[CAS NO. 1210004-12-8] JZL195
PRODUCTS SPECIFICATIONS [1210004-12-8]
DESCRIPTION [1210004-12-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 433.46 |
| Molecular Formula | C24H23N3O5 |
| SMILES | O=C(OC1=CC=C([N+]([O-])=O)C=C1)N(CC2)CCN2CC3=CC(OC4=CC=CC=C4)=CC=C3 |
1 Publications Citing Use of MCE
Summary
JZL195 is a selective and efficacious dual fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) inhibitor with IC 50 s of 2 and 4 nM, respectively [1] .
IC50 & Target
IC50: 2 nM (FAAH), 4 nM (MAGL) [1]
In Vitro
JZL195 produces near-complete blockade of FP-Rh labeling of both mouse brain FAAH and MAGL at concentrations as low as 100 nM (IC
50
values of 13 and 19 nM, respectively)
[1]
.
JZL195 inhibits rat and human FAAH and MAGL enzymes with IC
50
values in the range of ≈10-100 nM based on competitive ABPP assays
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
JZL195 (20 mg/kg; i.p.) produces an antinociceptive response in the tail immersion assay [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male C57BL/6J mice [1] |
| Dosage: | 20 mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Produced a much greater antinociceptive response in the tail immersion assay compared with inhibitors of either FAAH or MAGL alone. |
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 : 50 mg/mL ( 115.35 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3070 mL | 11.5351 mL | 23.0702 mL |
| 5 mM | 0.4614 mL | 2.3070 mL | 4.6140 mL |
| 10 mM | 0.2307 mL | 1.1535 mL | 2.3070 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution
References
- [1] Long JZ, et al. Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid crosstalk in vivo. Proc Natl Acad Sci U S A. 2009 Dec 1;106(48):20270-5.
- [2] Anderson WB, et al. Actions of the dual FAAH/MAGL inhibitor JZL195 in a murine inflammatory pain model. Neuropharmacology. 2014 Jun;81:224-30.