SML2985

AM-0902

≥98% (HPLC)

• Synonyme(s) : 1-((3-(4-Chlorophenethyl)-1,2,4-oxadiazol-5-yl)methyl)-7-methyl-1H-purin-6(7H)-one, 1-[[3-[2-(4-Chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-1,7-dihydro-7-methyl-6H-Purin-6-one, AM 0902, AMG0902
• Formule empirique (notation de Hill): C₁₇H₁₅ClN₆O₂
• Numéro CAS: 1883711-97-4
• Poids moléculaire : 370.79
• Code UNSPSC : 51111800
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: powder
• Couleur: white to beige
• Solubilité: DMSO: 2 mg/mL, clear
• Température de stockage: 2-8°C
• Chaîne SMILES: Clc1ccc(cc1)CCc2n[o]c(n2)C[n]3[c](c4[n](cnc4nc3)C)=O
• InChI: 1S/C17H15ClN6O2/c1-23-9-19-16-15(23)17(25)24(10-20-16)8-14-21-13(22-26-14)7-4-11-2-5-12(18)6-3-11/h2-3,5-6,9-10H,4,7-8H2,1H3
• Clé InChI: AWJBWNUUODWOKQ-UHFFFAOYSA-N

Description

Actions biochimiques/physiologiques

AM-0902 (AMG0902) is a potent and selective transient receptor potential A1 (TRPA1) antagonist (rat/human TRPA1 IC50 = 71/131 nM against AITC-induced 45Ca²⁺ influx in respective CHO transfectants with [AITC] = EC90 = 3 μM/hTRPA1 or 35 μM/rTRPA1; human/rat IC50 = 24/20 nM by FLIPR) with little potency against human TRPV1/4, human CYP3A4/2D6, rat TRPV1/3, rat TRPM8, or mouse NaV1.7. AM-0902 effectively reduces AITC-induced flinching in a rat pain model (by 65% and 85%, respectively, with 10 or 30 mg/kg AM-0902 p.o. 1 hr prior to AITC injection) with good pharmacokinetic properties, oral availability and brain exposure (F = 60%, B/P = 0.2; 30 mg/kg p.o. in rats) in vivo.

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable