KT-109

KT-109用途

KT-109是DAGLβ的有效选择性抑制剂,IC50为42 nM,对DAGLα的选择性约为60倍；对内源性大麻素信号传导中涉及的其他关键酶(包括FAAH,MAGL和ABHD11)的活性可忽略不计；破坏脂质网络参与巨噬细胞炎症反应,降低2-AG,以及小鼠腹膜巨噬细胞中的花生四烯酸和类二十烷酸；在炎症和神经性疼痛的小鼠模型中逆转伤害性行为；具有一个剩余的脱靶ABHD6(IC50=16nM)。

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KT-109名称

[ CAS 号 ]:
1402612-55-8

[ 中文名 ]:
(4-([1,1′-联苯]-4-基)-1H-1,2,3-三唑-1-基)(2-苄基哌啶 1-基)甲酮

[ 英文名 ]:
KT-109

[英文别名 ]:

KT-109生物活性

[ 描述 ]:

[参考文献]

References 1. Hsu KL, et al. Nat Chem Biol. 2012 Dec;8(12):999-1007. 2. Wilkerson JL, et al. Br J Pharmacol. 2016 May;173(10):1678-92. 3. Shin M, et al. Mol Pharm. 2017 Sep 13. doi: 10.1021/acs.molpharmaceut.7b00657. View Related Products by Target Diacylglycerol Lipase (DAGL)

KT-109物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
637.3±53.0 °C at 760 mmHg

[ 分子式 ]:
C₂₇H₂₆N₄O

[ 分子量 ]:
422.522

[ 闪点 ]:
339.3±30.9 °C

[ 精确质量 ]:
422.210663

[ LogP ]:
5.23

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
0.0±1.9 mmHg at 25°C

[ 折射率 ]:
1.653

[ 储存条件 ]:
2-8°C

KT-109安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H413

[ 警示性声明 ]:
P301 + P312 + P330

[ 危害码 (欧洲) ]:
Xn

[ 危险品运输编码 ]:
NONH for all modes of transport

KT-109文献

DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses.

Nat. Chem. Biol. 8(12) , 999-1007, (2012)

The endocannabinoid 2-arachidonoylglycerol (2-AG) is biosynthesized by diacylglycerol lipases DAGLα and DAGLβ. Chemical probes to perturb DAGLs are needed to characterize endocannabinoid function in b...

Development and optimization of piperidyl-1,2,3-triazole ureas as selective chemical probes of endocannabinoid biosynthesis.

J. Med. Chem. 56(21) , 8257-69, (2013)

We have previously shown that 1,2,3-triazole ureas (1,2,3-TUs) act as versatile class of irreversible serine hydrolase inhibitors that can be tuned to create selective probes for diverse members of th...

Serine hydrolase inhibitors block necrotic cell death by preventing calcium overload of the mitochondria and permeability transition pore formation.

J. Biol. Chem. 289(3) , 1491-504, (2014)

Perturbation of calcium signaling that occurs during cell injury and disease, promotes cell death. In mouse lung fibroblasts A23187 triggered mitochondrial permeability transition pore (MPTP) formatio...

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