ARN-19702

ARN19702 is an orally active, reversible N-Acylethanolamine acid amidase(NAAA) inhibitor (IC50 on human NAAA = 230 nM) that produces remarkable protective effects against multiple sclerosis in mice.

ARN-19702 Chemical Structure

ARN-19702 Chemical Structure

CAS: 1971937-18-4

Purity & Quality Control

Batch: E045401 DMSO] 89 mg/mL] false] Ethanol] 4 mg/mL] false] Water] Insoluble] false Purity: 99.62%
99.62

Biological Activity

Description ARN19702 is an orally active, reversible N-Acylethanolamine acid amidase(NAAA) inhibitor (IC50 on human NAAA = 230 nM) that produces remarkable protective effects against multiple sclerosis in mice.
Targets
NAAA [1]
0.23 μM
In vitro
In vitro

ARN19702 is a selective, orally active, reversible and brain-penetrant N-acylethanolamine acid amidase (NAAA), by a non-covalent mechanism.[1]

Cell Research Cell lines HEK293 cells
Concentrations --
Incubation Time 2 h
Method

Lysosomal extracts of hNAAA-overexpressing HEK293 cells are incubated with vehicle (2% DMSO), ARN-19702, for 2 h before addition of activity-based NAAA probe.

In Vivo
In vivo

ARN-19702 attenuates the spontaneous nocifensive response elicited and the hypersensitivity in male mouse model of acute and neuropathic pain, also reduces nociception associated with paclitaxel-induced neuropathy without development of subacute antinociceptive tolerance in male rat model of acute and neuropathic pain.[2]

Animal Research Animal Models mouse and rat models of acute and neuropathic pain
Dosages 3-10 mg/kg for male rats; 0.1-30 mg/kg for male mice
Administration p.o.

Chemical lnformation & Solubility

Molecular Weight 447.55 Formula

C21H22FN3O3S2

CAS No. 1971937-18-4 SDF --
Smiles CC[S](=O)(=O)C1=CC=CC=C1C(=O)N2CCN(CC2C)C3=NC4=CC=C(F)C=C4S3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 89 mg/mL ( (198.86 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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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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