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Merck

J3455

Sigma-Aldrich

JZL 184 水合物

≥97% (HPLC)

别名:

JZL184 hydrate

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About This Item

经验公式(希尔记法):
C27H24N2O9 · xH2O
分子量:
520.49 (anhydrous basis)
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

品質等級

化驗

≥97% (HPLC)

形狀

powder

顏色

light yellow to yellow-green

溶解度

DMSO: >20 mg/mL

儲存溫度

2-8°C

SMILES 字串

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 密鑰

HNSBVGMOKGQJLT-UHFFFAOYSA-N

應用

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

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.

特點和優勢

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.

象形圖

Skull and crossbones

訊號詞

Danger

危險聲明

危險分類

Acute Tox. 3 Oral

儲存類別代碼

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

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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其他客户在看

Olga Karpińska et al.
American journal of physiology. Regulatory, integrative and comparative physiology, 312(6), R883-R893 (2017-03-31)
Recent evidence suggests that endocannabinoids acting via cannabinoid CB

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