JZL 195

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JZL 195 is a potent dual inhibitor of Monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH), enzymes that degrade the endocannabinoids 2-arachidonoylglycerol (2-AG) and anandamide (AEA), the endogenous ligands for the cannabinoid G-protein coupled receptors CB1 and CB2. IC50 values are 2 nM for MAGL and4 nM for FAAH. JZL195 has been shown to inhibit endocannabinoid hydrolysis andelevate 2-AG and AEA levels in vivo.

Product Description

 

JZL 195 video

 

 


 

I.JZL 195 basic Characters:

 

Name: JZL 195
CAS: 1210004-12-8
Molecular Formula: C24H23N3O5
Molecular Weight: 433.457
Melt Point:
-20°C
Color: White solid

 


 

II. JZL 195 cycle

 

1.Names:

Synonym:
JZL 195;4-nitrophenyl 4-(3-phenoxybenzyl)piperazine-1-carboxylate;4-[(3-Phenoxyphenyl)methyl]-1-piperazinecarboxylic acid 4-nitrophenyl ester

 

2. JZL 195 Usage:

Fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) mediate the hydrolysis of the endocannabinoids arachidonoyl ethanolamide (AEA) and 2-arachidonoylglycerol (2-AG), respectively. JZL 195 is a potent inhibitor of both FAAH andMAGL (IC50s = 2 and 4 nM, respectively).1 It poorly inhibits neuropathy target esterase and ABHD6 and does not inhibit other brain serine hydrolases. JZL 195 displays time-dependent inhibition of FAAH and MAGL in vivo, consistent with a covalent mechanism of activation.1 The in vivo inhibitory actions of JZL 195 against FAAHand MAGL are comparable to those of the selective inhibitors PF-3845 (Item No. 13279) and JZL 184 (Item No. 13158), respectively.1 Through its inhibitory actions, JZL 195 simultaneously augments brain levels of AEA and 2-AG, producing antinociceptive, cataleptic, and hypomotility effects like those produced by direct CB1 agonists. JZL 195 is also offered as part of the Tocriscreen Plus.

 

3.What is the dosage of JZL 195 ?

Solubility:
DMSO to 50 mM
ethanol to 5 mM
Stability and Solubility Advice:
Some solutions can be difficult to obtain and can be encouraged by rapid stirring, sonication or gentle warming (in a 45-60°C water bath). Information concerning product stability, particularly in solution, has rarely been reported and in most cases we can only offer a general guide. Our standard recommendations are: SOLIDS: Provided storage is as stated on the product label and the vial is kept tightly sealed, the product can be stored for up to 6 months from date of receipt. SOLUTIONS: We recommend that stock solutions, once prepared, are stored aliquoted in tightly sealed vials at -20°C or below and used within 1 month. Wherever possible solutions
should be made up and used on the same day.

 

4.How JZL 195 works?

The dual FAAH/MAGL inhibitor JZL195 has enhanced effects on endocannabinoid transmission and motor behavior in rats as compared to those of the MAGL inhibitorJZL184.
The biological actions of the endocannabinoids anandamide and 2-arachidonoyl glycerol (2-AG) are terminated by enzymatic hydrolysis of these lipids via fatty acid amide hydrolase (FAAH ) and monoacylglycerol lipase (MAGL), respectively. While several selective FAAH inhibitors have been developed and characterized in vitro and in vivo, none of the initial MAGL blockers have shown adequate potency and specificity for in vivo applications. More recently, a selective MAGL inhibitor, JZL184, hasbeen shown to produce a long-lasting elevation of brain 2-AG, as well as cannabinoid-like behavioral responses in mice. However, its effectiveness in rats remains controversial. Indeed, although JZL184 can elicit behavioral responses that are mediated, at least in part, via activation of cannabinoid CB1 receptors, several reports indicate that this compound does not alter 2-AG levels in this species. In this study we compared the behavioral and neurochemical effects of JZL 184 with those of thedual FAAH/MAGL inhibitor JZL195, and showed that systemic administration of the former can selectively elevate brain 2-AG in rats and produce motor suppression through a CB1-independent mechanism. These findings indicate that, despite its lowerpotency against rat MAGL, JZL184 can be used to enhance 2-AG transmission andelicit behavioral responses in rodents.
As our research,in contrast to JZL195, which decreased motor activity at all doses tested, JZL184 was effective only at the highest dose (30 mg/kg, p<0.05). The motor effects of both JZL compounds are also presented as time course over a 60 min period.

 

5.Warning:

5.1 Conditions for safe storage, including any incompatibilities.
Store in cool, well-ventilated area. Keep away from direct sunlight. Keep container tightly sealed until ready for use.Recommended storage temperature: Store at -20°C.
5.2 Use in a chemical fume hood, with air supplied by an independent system. Avoid inhalation, contact with eyes, skin and clothing. Avoid the formation of dust andaerosols. Use in a well-ventilated area. Keep away from sources of ignition. Avoid prolonged or repeated exposure.
5.3 Use in a laboratory fume hood where possible.
5.4 Please note that tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due toslight batch-to-batch variations.
5.6 Reactivity:Stable under recommended transport or storage conditions.
5.7 Chemical stability:Stable under recommended storage conditions.
5.8 Possibility of hazardous reactions:Hazardous reactions will not occur under normal transport or storage conditions. Decomposition may occur on exposure to conditions or materials listed below.
5.9 Conditions to avoid:Heat, moisture;Incompatible materials:Strong acids/alkalis, strong oxidising/reducing agents;Hazardous decomposition products:In combustion mayemit toxic fumes.

 

6.JZL 195:

Min order 10grams.
The inquiry on normal quantity(Within 1kg) can be sent out in 12 hours after payment.
For larger order can be sent out in 3 working days after payment.

 

7.JZL 195 Recipes:

To inquiry our Customer Representitive(CSR) for details, for your reference.

 

8.JZL 195 Marketing:

To be provided in the coming future.

 

9.Does JZL 195 Have Any Side Effects?

Dual inhibitor of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) (IC50 values are 2 and 4 nM respectively). Elevates anandamide and 2-arachidonoylglycerol levels in vivo. Shown to impair short-term memory in mice.

 


 

III. JZL 195 HNMR

 

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IV. How to buy JZL 195 from AASraw?

 

1.To contact us by our email inquiry system,or online skypecustomer service representative(CSR).
2.To provide us your inquired quantity and address.
3.Our CSR will provide you the quotation, payment term, tracking number, delivery ways and estimated arrival date(ETA).
4.Payment done and the goods will be sent out in 12 hours(For order within 10kg).
5.Goods received and give comments.

 


 

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