[3-[4-[1-(2-phenylpiperidine-1-carbonyl)triazol-4-yl]phenyl]phenyl]-piperidin-1-ylmethanone

• 常用名: [3-[4-[1-(2-phenylpiperidine-1-carbonyl)triazol-4-yl]phenyl]phenyl]-piperidin-1-ylmethanone
• 英文名: KT185
• CAS号: 1472640-86-0
• 分子量: 519.64
• 密度: N/A
• 沸点: N/A
• 分子式: C₃₂H₃₃N₅O₂
• 熔点: N/A
• 闪点: N/A

用途

KT185 是口服有效的、能渗透大脑的ABHD6 的选择性抑制剂,其在 Neuro2A 细胞中测得的 IC50 值为0.21 nM。

名称

• 中文名: [3-[4-[1-(2-phenylpiperidine-1-carbonyl)triazol-4-yl]phenyl]phenyl]-piperidin-1-ylmethanone
• 英文名: KT185

生物活性

• 描述: KT185 是口服有效的、能渗透大脑的ABHD6 的选择性抑制剂,其在 Neuro2A 细胞中测得的 IC50 值为0.21 nM。
• 相关类别:
  研究领域 >> 其他
  信号通路 >> 代谢酶/蛋白酶 >> MAGL
• 靶点实验:

  IC50: ABHD6 (0.21 nM in Neuro2A cells)[1].

• 参考文献:

  [1]. Hsu KL, et al. Discovery and optimization of piperidyl-1,2,3-triazole ureas as potent, selective, and in vivo-active inhibitors of α/β-hydrolase domain containing 6 (ABHD6). J Med Chem. 2013 Nov 14;56(21):8270-9.

物理化学性质

• 分子式: C₃₂H₃₃N₅O₂
• 分子量: 519.64
• InChIKey: SGQNTNACVSWXMA-UHFFFAOYSA-N
• SMILES: O=C(c1cccc(-c2ccc(-c3cn(C(=O)N4CCCCC4c4ccccc4)nn3)cc2)c1)N1CCCCC1
• 外观性状: 固体
• 储存条件: 2-8°C，密封，干燥

安全信息

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

靶点实验

查看更多实验

实验名称：Inhibition of ABHD6 in FP-rhodamine-labelled mouse brain membrane at 10 nM preincubat... 来源：ChEMBL 靶标：Monoacylglycerol lipase ABHD6 External Id：CHEMBL3268596

实验名称：In vivo inhibition of ABHD6 in C57Bl/6 mouse liver at 20 mg/kg, ip after 4 hrs by FP-... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL3269001

实验名称：In vivo inhibition of ABHD6 in C57Bl/6 mouse liver at 5 to 10 mg/kg, ip after 4 hrs b... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL3269000

实验名称：In vivo inhibition of ABHD6 in C57Bl/6 mouse brain at 20 mg/kg, po after 4 hrs by FP-... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL3269003

实验名称：In vivo inhibition of FAAH in C57Bl/6 mouse brain up to 40 mg/kg, po after 4 hrs by F... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL3269002

实验名称：In vivo inhibition of ABHD6 in C57Bl/6 mouse liver at 10 to 40 mg/kg, po after 4 hrs ... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL3269005

实验名称：Inhibition of Aadacl1 in mouse Neuro2a cells at 3 nM after 4 hrs by ABPP-SILAC assay 来源：ChEMBL 靶标：Neutral cholesterol ester hydrolase 1 External Id：CHEMBL3269006

实验名称：Inhibition of ABHD6 in FP-rhodamine-labelled mouse brain membrane at 1 nM preincubate... 来源：ChEMBL 靶标：Monoacylglycerol lipase ABHD6 External Id：CHEMBL3268605

实验名称：Inhibition of FP-rhodamine-labelled recombinant mouse DAGLbeta expressed in HEK293T c... 来源：ChEMBL 靶标：Diacylglycerol lipase-beta External Id：CHEMBL3268606

实验名称：Inhibition of FP-rhodamine-labelled recombinant mouse LYPLA2 at 10 uM preincubated fo... 来源：ChEMBL 靶标：Acyl-protein thioesterase 2 External Id：CHEMBL3268611

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