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7-Transmembrane receptors
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P4pal10
P4pal10
Cat. No. PR-100
Structure:
Pal-Ser-Gly-Arg-Arg-Tyr-Gly-His-Ala-Leu-Arg-NH2
Other Names:
Pepducin P4Pal10, palmitoyl-SGRRYGHALR-amide, P4pal-10
Activity:
PAR4 antagonist
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.
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
Related data
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Technical Data
| Structure | Pal-Ser-Gly-Arg-Arg-Tyr-Gly-His-Ala-Leu-Arg-NH2 |
| CAS Number | 1021346-05-3 |
| Molecular Weight | 1409.72 |
| Formula | C65H112N22O13 |
| Sequence | Pal-SGRRYGHALR-NH2 |
| Modifications | C terminal palmitoylation, N terminal amide |
Solubility and Storage
| Solubility | Soluble in DMSO |
| Appearance | Freeze dried solid |
| Storage | Store dry, frozen and in the dark |
Batch Specific Data
| Purity | >95% by hplc |
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Recent citations
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