| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
ARN19702 targets N-acylethanolamine acid amidase (NAAA), a lysosomal enzyme that hydrolyzes palmitoylethanolamide (PEA), an endogenous lipid mediator with anti-inflammatory and analgesic properties. By inhibiting NAAA, ARN19702 increases PEA levels, thereby enhancing its beneficial effects on pain and inflammation. ARN19702 is a selective, orally active, reversible, and brain-penetrant NAAA inhibitor with an IC50 of ~230 nM for human NAAA.
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| ln Vitro |
In vitro, ARN19702 is a selective, reversible inhibitor of human NAAA with an IC50 of ~230 nM. It inhibits NAAA by a non-covalent mechanism. These in vitro properties make ARN19702 a valuable tool for studying NAAA function and the role of PEA in pain and inflammation pathways.
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| ln Vivo |
ARN19702 (3-10 mg/kg; oral; daily; for 7 days) reduces nociception associated with paclitaxel-induced neuropathy without inducing subacute antinociceptive tolerance in male rats [1] . In male mice, ARN19702 (0.1-30 mg/kg; p.o.) dose-dependently attenuates the spontaneous nociceptive response induced by intraplantar injection of formalin as well as intraplantar injection of carrageenan, paw incision, or sciatic nerve Hypersensitivity reaction caused by ligation[1]. ..ARN19702 (3-10 mg/kg; oral) exerts significant protective effects against multiple sclerosis in mice [2]. Pharmacokinetic properties of ARN19702 in mice 3 mg/kg, iv 3 mg/kg, po Cmax (ng/mL) 1660±166 613±68 Tmax (min) (5.0) 30 CL (mL/min/Kg ) 33.2±1.6 49 ±8 t1/2 (min) 73.9±3.7 104±16 AUC plasma (h×ng/mL) 1366.8±68.3 988±157 AUC brain (h×ng/mL) 404.3±109.1 181±28 F (%) - 72±11
In vivo, ARN19702 has pain relief effects and exhibits a broad analgesic profile. As an orally active and brain-penetrant compound, it is suitable for central nervous system applications. ARN19702 is currently under preclinical investigation for central nervous system-related conditions. However, detailed in vivo efficacy data are limited in publicly available sources. |
| Enzyme Assay |
The in vitro enzyme assay for ARN19702 involves measuring its inhibition of NAAA enzymatic activity. Recombinant human NAAA is incubated with the compound at various concentrations in the presence of a fluorescent or radiolabeled PEA substrate. NAAA activity is measured by quantifying the production of palmitic acid or ethanolamine using HPLC, mass spectrometry, or fluorescence-based assays. The IC50 for NAAA inhibition is calculated from dose-response curves.
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| Cell Assay |
The in vitro cell-based assay for ARN19702 involves culturing cells that express NAAA and treating them with the compound to assess effects on PEA hydrolysis. Cells are treated with ARN19702 at various concentrations, and PEA levels in cell lysates or conditioned media are measured by LC-MS/MS or ELISA. Inflammatory cytokine production or pain-related signaling pathways can be assessed to evaluate functional effects of NAAA inhibition. Cell viability is assessed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
Animal/Disease Models: SD (SD (Sprague-Dawley)) rats (200-220 g) injected with paclitaxel [1]
Doses: 3 mg/kg and 10 mg/kg Route of Administration: Oral; injection. Daily; 7 days in a row (subchronic) Experimental Results: diminished nociception associated with paclitaxel-induced neuropathy. In vivo animal studies for ARN19702 have been conducted in preclinical models of pain. Rodents are administered ARN19702 orally at various doses, and analgesic effects are assessed using standard pain models such as the formalin test, hot plate test, or von Frey test. Inflammatory markers and PEA levels in tissues may be measured. ARN19702 is currently under preclinical investigation for central nervous system-related conditions. Standard protocols for pain models are employed. |
| ADME/Pharmacokinetics |
ARN19702 is an orally active small molecule with favorable pharmacokinetic properties. It is a brain-penetrant compound, making it suitable for central nervous system applications. It has a molecular weight of 447.55 and a molecular formula of C21H22FN3O3S2. The compound can be formulated for in vivo administration. Detailed PK parameters such as half-life, Cmax, and bioavailability are available from preclinical studies.
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| Toxicity/Toxicokinetics |
The toxicity profile of ARN19702 has been evaluated in preclinical studies. As an NAAA inhibitor that increases PEA levels, its primary safety concerns would relate to on-target effects on pain and inflammation pathways. Standard toxicology assessments would include acute and sub-chronic toxicity studies in rodents and dogs, with endpoints including clinical signs, body weight, clinical pathology, and histopathology. No significant toxicity has been reported in available literature.
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| References |
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| Additional Infomation |
ARN19702 is a research compound and has not been approved for clinical use. It is a selective, orally active, reversible, and brain-penetrant inhibitor of NAAA with an IC50 of ~230 nM for human NAAA. ARN19702 exhibits a broad analgesic profile and has pain relief effects. It is currently under preclinical investigation for central nervous system-related conditions and is a valuable tool for studying NAAA function and pain pathways.
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| Molecular Formula |
C21H22FN3O3S2
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| Molecular Weight |
447.5461
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| Exact Mass |
447.11
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| Elemental Analysis |
C, 56.36; H, 4.96; F, 4.25; N, 9.39; O, 10.72; S, 14.33
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| CAS # |
1971937-18-4
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| PubChem CID |
132145761
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| Appearance |
Solid powder
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| LogP |
3.9
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
732
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCS(=O)(=O)C1=CC=CC=C1C(=O)N2CCN(C[C@@H]2C)C3=NC4=C(S3)C=C(C=C4)F
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| InChi Key |
UKQOLPNYRVPCBM-AWEZNQCLSA-N
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| InChi Code |
InChI=1S/C21H22FN3O3S2/c1-3-30(27,28)19-7-5-4-6-16(19)20(26)25-11-10-24(13-14(25)2)21-23-17-9-8-15(22)12-18(17)29-21/h4-9,12,14H,3,10-11,13H2,1-2H3/t14-/m0/s1
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| Chemical Name |
(S)-(2-(ethylsulfonyl)phenyl)(4-(6-fluorobenzo[d]thiazol-2-yl)-2-methylpiperazin-1-yl)methanone
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| Synonyms |
ARN19702; ARN 19702; ARN-19702;
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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) |
DMSO : ~100 mg/mL (~223.44 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2344 mL | 11.1719 mL | 22.3439 mL | |
| 5 mM | 0.4469 mL | 2.2344 mL | 4.4688 mL | |
| 10 mM | 0.2234 mL | 1.1172 mL | 2.2344 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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