MedKoo Cat#: 532473 | Name: PL265

Description:

WARNING: This product is for research use only, not for human or veterinary use.

PL265 is a dual enkephalinase inhibitor with analgesic potential. Studies demonstrate the ability of PL265 to prevent the degradation of endogenous ENKs, and to counteract cancer-induced bone thermal hyperalgesia in mice. Chronic PL265 topical administration also decreased Iba1 and neuronal injury marker (ATF3) staining in the nucleus of primary sensory neurons of ipsilateral trigeminal ganglion. PL265 was shown to be safe and well-tolerated and inhibited both of its target enzymes, aminopeptidase N (APN) and neprilysin (NEP), which are responsible for the degradation of enkephalins

Chemical Structure

PL265
PL265
CAS#1206514-62-6

Theoretical Analysis

MedKoo Cat#: 532473

Name: PL265

CAS#: 1206514-62-6

Chemical Formula: C27H35N2O9P

Exact Mass: 562.2080

Molecular Weight: 562.56

Elemental Analysis: C, 57.65; H, 6.27; N, 4.98; O, 25.60; P, 5.51

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
Synonym
PL265; PL 265; PL-265.
IUPAC/Chemical Name
(2S)-2-[[(2S)-2-[[hydroxy-[(1R)-1-(2-methylpropanoyloxymethoxycarbonylamino)ethyl]phosphoryl]methyl]-3-(4-phenylphenyl)propanoyl]amino]propanoic acid
InChi Key
HLACXNCYLIKGES-YCRNBWNJSA-N
InChi Code
InChI=1S/C27H35N2O9P/c1-17(2)26(33)37-16-38-27(34)29-19(4)39(35,36)15-23(24(30)28-18(3)25(31)32)14-20-10-12-22(13-11-20)21-8-6-5-7-9-21/h5-13,17-19,23H,14-16H2,1-4H3,(H,28,30)(H,29,34)(H,31,32)(H,35,36)/t18-,19+,23+/m0/s1
SMILES Code
C[C@H](NC([C@@H](CP([C@@H](NC(OCOC(C(C)C)=O)=O)C)(O)=O)CC1=CC=C(C2=CC=CC=C2)C=C1)=O)C(O)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
PL265 is a Dual ENKephalinase Inhibitor (DENKI), a small molecule with only one active metabolite (PL254) which acts by inhibiting the enkephalin-degrading enzymes APN (aminopeptidase N) and NEP (neprilysin), thereby increasing the local concentration of enkephalins triggering a local and sustainable pain relief.

Preparing Stock Solutions

The following data is based on the product molecular weight 562.56 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Bonnard E, Poras H, Fournié-Zaluski MC, Roques BP. Preventive and alleviative effects of the dual enkephalinase inhibitor (Denki) PL265 in a murine model of neuropathic pain. Eur J Pharmacol. 2016 Oct 5;788:176-82. doi: 10.1016/j.ejphar.2016.05.041. Epub 2016 Jun 4. PubMed PMID: 27266667.