM	0.0788 mL	0.3942 mL	0.7883 mL	1.9709 mL
	30 mM	0.0657 mL	0.3285 mL	0.6570 mL	1.6424 mL
	40 mM	0.0493 mL	0.2464 mL	0.4927 mL	1.2318 mL
	50 mM	0.0394 mL	0.1971 mL	0.3942 mL	0.9854 mL
	60 mM	0.0328 mL	0.1642 mL	0.3285 mL	0.8212 mL
	80 mM	0.0246 mL	0.1232 mL	0.2464 mL	0.6159 mL
	100 mM	0.0197 mL	0.0985 mL	0.1971 mL	0.4927 mL

Elcubragistat Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Elcubragistat1446817-84-0ABX-1431ABX1431ABX 1431MAGLMonoacylglycerol lipaseInhibitorinhibitorinhibit

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Elcubragistat (Synonyms: ABX-1431)

Customer Review

Elcubragistat Related Antibodies

1 Publications Citing Use of MCE Elcubragistat

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•Related Screening Libraries:

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Elcubragistat Related Antibodies

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Complete Stock Solution Preparation Table

Elcubragistat Related Classifications

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