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Purity: ≥98%
JZL195 is a potent, selective and efficacious dual FAAH/MAGL (fatty acid amide hydrolase/monoacylglycerol lipase) inhibitor with IC50 of 13 nM and 19 nM for mouse brain FAAH and MAGL respectively. JZL195 exhibits broad activity in the tetrad test for CB1 agonism, causing analgesia, hypomotilty, and catalepsy. Comparison of JZL195 to specific FAAH and MAGL inhibitors identified behavioral processes that were regulated by a single endocannabinoid pathway (e.g., hypomotility by the 2-AG/MAGL pathway) and, interestingly, those where disruption of both FAAH and MAGL produced additive effects that were reversed by a CB1 antagonist. In addition, JZL195 reduces inflammation induced allodynia at doses below those which produce side-effects, and displays greater efficacy that FAAH or MAGL inhibitors. Thus, dual FAAH/MAGL inhibition has the potential to alleviate inflammatory pain with reduced cannabinoid-like side-effects.
| ln Vitro |
FP-Rh labeling of mouse brain FAAH and MAGL is nearly completely blocked by JZL195 at concentrations as low as 100 nM (IC50 values of 13 and 19 nM, respectively)[1]. According to competitive ABPP assays, JZL195 inhibits the rat and human FAAH and MAGL enzymes with IC50 values in the range of ≈10-100 nM[1].
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| ln Vivo |
In the tail immersion assay, JZL195 (20 mg/kg; ip) elicits an antinociceptive response[1].
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| Animal Protocol |
Animal/Disease Models: Male C57BL/6J mice[1]
Doses: 20 mg/kg Route of Administration: intraperitoneal (ip)injection Experimental Results: Produced a much greater antinociceptive response in the tail immersion assay compared with inhibitors of either FAAH or MAGL alone. |
| 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. |
| Molecular Formula |
C₂₄H₂₃N₃O₅
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| Molecular Weight |
433.46
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| CAS # |
1210004-12-8
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| Related CAS # |
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| SMILES |
O=C(OC1=CC=C([N+]([O-])=O)C=C1)N(CC2)CCN2CC3=CC(OC4=CC=CC=C4)=CC=C3
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.77 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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