P4pal10 peptide

P4pal10 peptide

• Handling and Storage of Synthetic Peptides
• Material Safety Data Sheets (MSDS)

Palmitolyl-SGRRYGHALR-NH2

Palmitolyl-Ser-Gly-Arg-Arg-Tyr-Gly-His-Ala-Leu-Arg-NH2

10

95.28%

C₆₅H₁₁₂N₂₂O₁₃

1409.72

Synthetic

Powder

P4pal10 is a pepducin with a peptide sequence identical to part of the third intracellular loop of the protease activated receptor 4 (PAR4) which acts as a PAR4 antagonist. P4pal10 has no agonist activity as measured by platelet aggregation, intracellular Ca2+ release or InsP production, but preincubation of human platelets with P4pal10 completely blocks aggregation in response to PAR4 activators. Infusion of P4Pal10 into mice extends bleeding time and protects against systemic platelet activation, and in rat models of myocardial injury, P4pal10 treatment before ischemia significantly decreases infarct size when given before, during, and after ischemia. P4Pal10 also inhibits signaling downstream of the Gαi-coupled FPR2.

Normally, this peptide will be delivered in lyophilized form and should be stored in a freezer at or below -20 °C. For more details, please refer to the manual:Handling and Storage of Synthetic Peptides

• Covic et al (2002) Pepducin-based intervention of thrombin-receptor signaling and systemic platelet activation. Nat Med. 8(10) 1161 PMID: 12357249
• Strande et al (2008) Inhibiting protease-activated receptor 4 limits myocardial ischemia/reperfusion injury in rat hearts by unmasking adenosine signaling. J Pharmacol Exp Ther. 324(3) 1045 PMID: 18055876
• Holdfeldt et al (2020) The PAR4-derived pepducin P4Pal10 lacks effect on neutrophil GPCRs that couple to Gαq for signaling but distinctly modulates function of the Gαi-coupled FPR2 and FFAR2. Biochem Pharmacol. 180 114143 PMID: 32653592

Trifluoroacetic acid (TFA) has a significant impact on peptides due to its role in the peptide synthesis process.

TFA is essential for the protonation of peptides that lack basic amino acids such as Arginine (Arg), Histidine (His), and Lysine (Lys), or ones that have blocked N-termini. As a result, peptides often contain TFA salts in the final product.

TFA residues, when present in custom peptides, can cause unpredictable fluctuations in experimental data. At a nanomolar (nM) level, TFA can influence cell experiments, hindering cell growth at low concentrations (as low as 10 nM) and promoting it at higher doses (0.5–7.0 mM). It can also serve as an allosteric regulator on the GlyR of glycine receptors, thereby increasing receptor activity at lower glycine concentrations.

In an in vivo setting, TFA can trifluoroacetylate amino groups in proteins and phospholipids, inducing potentially unwanted antibody responses. Moreover, TFA can impact structure studies as it affects spectrum absorption.