Selective and Potent Peptide Agonist for Protease-Activated Receptor 2 (PAR2) Now Available from Peptides International

Protease-Activated Receptor Activating Peptides
(PAR-AP)
Peptide Agonist and Antagonist for PAR
Now Available from Peptides International

Proteinase-activated receptor (PAR) is a unique member of the G protein-coupled receptor (GPCR) family that is activated primarily by proteases. Protease cleavage exposes a tethered ligand at the N-terminus that binds to a conserved region in the second extracellular loop, leading to intracellular signaling. Recent findings suggest a complete shift in thinking regarding the roles of proteases as signaling molecules that can act as agonists or antagonists.¹

There are currently 4 known PARs: PAR₁ PAR_3,and PAR₄, which are activated primarily by thrombin, and PAR₂ activated by trypsin. The importance of these receptors is indicated by their diverse participation in a number of physiological responses. PARs have been reported to relax tracheal and bronchial smooth muscle cells, participate in platelet regulation, increase survival of neurons during HIV infection, play a role in skin pigmentation and arthritis, and participate in hypotension, arterial vasodilation in diabetes, gastric secretions, and leukocyte rolling and adhesion in the cardiovascular system.^2-7 PAR participation in tissue repair, cell survival, and inflammation following injury indicates that it may play an important role in controlling inflammatory-mediated diseases as well. In addition, PAR₁ and PAR₂ are expressed by a wide number of tumor cells including breast and colon cancers, suggesting a role in angiogenesis.^9,10 For these and other diseases where PAR plays a central role, the receptor may act as a potential therapeutic target.

PAR-activating peptides (PAR-APs) are short synthetic peptides that mimic the tethered ligand domains of PARs. They have been a popular alternative for PAR activation because they stimulate receptors in a protease-independent manner, avoiding activation of non-PAR related responses associated with the use of proteases. PAR-APs have been used successfully to determine important amino acid residues in the tethered ligand sequence and for in vivo and in vitro structure/function studies. Peptides International offers a variety of PAR-AP agonists and antagonists for your research needs.

NEW PAR peptides are now available and included in our brochure please download the latest version: NEW PAR Peptides PDF
CODE	Proteinase-Activated Receptor Activating Peptides (PAR-AP)	QTY	USD
PAR-3676-PI	H-Ser-Phe-Leu-Leu-Arg-Asn-NH₂ SFLLRN-Amide Selective Protease-Activated Receptor 1 (PAR1) Agonist	1 mg 5 mg	45 179
PAR-3665-PI	H-Thr-Phe-Leu-Leu-Arg-NH₂ TFLLR-Amide TFLLR -NH₂ Protease-Activated Receptor 1 (PAR₁) Agonist	1 mg 5 mg	65 195
PAR-3695-PI	H-Arg-Leu-Leu-Phe-Thr-NH₂ RLLFT-Amide PAR1 Inactive or Negative Control Peptide	1 mg 5 mg	65 195
PAR-3925-PI	H-Thr-Phe-Leu-Leu-Arg-Asn-Pro-Asn-Asp-Lys-NH₂ TFLLRNPNDK-Amide PAR1 Agonist	1 mg 5 mg	59 225
PAR-3926-PI	H-Phe-Thr-Leu-Leu-Arg-Asn-Pro-Asn-Asp-Lys-NH₂ FTLLRNPNDK-Amide Control Peptide for PAR1 Agonist	1 mg 5 mg	59 225
PAR-3913-PI	H-Leu-Ser-Ile-Gly-Arg-Leu-NH₂ LSIGRL-Amide Protease-Activated Receptor 2 (PAR2) Control Peptide of PAR-3664-PI	1 mg 5 mg	45 179
PAR-3888-PI	H-Phe-Ser-Leu-Leu-Arg-Tyr-NH₂ FSLLRY-Amide Selective PAR₂ Antagonist	1 mg 5 mg	35 139
PAR-3906-PI	H-Tyr-Arg-Leu-Leu-Ser-Phe-NH₂ YRLLSF-Amide Protease-Activated Receptor 2 (PAR2) Negative Control Peptide of PAR-3888-PI	1 mg 5 mg	35 139
PAR-3920-PI	H-Leu-Ser-Ile-Gly-Lys-Val-NH₂ LSIGKV-Amide Protease-Activated Receptor 2 (PAR2) Negative Control Peptide	1 mg 5 mg	45 179
PAR-3889-PI	H-Ser-Leu-Ile-Gly-Lys-Val-NH₂ SLIGKV-Amide PAR₂ Tethered Ligand (Human) / PAR₂ Agonist	1 mg 5 mg	35 139
PAR-3896-PI	H-Val-Lys-Gly-Ile-Leu-Ser-NH₂ VKGILS-Amide Negative Control of PAR2 Agonist PAR-3889-PI	1 mg 5 mg	35 139
PAR-3689-PI	H-Thr-Phe-Arg-Gly-Ala-Pro-NH₂ TFRGAP-Amide PAR₃ Tethered Ligand (Human) / Activates PAR₁ and PAR₂	1 mg 5 mg	45 179
PAR-3691-PI	H-Ser-Phe-Asn-Gly-Gly-Pro-NH₂ SFNGGP-Amide PAR₃ Tethered Ligand (Murine) / Activates PAR₁ and PAR₂	1 mg 5 mg	45 179
PAR-3676-PI	H-Ser-Phe-Leu-Leu-Arg-Asn-NH₂ SFLLRN-Amide Selective Protease-Activated Receptor 1 (PAR1) Agonist	1 mg 5 mg	45 179
PAR-3665-PI	H-Thr-Phe-Leu-Leu-Arg-NH₂ TFLLR-Amide TFLLR -NH₂ Protease-Activated Receptor 1 (PAR₁) Agonist	1 mg 5 mg	65 195
PAR-3695-PI	H-Arg-Leu-Leu-Phe-Thr-NH₂ RLLFT-Amide PAR1 Inactive or Negative Control Peptide	1 mg 5 mg	65 195
PAR-3663-PI	2-Furoyl-Leu-Ile-Gly-Arg-Leu-Orn-NH₂ 2-Furoyl-LIGRLO-Amide Potent and Selective Protease-Activated Receptor 2 (PAR₂) Agonist	1 mg 5 mg	75 215
PAR-3664-PI	H-Ser-Leu-Ile-Gly-Arg-Leu-NH₂ SLIGRL-Amide SLIGRL-NH₂ Protease-Activated Receptor 2 (PAR₂) Agonist	1 mg 5 mg	65 195
PAR-3677-PI	3-Mercaptopropionyl-Phe-Cha-Cha-Arg- Lys-Pro-Asn-Asp-Lys-NH₂ Protease-Activated Receptor 1 (PAR1) Antagonist / Protease-Activated Receptor 2 (PAR2) Agonist	1 mg 5 mg	115 460
PAR-3672-PI	H-Gly-Tyr-Pro-Gly-Lys-Phe-NH₂ GYPGKF-Amide Selective Protease-Activated Receptor 4 (PAR4) Agonist	1 mg 5 mg	45 179
PAR-3673-PI	H-Gly-Tyr-Pro-Gly-Gln-Val-NH₂ GYPGQV-Amide Selective Protease-Activated Receptor 4 (PAR4) Agonist	1 mg 5 mg	45 179
PAR-3674-PI	H-Ala-Tyr-Pro-Gly-Lys-Phe-NH₂ AYPGKF-Amide Selective Protease-Activated Receptor 4 (PAR4) Agonist	1 mg 5 mg	45 179
PAR-3675-PI	trans-Cinnamoyl-Tyr-Pro-Gly-Lys-Phe-NH₂ trans-cinnamoyl-YPGKF-Amide Selective Protease-Activated Receptor 4 (PAR4) Antagonist	1 mg 5 mg	65 195

1. M.D. Hollenberg and S.J. Compton, Pharm. Rev., 54, 203 (2002). (Review)

2. A. Kawabata, S. Kubo, T. Ishiki, N. Kawao, F. Sekiguchi, R. Kuroda, M.D. Hollenberg, T. Kanke, and N. Saito, J. Pharmacol. Exp. Ther., 311,402 (2004).

3. C.K. Derian, B.P. Damiano, M.F. Addo, A.L. Darrow, M.R. D'Andrea, M. Nedelman, H.C. Zhang, B.E. Maryanoff, and P. Andrade-Gordon, J. Pharmacol. Ex.p Ther., 304, 855 (2003).

4. F. Noorbakhsh, N. Ergnolle, J.C. McArthur, C. Silva, M. Vodjgani, P. Andrade-Gordon, M.D. Hollenberg, and C. Power, J. Immunol., 174, 7320 (2005).

5. M. Seiberg, C. Paine, E. Sharlow, P. Andrade-Gordon, M. Costanzo, M. Eisinger, and S.S. Shapiro, Exp. Cell. Res., 254, 25 (2000).

6. W.R. Ferrell, J.C. Lockhart, E.B. Kelso, L. Dunning, R. Plevin, S.E. Meek, A.J.H. Smith, G.D. Hunter, J.S. McLean, F. McGarry, R. Ramage, L. Jiang, T. Kanke, and J. Kawagoe, J. Clin. Invest., 111, 35 (2003).

7. F. Roviezzo, M. Bucci, V. Brancaleone, A. Di Lorenzo, P. Geppetti, S. Farneti, L. Parente, G. Jungarella, S. Fiorucci, and G. Cirino, Arteriosclerosis, Thrombosis, and Vasc. Biol., 25, 2349 (2005).

8. N. Vergnolle, C.K. Derian, M.R. D’Andrea, M. Steinhoff, and P.l. Andrade-Gorden, J. of Immun., 169, 1467 (2002).

9. D. Darmoul, V. Gratio, H. Devaud, T. Lehy, and M. Laburthe, Am. J. Patho., 162, 1503 (2003).

10. S. Even-Ram , B. Uziely , P. Cohen , S. Grisaru-Granovsky , M. Maoz , Y. Ginzburg , R. Reich R, I. Vlodavsky I, and R. Bar-Shavit, Nat. Med., 4, 909 (1998).

NEW PAR peptides are now available and included in our brochure
please download latest version NEW PAR Peptides PDF

Proteinase-Activated Receptor (PAR) Peptides

Proteinase-activated receptors	PAR₁	PAR₂	PAR₃	PAR₄
Alternate designators	Thrombin receptor	Trypsin receptor	Thrombin receptor	Thrombin receptor
Tethered ligand sequences	SFLLR (h), SFFLR (m,r)	SLIGKV (h), SLIGRL (m,r)	TFRGAP (h), See product listing PAR-3689-PI SFNGGP (m) See product listing PAR-3691-PI	GYPGQV (h), GYPGKF (m)
Subtype selective peptide agonists	SFLLRN-NH₂ (PAR-3676-PI), TFRIFD, TFLLR-NH₂(PAR-3665-PI)	SLIGKV-NH₂ (PAR-3889-PI), SLIGRL-NH₂(PAR-3664-PI), trans-cinnamoyl- LIGRLO-NH₂, 2-Furoyl- LIGRLO-Amide (PAR-3663-PI)	None reported	GYPGKF-NH₂(PAR-3672-PI) GYPGQV-NH₂(PAR-3673-PI) AYPGKF-NH₂(PAR-3674-PI)
Antagonists	4 Reported Mercaptopropionyl- Phe-Cha-Cha-Arg-Lys- Pro-Asn-Asp-Lys-NH₂(PAR-3677-PI) trans-cinnamoyl- parafluoro-Phe- paraguanidino-Phe- Leu-Arg-Arg-NH_2, and Non-peptide antagonists: RWJ56110 and RWJ58259	FSLLRY-Amide (PAR-3888-PI)	None reported	1 Reported trans-cinnamoyl- YPGKF-NH₂(PAR-3675-PI)

h=human, m=mouse, r=rat
Summarized from PAR review by Morley D. Hollenberg and Steven J. Compton
M.D. Hollenberg and S.J. Compton, Pharm. Rev., 54, 203 (2002). Review

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PO Box 24658
Louisville, Kentucky 40224 USA
Phone: 502-266-8787 or 800-777-4779
Fax: 502-267-1FAX (1329)
Email: peptides@pepnet.com

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