(4-([1,1′-Biphenyl]-4-yl)-1<I>H</I>-1,2,3-triazol-1-yl)(2-benzylpiperidin-1-yl)methanone

产品名称：

1402612-55-8
KT109
(4-([1,1′-Biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl)(2-benzylpiperidin-1-yl)methanone

产品介绍：

产品说明

包装

5, 25 mg in glass bottle

生化/生理作用

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.

基本信息

经验(实验)分子式	C₂₇H₂₆N₄O
分子量	422.52
NACRES	NA.77

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
颜色	white to beige
溶解性	DMSO: 10 mg/mL, clear
储存温度	2-8℃
SMILES string	O=C(N1CCCCC1Cc2ccccc2)n3cc(nn3)-c4ccc(cc4)-c5ccccc5

安全信息

象形图
警示用语：	Warning
危险声明	H302 - H413
预防措施声明	P273 - P301 + P312 + P330
危险分类	Acute Tox. 4 Oral - Aquatic Chronic 4
储存分类代码	11 - Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable