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ARN19702

Catalog No. T9528 CAS 1971937-18-4

ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC 50 of 230 nM for human NAAA. ARN19702 exhibits a broad analgesic profile [1] [2].

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ARN19702, CAS 1971937-18-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 51.00
5 mg	In stock	$ 122.00
10 mg	In stock	$ 197.00
25 mg	In stock	$ 389.00
50 mg	In stock	$ 622.00
100 mg	In stock	$ 978.00
200 mg	In stock	$ 1,320.00
500 mg	In stock	$ 1,960.00
1 mL * 10 mM (in DMSO)	In stock	$ 133.00

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Purity: 100.00%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC 50 of 230 nM for human NAAA. ARN19702 exhibits a broad analgesic profile [1] [2].
Targets&IC50	NAAA:230 nM
In vivo	ARN19702, administered orally (po) at dosages of 3-10 mg/kg daily for seven consecutive days, effectively reduces Paclitaxel-induced neuropathic nociception in male rats without causing subacute antinociceptive tolerance [1]. In male mice, ARN19702 demonstrates a dose-dependent reduction in spontaneous nocifensive behaviors triggered by intraplantar formalin, and alleviates hypersensitivity following intraplantar carrageenan injection, paw incision, or sciatic nerve ligation, at dosages ranging from 0.1-30 mg/kg (po) [1]. Additionally, at a dosage range of 3-10 mg/kg (po), ARN19702 offers significant protection against multiple sclerosis in mice [2]. Pharmacokinetic analysis in mice reveals that at a 3 mg/kg dosage, ARN19702 achieves a maximum concentration (Cmax) of 1660±166 ng/mL and 613±68 ng/mL for intravenous (i.v.) and oral administration respectively, with corresponding times to reach Cmax (Tmax) of approximately 5.0 minutes (i.v.) and 30 minutes (po). The clearance (CL) rates stand at 33.2±1.6 mL/min/kg (i.v.) and 49±8 mL/min/kg (po), with half-lives (t 1/2) of 73.9±3.7 minutes (i.v.) and 104±16 minutes (po). Area under the curve (AUC) measurements indicate plasma levels of 1366.8±68.3 h×ng/mL (i.v.) and 988±157 h×ng/mL (po), and brain levels of 404.3±109.1 h×ng/mL (i.v.) and 181±28 h×ng/mL (po), with an oral bioavailability (F) of 72±11%.

Molecular Weight	447.55
Formula	C21H22FN3O3S2
CAS No.	1971937-18-4

Storage

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

Solubility Information

DMSO: 50 mg/mL (111.72 mM)

References and Literature

1. Yannick Fotio, et al. Antinociceptive Profile of ARN19702, (2-Ethylsulfonylphenyl)-[(2S)-4-(6-fluoro-1,3-benzothiazol-2-yl)-2-methylpiperazin-1-yl]methanone, a Novel Orally Active N-Acylethanolamine Acid Amidase Inhibitor, in Animal Models. J Pharmacol Exp Ther. 2021 Aug;378(2):70-76. 2. Marco Migliore Dr, et al. Second-Generation Non-Covalent NAAA Inhibitors are Protective in a Model of Multiple Sclerosis. Angew Chem Int Ed Engl. 2016 Sep 5;55(37):11193-11197.

Citations

1. Zhou L, Tian M, Zhang B, et al.Lysosome targeting fluorescent probe for NAAA imaging and its applications in the drug development for anti-inflammatory.International Journal of Biological Macromolecules.2024: 130307.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compound Library Orally Active Compound Library Bioactive Compounds Library Max NO PAINS Compound 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.

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Keywords

ARN19702 1971937-18-4 Others ARN 19702 ARN-19702 inhibitor inhibit

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