SML1364

KT109

≥98% (HPLC)

• Synonyme(s) : (4-([1,1′-Biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl)(2-benzylpiperidin-1-yl)methanone
• Formule empirique (notation de Hill): C₂₇H₂₆N₄O
• Numéro CAS: 1402612-55-8
• Poids moléculaire : 422.52
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: powder
• Couleur: white to beige
• Solubilité: DMSO: 10 mg/mL, clear
• Température de stockage: 2-8°C
• Chaîne SMILES: O=C(N1CCCCC1Cc2ccccc2)n3cc(nn3)-c4ccc(cc4)-c5ccccc5

Description

Actions biochimiques/physiologiques

KT109 is a potent and selective inhibitor of Diacylglycerol lipase DAGLβ. Diacylglycerol lipases DAGLα and DAGLβ are serine hydrolases that biosynthesize the endocannabinoid 2-arachidonoylglycerol (2-AG). A lack of selective inhibitors has hampered study of these lipases. KT109 is a potent and selective DAGLβ inhibitor with an IC₅₀ of 42 nM, ~60-fold selectivity for DAGLβ over DAGLα, and negligible activity against FAAH, MGLL and ABHD11, other key enzymes involved in endocannabinoid signaling. KT109 shows some inhibitory activity against PLA2G7 (IC₅₀ = 1 μM) but no inhibitory activity against cytosolic phospholipase A2 (cPLA2 or PLA2G4A). The main off target inhibition against ABHD6 (IC₅₀ = 16 nM) can be controlled for by use of the related compound, KT195, a potent (IC₅₀ = 10 nM) and selective ABHD6 inhibitor with negligible activity against DAGLβ. KT109 disrupts the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids, in mouse peritoneal macrophages.

Informations sur la sécurité

• Pictogrammes: GHS07
• Mention d'avertissement: Warning
• Mentions de danger: H302,H413
• Conseils de prudence: P273 - P301 + P312 + P330
• Classification des risques: Acute Tox. 4 Oral - Aquatic Chronic 4
• 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