PL265

PL265 is an orally active dual enkephalinase inhibitor. PL265 is a prodrug of PL254, which can simultaneously and efficiently inhibit neutral endopeptidase (Neprilysin) and Aminopeptidase N. PL265 can effectively protect and significantly increase the local concentration of enkephalins (such as Met-Enkephalin and Leu-Enkephalin) released by cells at the pain or inflammation sites, thereby activating μ and δ opioid receptors to produce a potent analgesic effect. PL254 can also inhibit leukotriene A4 hydrolase (LTA4H), which may contribute to its additional anti-inflammatory effect by reducing the production of pro-inflammatory mediator leukotriene B4 (LTB4) . PL265 can be used in non-addictive chronic pain research[1].

Product Specifications

CAS Number

[1206514-50-2]

UNSPSC

12352005

Target

Endogenous Metabolite; Leukotriene Receptor; Opioid Receptor

Related Pathways

GPCR/G Protein; Metabolic Enzyme/Protease; Neuronal Signaling

Field of Research

Inflammation/Immunology; Neurological Disease

Smiles

CC(C)C(OC(C)OC(N[C@@H](C)P(C[C@@H](CC1=CC=C(C2=CC=CC=C2)C=C1)C(N[C@@H](C)C(O)=O)=O)(O)=O)=O)=O

Molecular Formula

C28H37N2O9P

Molecular Weight

576.58

References & Citations

[1]Bonnard E, et al. Long-lasting oral analgesic effects of N-protected aminophosphinic dual ENKephalinase inhibitors (DENKIs) in peripherally controlled pain. Pharmacol Res Perspect. 2015 Mar;3 (2) :e00116. |[2]Reaux-Le Goazigo A, et al. Dual enkephalinase inhibitor PL265: a novel topical treatment to alleviate corneal pain and inflammation. Pain. 2019 Feb 1;160 (2) :307-21.