KT-109

更新时间：2024-01-13 11:05:19

KT-109结构式	常用名	KT-109	英文名	KT-109
	CAS号	1402612-55-8	分子量	422.522
	密度	1.2±0.1 g/cm3	沸点	637.3±53.0 °C at 760 mmHg
	分子式	C₂₇H₂₆N₄O	熔点	N/A
	MSDS	中文版美版	闪点	339.3±30.9 °C
	符号	GHS07	信号词	Warning

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)。

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	(2-Benzyl-1-piperidinyl)[4-(4-biphenylyl)-1H-1,2,3-triazol-1-yl]methanone
英文别名	更多

描述	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)。
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)

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)

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

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

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...

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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...

(2-Benzyl-1-piperidinyl)[4-(4-biphenylyl)-1H-1,2,3-triazol-1-yl]methanone

Methanone, (4-[1,1'-biphenyl]-4-yl-1H-1,2,3-triazol-1-yl)[2-(phenylmethyl)-1-piperidinyl]-