PL37

CAT: 0804-HY-19876Size: 1 EachDry Ice: NoHazardous: No

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CAT#:0804-HY-19876Size:1 Each

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Description

PL37 (Debio-0827) is an orally active Enkephalinase dual inhibitor (dual inhibition refers to the simultaneous inhibition of Neutral Endopeptidase and Aminopeptidase N activities) . PL37 exerts its anti-hyperalgesic effects by activating μ-opioid receptors (µ-opioid receptors), with an ED50 value of 13.4 mg/kg for analgesic effects in mice. PL37 can be used to study diabetic neuropathic pain[1][2][3][4].

CAS Number

935481-06-4

Product Name Alternative

Debio-0827

UNSPSC

12352005

Target

Aminopeptidase; Neprilysin; Opioid Receptor

Type

Reference compound

Related Pathways

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

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/pl37.html

Smiles

CSCC[C@H](N)CSSC[C@@H](CC1=CC=CC=C1)C(NCC(OC(C)OC(OCC)=O)=O)=O

Molecular Formula

C22H34N2O6S3

Molecular Weight

518.71

References & Citations

[1]Menéndez L, et al. Inhibition of osteosarcoma-induced thermal hyperalgesia in mice by the orally active dual enkephalinase inhibitor PL37. Potentiation by gabapentin. Eur J Pharmacol. 2008 Oct 31;596 (1-3) :50-5. |[2]Tesfaye S. PL37: a new hope in the treatment of painful diabetic neuropathy?[J]. Pain Management, 2016, 6 (2) : 129-132.|[3]González-Rodríguez S, et al. Involvement of enkephalins in the inhibition of osteosarcoma-induced thermal hyperalgesia evoked by the blockade of peripheral P2X3 receptors. Neurosci Lett. 2009 Nov 20;465 (3) :285-9.|[4]Descheemaeker A, et al. Dual enkephalinase inhibitor PL37 as a potential novel treatment of migraine: evidence from a rat model. Brain. 2022 Aug 27;145 (8) :2664-2670.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

Phase 1

PL37

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