JP83

JP83

Catalog Number:
L002373133APE
Mfr. No.:
APE-C4983
Price:
$226
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      • Overview
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          Background

          IC50: 14 nM for the human recombinant enzymeJP83 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.

      • Properties
        • Alternative Name
          3'-carbamoyl-biphenyl-3-yl-hexylphenylcarbamate
          CAS Number
          887264-44-0
          Molecular Formula
          C26H28N2O3
          Molecular Weight
          416.5
          Appearance
          A crystalline solid
          Purity
          98.00%
          Solubility
          ≤1mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
          Storage
          Store at -20°C

          * For Research Use Only

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