JP83 |
Catalog No.GC12546
One-Click Copy Product Info
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irreversible fatty acyl amide hydrolase (FAAH) inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 887264-44-0
Sample solution is provided at 25 µL, 10mM.
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IC50: 14 nM for the human recombinant enzyme
JP83 is an irreversible fatty acyl amide hydrolase (FAAH) inhibitor.
The enzyme fatty acyl amide hydrolase (FAAH) is capable of hydrolyzing anandamide and other esters and amides with long unsaturated acyl chains, which is widely expressed in brain and other tissues.
In vitro: JP83 was identified as an irreversible FAAH inhibitor of the carbamate class when it was tested using radiolabeled oleamide as the substrate. MS results indicated that it inhibited FAAH by carbamylation of the enzyme’s serine nucleophile. In addition, JP83 was found to be able to inhibit FAAH with equal or greater potency than URB597 [1].
In vivo: Mice were treated with JP104, a close analog of JP83, after which they were sacrificed and their tissues removed for click chemistry analysis. It was found that at 1 mg/kg of JP104, FAAH labeling was ~80% of maximum in the brain, while none of the liver and kidney targets were modified to greater than 20%. Furthermore, the nearly complete inactivation of brain FAAH by JP104 at 1 mg/kg was confirmed by competitive ABPP studies with FP-Rh. In contrast, JP104 couldnot reduce the intensity of FP-Rh signals in liver and kidney proteomes significantly [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Alexander, J. P., and Cravatt, B.F. Mechanism of carbmate inactivation of FAAH: Implications for the design of covalent inhibitors and in vivo functional probes for enzymes. Chemistry & Biology 12, 1179-1187 (2005).
| Cas No. | 887264-44-0 | SDF | |
| Chemical Name | 3'-carbamoyl-biphenyl-3-yl-hexylphenylcarbamate | ||
| Canonical SMILES | O=C(NCCCCCCc1ccccc1)Oc1cccc(c1)c1cccc(c1)C(=O)N | ||
| Formula | C26H28N2O3 | M.Wt | 416.5 |
| Solubility | ≤1mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.401 mL | 12.0048 mL | 24.0096 mL |
| 5 mM | 480.2 μL | 2.401 mL | 4.8019 mL |
| 10 mM | 240.1 μL | 1.2005 mL | 2.401 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)