P4pal10 TFA 

P4pal10 TFA is the TFA salt form of P4pal10 (HY-P5875). P4pal10 TFA is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 TFA inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 TFA reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 TFA ameliorates the injury in rats myocardial ischemia/reperfusion (I/R) models^[1][2][3].

1409.72 (free base)

C₆₅H₁₁₂N₂₂O₁₃.xC₂HF₃O₂

Solid

White to off-white

{Pal}-Ser-Gly-Arg-Arg-Tyr-Gly-His-Ala-Leu-Arg-NH2

{Pal}-SGRRYGHALR-NH2

OC(C=C1)=CC=C1C[C@@H](C(NCC(N[C@H](C(N[C@@H](C)C(N[C@@H](CC(C)C)C(N[C@H](C(N)=O)CCCNC(N)=N)=O)=O)=O)CC2=CN=CN2)=O)=O)NC([C@H](CCCNC(N)=N)NC([C@H](CCCNC(N)=N)NC(CNC([C@H](CO)NC(CCCCCCCCCCCCCCC)=O)=O)=O)=O)=O.OC(C(F)(F)F)=O.[x]

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [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.  [Content Brief]

  [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.  [Content Brief]

  [3]. Wielders SJ, et al., Anticoagulant and antithrombotic properties of intracellular protease-activated receptor antagonists. J Thromb Haemost. 2007 Mar;5(3):571-6.  [Content Brief]