| Identification | Back Directory | [Name]
L-Argininamide, N-(1-oxohexadecyl)-L-serylglycyl-L-arginyl-L-arginyl-L-tyrosylglycyl-L-histidyl-L-alanyl-L-leucyl- | [CAS]
1021346-05-3 | [Synonyms]
P4pal10
L-Argininamide, N-(1-oxohexadecyl)-L-serylglycyl-L-arginyl-L-arginyl-L-tyrosylglycyl-L-histidyl-L-alanyl-L-leucyl- | [Molecular Formula]
C65H112N22O13 | [MOL File]
1021346-05-3.mol | [Molecular Weight]
1409.72 |
| Hazard Information | Back Directory | [Uses]
P4pal10 is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 ameliorates the injury in mice myocardial ischemia/reperfusion (I/R) models[1][2][3]. | [Biological Activity]
PAR4antagonist which shows no agonist activity (as measured by platelet aggregation, intracellular Ca2+release or InsP production). Also inhibits Gαi-coupled formylpeptide FPR2 receptor downstream signaling but does not inhibit downstream signaling of the Gαq-coupled P2Y2 and PAF receptors. Additionally activates the FFAR2 short chain fatty acid receptor. Inhibits platelet aggregation and shows cardioprotective effects by decreasing infarct size before ischemia. | [IC 50]
PAR4 | [storage]
-20°C | [References]
[1] Houle S, et al. Neutrophils and the kallikrein-kinin system in proteinase-activated receptor 4-mediated inflammation in rodents. Br J Pharmacol. 2005 Nov;146(5):670-8. DOI:10.1038/sj.bjp.0706371
[2] Strande JL, et al., Inhibiting protease-activated receptor 4 limits myocardial ischemia/reperfusion injury in rat hearts by unmasking adenosine signaling. J Pharmacol Exp Ther. 2008 Mar;324(3):1045-54. DOI:10.1124/jpet.107.133595
[3] Wielders SJ, et al., Anticoagulant and antithrombotic properties of intracellular protease-activated receptor antagonists. J Thromb Haemost. 2007 Mar;5(3):571-6. DOI:10.1111/j.1538-7836.2007.02364.x |
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