1,6-双(环己基脒基羰基氨基)己烷

简介生物活性靶点体外研究体内研究 1,6-双(环己基脒基羰基氨基)己烷试剂级价格

1,6-双(环己基脒基羰基氨基)己烷

CAS号:83654-05-1
英文名:1,6-BIS(CYCLOHEXYLOXIMINOCARBONYLAMINO)HEXANE
中文名:1,6-双(环己基脒基羰基氨基)己烷
CBNumber:CB9686432
分子式:C20H34N4O4
分子量:394.52
MOL File:83654-05-1.mol

1,6-双(环己基脒基羰基氨基)己烷化学性质

熔点 :118-121℃
密度 :1.21±0.1 g/cm3(Predicted)
RTECS号 :GW1485000
储存条件 :Sealed in dry,Room Temperature
溶解度 :DMSO: 9 mg/mL
形态 :solid
酸度系数(pKa) :13.81±0.46(Predicted)
颜色 :white
稳定性 :Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months

安全信息

安全说明 :22-24/25
WGK Germany :3

1,6-双(环己基脒基羰基氨基)己烷性质、用途与生产工艺

简介
1,6-双(环己基脒基羰基氨基)己烷可抑制多种细胞类型和组织中的DAG 脂肪酶活性，包括犬血小板、牛肾上腺嗜铬细胞、人肾上腺肾小球细胞、大鼠甲状腺叶和胰腺小叶。犬血小板中的 IC50 为 4 μM。
生物活性 RHC 80267 (U-57908) 是一种有效的、具有选择性的 diacylglycerol lipase (DAGL, DAG lipase) 的抑制剂，其对 cholinesterase 活性的IC50值为4 μM。RHC 80267 可抑制 cyclooxygenase (COX) 的活性，phospholipase C (PLC) 的活性和 phosphatidylcholine (PC) 的水解作用。
靶点
Target Value
cholinesterase
(Cell-free assay) 4 μM
体外研究

The potentiation by RHC 80267 of the relaxation to acetylcholine could be caused by the inhibition of cholinesterase: (1) RHC 80267 does not affect the responses to carbachol, the carbamyl derivative of acetylcholine which only differs from acetylcholine by its resistance to hydrolysis by cholinesterase, and (2) the effect of RHC 80267 is mimicked by the inhibitor of cholinesterase neostigmine, RHC 80267 showing no additional effect in the presence of a maximally effective concentration of neostigmine. The determination of the effect of RHC 80267 on the cholinesterase activity of brain homogenate confirmed that RHC 80267 inhibits this enzyme in the same range of concentrations increasing the relaxation to acetylcholine, namely at 1-10 μM.
体内研究

RHC 80267 (40 μM) enhances contractions induced by U46619 (a thromboxane A2 analog) in human and rat pulmonary arteries (hPAs and rPAs, respectively) and by angiotensin II (ANG II) in rPAs in an endothelium-dependent manner.