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475741

JZL 184 hydrate

Name: JZL 184 hydrate
Brand: MM

The MAGL Inhibitor III, JZL184, also referenced under CAS 1101854-58-3, controls the biological activity of MAGL.

別名:

MAGL Inhibitor III, JZL184, 4-Nitrophenyl-4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate, Monoacylglycerol Lipase Inhibitor III, JZL184

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この商品について

実験式（ヒル表記法）:

C₂₇H₂₄N₂O₉

CAS番号:

1101854-58-3

分子量:

520.49

MDL number:

MFCD11976911

UNSPSC Code:

12352200

NACRES:

NA.77

Assay:

≥97% (HPLC)

Form:

solid

Storage condition:

OK to freeze, protect from light

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特性

製品名

MAGL Inhibitor III, JZL184, The MAGL Inhibitor III, JZL184, also referenced under CAS 1101854-58-3, controls the biological activity of MAGL.

Quality Segment

100

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

white to off-white

solubility

DMSO: 10 mg/mL

shipped in

wet ice

storage temp.

−20°C

SMILES string

[N+](=O)([O-])c1ccc(cc1)OC(=O)N2CCC(CC2)C(O)(c5cc6c(cc5)OCO6)c3cc4c(cc3)OCO4

InChI

1S/C27H24N2O9/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

InChI key

SEGYOKHGGFKMCX-UHFFFAOYSA-N

詳細

General description

A cell-permeable, blood-brain-barrier-permeant, and orally available carbamate compound that selectively inhibit MAGL (monoacylglycerol lipase) activity over FAAH (fatty acid amide hydrolase) and 35 other murine brain serine hydrolases, both in vitro (IC₅₀ = 6 - 8 nM against 2-AG hydrolysis by MAGL vs. 4 µM against anandamide/AEA hydrolysis by FAAH) and in mice in vivo (5-fold 2-AG enhancement and 75% MAGL activity inhibition in brain membrane from mice 4 hr after a single JZL184 dosage at 4 mg/kg via i.p.) in an irreversible, time- and dose-dependent manner. A great complement to the FAAH inhibitor URB597 (Cat. No. 341249 ) in differentiating the roles of CB1 and CB2 (type I and II cannabinoid receptors) in eCB- (endocannabinoid) mediated cellular signaling and in vivo physiological effects. Reported to be equally effective against human and murine MAGL, but inhibit rat MAGL with a ~10-fold lower potency.

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Nomura, D.K., et al. 2010. Cell140, 49.
Long, J.Z., et al. Nature Chem. Biol.16, 744.
Long, J.Z., et al. 2009. Nature Chem. Biol.5, 37.
Pan, B., et al. 2009. J. Pharmacol. Exp. Ther.331, 591.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

保管分類

11 - Combustible Solids

一体何が起きているの？

WGK 2

引火点 (F)

Not applicable

引火点（°C）