Formulation: A solid
Formal Name: N-(1-oxohexadecyl)-L-serylglycyl-L-arginyl-L-arginyl-L-tyrosylglycyl-L-histidyl-L-alanyl-L-leucyl-L-argininamide, trifluoroacetate salt
Purity: ≥98%
Formula Markup: C65H112N22O13 • XCF3COOH
Formula Weight: 1409,7
Shelf life (days): 1460
Notes: P4pal10 is a pepducin antagonist of proteinase-activated receptor 4 (PAR4) and formyl peptide receptor 2 (FPR2), as well as an agonist of free fatty acid receptor 2 (FFAR2/GPR43).{21094,66196} It is composed of a peptide that corresponds to the third intracellular loop of human PAR4 that is conjugated to palmitic acid (Item No. 10006627).{21094} P4pal10 selectively inhibits the aggregation of isolated human platelets induced by the PAR4 peptide agonist AYPGKF-NH2 (Item No. 24258; IC50 = 0.5-1 µM) over the PAR1 peptide agonist SFLLRN-NH2 (Item No. 36881), the TP receptor agonist U-46619 (Item No. 16450), the platelet glycoprotein Ib (GPIb), GPIX, and GPV agonist ristocetin, ADP (Item No. 21121), or collagen at 5 µM. It inhibits increases in intracellular calcium induced by the FPR1 and FPR2 agonist WKYMVm but not by the FPR1 agonist fMLF in isolated human neutrophils and induces superoxide production in TNF-α primed isolated human neutrophils stimulated with the FFAR2 allosteric modulator Cmp58.{66196} P4pal10 (1, 3, or 10 µg/kg) reduces myocardial infarct size in a rat model of coronary artery ligation-induced ischemia-reperfusion injury.{67051} It increases the paw withdrawal threshold in rat models of osteoarthritis induced by monoiodoacetate injection into the knee joint or medial meniscal transection.{66197}
English
Deutsch
