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JZL184水合物,JZL 184 hydrate;≥97% (HPLC)

别名: JZL184 hydrate Empirical Formula (Hill Notation): C27H24N2O9 · xH2O CAS号: 1101854-58-3 分子量: 520.49 (anhydrous basis) MDL编号: MFCD12912421 PubChem化学物质编号: 329815406 NACRES: NA.77
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): J3455
CAS号: 1101854-58-3
MDL号: MFCD12912421
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¥2,007.38

说明

JZL 184水合物已被用作单酰基甘油脂肪酶的抑制剂,以研究其对人成骨细胞分化和增殖[1]以及突触后神经元的影响。
JZL184选择性地抑制MAGL,MAGL是主要负责内源性大麻素2-花生四烯酰甘油(2-AG)降解的酶。Anandamide和2-AG是激活大麻素受体CB1和CB2的两种内源性内源性大麻素。Anandamide主要由脂肪酸酰胺水解酶(FAAH)代谢,而单酰基甘油脂肪酶(MAGL)被认为是主要负责降解2-AG的酶。很难分离两者的活性,因为目前可用的大多数MAGL抑制剂不具有选择性,并且还抑制FAAH或其他酶。JZL 184 是首款具有纳摩尔便携性的 MAGL 选择性抑制剂,对 MAGL 与 FAAH 的选择性超过 200 倍。当给予小鼠时,JZL184使大脑中2-花生四烯酰甘油的水平增加了约8倍,对anandamide的水平没有影响。

应用

JZL 184 hydrate has been used as an inhibitor of monoacylglycerol lipase to study its effect on human osteoblast differentiation and proliferation[1] and postsynaptic neurons.[2]
 

生化/生理作用

JZL184 selectively inhibits MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG). Anandamide and 2-AG are the two endogenous endocannabinoids that activate the cannabinoid receptors CB1 and CB2. Anandamide is predominantly metabolized by fatty acid amide hydrolase (FAAH), whereas monoacylglycerol lipase (MAGL) is thought to be the enzyme primarily responsible for the degradation of 2-AG. It is difficult to separate the activities of the two because most currently available inhibitors of MAGL are not selective, and also inhibit FAAH or other enzymes. JZL 184 is the first selective inhibitor of MAGL with nanomolar portency and over 200-fold selectivity for MAGL vs FAAH. When administered to mice, JZL184 increased levels of 2-arachidonoylglycerol in the brain by about 8-fold, with no effect on levels of anandamide.
 

特点和优势

This compound is featured on the Cannabinoid Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
 
 

属性

质量水平

测定

≥97% (HPLC)

形式

powder

颜色

light yellow to yellow-green

溶解性

DMSO: >20 mg/mL

储存温度

2-8°C

SMILES string

O.OC(C1CCN(CC1)C(=O)Oc2ccc(cc2)[N+]([O-])=O)(c3ccc4OCOc4c3)c5ccc6OCOc6c5

InChI

1S/C27H24N2O9.H2O/c30-26(38-21-5-3-20(4-6-21)29(32)33)28-11-9-17(10-12-28)27(31,18-1-7-22-24(13-18)36-15-34-22)19-2-8-23-25(14-19)37-16-35-23;/h1-8,13-14,17,31H,9-12,15-16H2;1H2

InChI key

HNSBVGMOKGQJLT-UHFFFAOYSA-N

 

安全信息

象形图

Skull and crossbones

警示用语:

Danger

危险声明

危险分类

Acute Tox. 3 Oral

储存分类代码

6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

商品规格
属性名称属性值
储存温度 Storage temp.2-8°C冷藏
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16