ARN19702

• CAT Number: I045146
• CAS Number: 1971937-18-4
• Purity: ≥95%
• Synonyms: (2-ethylsulfonylphenyl)-[(2S)-4-(6-fluoro-1,3-benzothiazol-2-yl)-2-methylpiperazin-1-yl]methanone
• InChI: 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
• InChIKey: UKQOLPNYRVPCBM-AWEZNQCLSA-N
• SMILES: CCS(=O)(=O)C1=CC=CC=C1C(=O)N2CCN(CC2C)C3=NC4=C(S3)C=C(C=C4)F

ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 230 nM for human NAAA. ARN19702 has pain relief effects[1][2].
ARN19702 (3-10 mg/kg; po; daily; for 7 consecutive days) reduces nociception associated with Paclitaxel-induced neuropathy without development of subacute antinociceptive tolerance in male rats[1].
In male mice, ARN19702 (0.1-30 mg/kg; po) attenuates in a dose-dependent manner the spontaneous nocifensive response elicited by intraplantar formalin injection and the hypersensitivity caused by intraplantar carrageenan injection, paw incision, or sciatic nerve ligation[1]..
ARN19702 (3-10 mg/kg; po) produces remarkable protective effects against multiple sclerosis in mice[2].
Pharmacokinetic properties of ARN19702 in mice

3 mg/kg,i.v
3 mg/kg, p.o.

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

AUCplasma (h×ng/mL)
1366.8±68.3
988±157

AUCbrain (h×ng/mL)
404.3±109.1
181±28

F (%)
–
72±11