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Products
Pharmacology
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- Technical support
- Resources
P2pal-18S
Cat. No. PR-120
Structure:
Palmitoyl-Arg-Ser-Ser-Ala-Met-Asp-Glu-Asn-Ser-Glu-Lys-Lys-Arg-Lys-Ser-Ala-Ile-Lys-NH2
Other Names:
P2pal-18S pepducin
Activity:
PAR2 antagonist
P2pal-18S is a cell-penetrating proteinase-activated receptor-2 (PAR2) antagonist, designed from a structural model of the PAR2 dimer. P2pal-18S is highly selective for PAR2 and has no antagonist activity at the closely related PAR1, PAR4, or CXCR1/2 IL-8 receptors in neutrophil chemotaxis assays. In vitro, P2pal-18S completely suppresses trypsin and mast cell tryptase signaling through PAR2 in neutrophils and colon cancer cells, and in vivo, it is highly efficacious in blocking PAR2-dependent inflammatory responses, preventing the development of neuroinflammatory disease in murine models of multiple sclerosis and experimental autoimmune encephalomyelitis (EAE).
Sevigny et al (2011) Interdicting protease-activated receptor-2-driven inflammation with cell-penetrating pepducins. Proc Natl Acad Sci U S A 108(20) 8491 PMID: 21536878
Michael et al (2013) Pharmacological inhibition of PAR2 with the pepducin P2pal-18S protects mice against acute experimental biliary pancreatitis. Am J Physiol Gastrointest Liver Physiol. 304(5) G516 PMID: 23275617
Eftekhari et al (2024)Blockade of Proteinase-Activated Receptor 2 (PAR2) Attenuates Neuroinflammation in Experimental Autoimmune Encephalomyelitis. J Pharmacol Exp Ther. 388(1) 12 PMID: 37699708
Related areas
All cell penetrating peptides >
All protease activated receptor modulators >
All immunology research categories >
Technical Data
| Structure | Palmitoyl-Arg-Ser-Ser-Ala-Met-Asp-Glu-Asn-Ser-Glu-Lys-Lys-Arg-Lys-Ser-Ala-Ile-Lys-NH2 |
| Molecular Weight | 2302.77 |
| Formula | C99H180N30O30S |
| Sequence | Palmitoyl-RSSAMDENSEKKRKSAIK-NH2 |
| Modifications | N terminal palmitoyl, C terminal amide |
Solubility and Storage
| Solubility | Soluble in DMSO |
| Appearance | Freeze dried solid |
| Storage | Store dry, frozen and in the dark |
Batch Specific Data
| Purity | >95% BPLC |
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Recent citations
A new publication from the University of Ljubljana uses MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2, the FRET substrate for the severe acute respiratory syndrome coronavirus main protease (SARS-CoV Mpro), to determine the inhibitory potential of plant polyphenols
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