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[CAS NO. 1101854-58-3] JZL184
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15249 |
| Brand: | MCE |
| CAS: | 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 |
2 Publications Citing Use of MCE
Summary
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
DMSO : ≥ 35 mg/mL ( 67.24 mM )
* "≥" means soluble, but saturation unknown.
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 |
References
- [1] Long JZ, et al. Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects. Nat Chem Biol. 2009 Jan;5(1):37-44.
- [2] Pan B, et al. Blockade of 2-arachidonoylglycerol hydrolysis by selective monoacylglycerol lipase inhibitor 4-nitrophenyl 4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate (JZL184) Enhances retrograde endocannabinoid signaling. J Pharma
Synonyms
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