[CAS NO. 1101854-58-3] JZL184

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PRODUCTS SPECIFICATIONS [1101854-58-3]

Catalog

HY-15249

Brand

MCE

CAS

1101854-58-3

DESCRIPTION [1101854-58-3]

Overview

MDL	-
Molecular Weight	520.49
Molecular Formula	C27H24N2O9
SMILES	OC(C1=CC=C(OCO2)C2=C1)(C3CCN(C(OC4=CC=C([N+]([O-])=O)C=C4)=O)CC3)C5=CC(OCO6)=C6C=C5

For research use only. We do not sell to patients.

2 Publications Citing Use of MCE

Summary

JZL 184 is a potent, selective and irreversible MAGL inhibitor that blocks 2-Arachidonoylglycerol (2-AG) hydrolysis in brain membranes ( IC ₅₀ of 8 nM). JZL 184 displays >300-fold selectivity for MAGL over FAAH ^[1] ^[2] .

IC50 & Target

IC50: 8 nM (2-Arachidonoylglycerol (2-AG) hydrolysis) ^[1]

In Vitro

JZL 184 displays IC ₅₀ values of 8 nM and 4 μM for blockade of 2-AG and oleamide (FAAH substrate) hydrolysis in brain membranes, respectively. Comparable inhibitory effects are observed with recombinant MAGL and FAAH when expressed in COS7 cells ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JZL 184 (4-40 mg/kg; intraperitoneal injection; once; C57Bl/6 mice) treatment produces a rapid and sustained blockade of brain 2-AG hydrolase activity in mice, resulting in 8-fold elevations in endogenous 2-AG levels that are maintained for at least 8 h. JZL 184-treated mice shows a remarkable array of CB1-dependent behavioral effects, including analgesia, hypomotility, and hypothermia ^[1] .
JZL 184 prolongs depolarization-induced suppression of excitation (DSE) in Purkinje neurons in cerebellar slices and DSE inhibition (DSI) in CA1 pyramidal neurons in hippocampal slices. JZL 184 produces greater enhancement of DSE/DSI in mouse neurons than that in rat neurons ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male C57Bl/6 mice (6-8 weeks old, 20-26 g) ^[1]
Dosage:	4 mg/kg, 8 mg/kg, 16 mg/kg, 40 mg/kg
Administration:	Intraperitoneal injection; once
Result:	Produced a rapid and sustained blockade of brain 2-AG hydrolase activity in mice, resulting in 8-fold elevations in endogenous 2-AG levels that were maintained for at least 8 h.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 35 mg/mL ( 67.24 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9213 mL	9.6063 mL	19.2127 mL
5 mM	0.3843 mL	1.9213 mL	3.8425 mL
10 mM	0.1921 mL	0.9606 mL	1.9213 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (4.80 mM); Suspended solution; Need ultrasonic
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

1-Piperidinecarboxylic acid, 4-[bis(1,3-benzodioxol-5-yl)hydroxymethyl]-, 4-nitrophenyl ester

JZL 184