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Protease-Activated Receptors
More Information »Protease-activated receptors (PARs, also known as thrombin receptors) are G-protein-coupled receptors, activated by cleavage of their N-terminal domains by serine proteases. Hydrolysis reveals a tethered peptide ligand, which affects transmembrane signaling.
Protease-Activated Receptor Products
Agonists |
|
Cat.No. |
Product Name / Activity |
| 3370 | AC 264613 |
| PAR2 receptor agonist | |
| 3369 | AC 55541 |
| Potent and selective PAR2 agonist | |
| 1487 | AY-NH2 |
| Selective PAR4 agonist | |
| 3015 | 2-Furoyl-LIGRLO-amide |
| Potent and selective PAR2 agonist | |
| 3394 | LRGILS-NH2 |
| Control peptide for SLIGRL-NH2 (Cat. No. 1468) | |
| 3494 | PAR 4 (1-6) |
| PAR4 peptide fragment; acts as a PAR4 agonist | |
| 3393 | RLLFT-NH2 |
| Control peptide for TFLLR-NH2 (Cat. No. 1464) | |
| 3010 | SLIGKV-NH2 |
| PAR2 receptor agonist | |
| 1468 | SLIGRL-NH2 |
| PAR2-activating peptide | |
| 1464 | TFLLR-NH2 |
| PAR1-activating peptide | |
| 1185 | Thrombin Receptor Agonist Peptide |
| Causes platelet aggregation and secretion | |
| 3497 | TRAP-6 |
| PAR1 peptide fragment (residues 42-47); acts as a PAR1 agonist | |
| 3392 | VKGILS-NH2 |
| Control peptide for SLIGKV-NH2 (Cat. No. 3010) | |
Antagonists |
|
Cat.No. |
Product Name / Activity |
| 3643 | FR 171113 |
| PAR1 antagonist | |
| 4751 |
FSLLRY-NH2
|
| PAR2 peptide antagonist | |
| 2614 | RWJ 56110 |
| Selective PAR1 antagonist | |
| 1592 | SCH 79797 dihydrochloride |
| Potent, selective non-peptide PAR1 antagonist | |
| 1488 | tcY-NH2 |
| Selective PAR4 antagonist | |
Modulators |
|
Cat.No. |
Product Name / Activity |
| 4755 |
Q94 hydrochloride
|
| Negative allosteric modulator at PAR1 receptor | |
Inhibitors |
|
Cat.No. |
Product Name / Activity |
| 2511 | APC 366 |
| Tryptase inhibitor | |
| 1798 | Gabexate mesylate |
| Serine protease inhibitor; inhibits thrombin, trypsin, kallikrein and plasmin | |
| 4570 | ML 161 |
| Inhibits PAR1-mediated platelet activation | |
Other |
|
Cat.No. |
Product Name / Activity |
| 3553 | Parstatin (human) |
| Peptide cleaved from PAR1 upon receptor activation | |
| 3554 | Parstatin (mouse) |
| Peptide cleaved from PAR1 upon receptor activation | |
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Cardiovascular Guide
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Regulation of Vascular Reactivity by GPCRs
Written by J.J. Maguire and A.P. Davenport
'Regulation of Vascular Reactivity by G-protein-coupled Receptors' summarizes the key GPCRs regulating vascular reactivity.
7-TM Receptor Signaling
Written by T. Kenakin et al
'Seven Transmembrane Receptor Signaling' highlights the multiple behaviors of 7-TMs including G-protein-dependent and -independent signaling as well as the concept of collateral efficacy
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