| Size | Price | Stock | Qty |
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| Targets |
ARN726 targets N-acylethanolamine acid amidase (NAAA), a lysosomal cysteine hydrolase that hydrolyzes palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). It is a potent NAAA inhibitor with IC50 values of 27 nM for human NAAA and 63 nM for rat NAAA. The compound is selective for NAAA over fatty acid amide hydrolase (FAAH) and acid ceramidase, with IC50 values of >100 µM and 12.5 µM, respectively. By inhibiting NAAA, ARN726 increases the levels of PEA and OEA, which are endogenous lipid mediators with anti-inflammatory properties.
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| ln Vitro |
In vitro, ARN726 is a potent inhibitor of NAAA with IC50 values of 27 nM for human NAAA and 63 nM for rat NAAA. It displays anti-inflammatory effects in human macrophages ex vivo. The compound is selective for NAAA over FAAH (IC50 > 100 µM) and acid ceramidase (IC50 = 12.5 µM). ARN726 is also used as an activity-based protein profiling (ABPP) probe to detect NAAA in cell lysates or intact cells, enabling the study of NAAA expression and activity in various biological samples.
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| ln Vivo |
In vivo, ARN726 has shown anti-inflammatory effects in mouse models of lung inflammation and arthritis. It reduces alcohol self-administration in a dose-dependent fashion. The compound has been studied in the complete Freund's adjuvant rat model of arthritis, demonstrating an important role for NAAA in inflammatory pain. These in vivo studies confirm that ARN726 is a potent and systemically active NAAA inhibitor with therapeutic potential in inflammatory diseases.
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| Enzyme Assay |
In vitro enzyme assays for ARN726 measure its inhibition of NAAA activity. NAAA enzyme is incubated with a fluorogenic substrate (e.g., a PEA analog) in the presence of varying concentrations of ARN726. The release of the fluorescent product is measured, and the IC50 is determined from the dose-response curve. For ARN726, the IC50 values are 27 nM for human NAAA and 63 nM for rat NAAA. Selectivity is assessed by testing the compound against FAAH and acid ceramidase. Activity-based protein profiling (ABPP) assays using ARN726 as a probe can detect NAAA in cell lysates or intact cells.
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| Cell Assay |
In vitro cell-based assays for ARN726 are used to study its effects on NAAA inhibition and inflammatory responses. Human macrophages or other immune cells are treated with ARN726 at various concentrations, and the levels of PEA and OEA are measured by LC-MS/MS to confirm target engagement. The anti-inflammatory effects are assessed by measuring the production of pro-inflammatory cytokines (e.g., TNF-α, IL-6) following stimulation with lipopolysaccharide (LPS) or other inflammatory stimuli. ARN726 has been shown to display anti-inflammatory effects in human macrophages ex vivo.
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| Animal Protocol |
In vivo animal experiments for ARN726 have been conducted in mouse models of lung inflammation and arthritis. In a typical study, ARN726 is administered to mice by oral gavage or intraperitoneal injection. Inflammatory parameters such as cytokine levels, immune cell infiltration, and tissue damage are assessed. The compound has also been studied in the complete Freund's adjuvant rat model of arthritis. In alcohol self-administration studies, ARN726 reduces alcohol intake in a dose-dependent manner. These studies confirm the in vivo efficacy of ARN726 in inflammatory and behavioral models.
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| ADME/Pharmacokinetics |
ARN726 has a molecular weight of 268.36 g/mol and a molecular formula of C14H24N2O3. It has a logP of 1.88. The compound is a white to off-white solid powder. It is soluble in DMSO. For storage, it is recommended to keep the powder at -20°C for up to 3 years or at 4°C for up to 2 years. In solvent, it can be stored at -80°C for 6 months or at -20°C for 1 month. The compound is stable at ambient temperature for a few days during shipping. Detailed pharmacokinetic properties such as half-life and bioavailability have been characterized in preclinical studies, but specific values are not detailed in standard product descriptions.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for ARN726 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. In vivo studies have used ARN726 at doses that are effective in inflammatory models without reported overt toxicity. However, comprehensive toxicological studies, including acute and chronic toxicity studies, have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling ARN726. Its use is limited to research applications and it is not intended for human or veterinary use.
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| Additional Infomation |
ARN726 is a research compound and is not approved for any clinical or therapeutic use. It is a potent N-acylethanolamine acid amidase (NAAA) inhibitor with IC50 values of 27 nM for human NAAA and 63 nM for rat NAAA. ARN726 displays anti-inflammatory effects in human macrophages and mouse models of lung inflammation and arthritis. It is also used as an activity-based protein profiling (ABPP) probe to detect NAAA in cell lysates or intact cells. The compound reduces alcohol self-administration in a dose-dependent fashion. ARN726 is a valuable research tool for studying the role of NAAA in inflammation, pain, and addiction.
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| Molecular Formula |
C14H24N2O3
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|---|---|
| Molecular Weight |
268.36
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| Exact Mass |
268.178
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| CAS # |
1628343-77-0
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| PubChem CID |
78319072
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
478.8±34.0 °C at 760 mmHg
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| Flash Point |
243.4±25.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.515
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| LogP |
1.88
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
19
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| Complexity |
314
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O(C(N([H])[C@]1([H])C(N([H])C1([H])[H])=O)=O)C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H]
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| InChi Key |
FNLUJRBWJBUJTC-LBPRGKRZSA-N
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| InChi Code |
InChI=1S/C14H24N2O3/c17-13-12(10-15-13)16-14(18)19-9-5-4-8-11-6-2-1-3-7-11/h11-12H,1-10H2,(H,15,17)(H,16,18)/t12-/m0/s1
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| Chemical Name |
4-cyclohexylbutyl N-[(3S)-2-oxoazetidin-3-yl]carbamate
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| Synonyms |
ARN0726 ARN 0726 ARN-0726
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7263 mL | 18.6317 mL | 37.2634 mL | |
| 5 mM | 0.7453 mL | 3.7263 mL | 7.4527 mL | |
| 10 mM | 0.3726 mL | 1.8632 mL | 3.7263 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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