2. Signaling Pathways
  3. GPCR/G Protein
  4. Protease Activated Receptor (PAR)
  5. Protease Activated Receptor (PAR) Inhibitor

Protease Activated Receptor (PAR) Inhibitor

Protease Activated Receptor (PAR) Isoform Comparison

Protease Activated Receptor (PAR) Inhibitors (12):

Cat. No. Product Name Effect Purity
  • HY-120261
    GB-88
    		Inhibitor 99.05%
    GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 μM.
  • HY-13965
    Parmodulin 2
    		Inhibitor 99.82%
    Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.
  • HY-P1260
    FSLLRY-NH2
    		Inhibitor 98.52%
    FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.
  • HY-P1260A
    FSLLRY-NH2 TFA
    		Inhibitor 99.43%
    FSLLRY-NH2 TFA is a protease-activated receptor 2 (PAR2) inhibitor.
  • HY-138558
    PAR-2-IN-1
    		Inhibitor 99.79%
    PAR-2-IN-1 is a protease-activated receptor-2 (PAR2) signaling pathway inhibitor with anti-inflammatory and anticancer effects.
  • HY-148016
    I-287
    		Inhibitor 99.36%
    I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gαq and Gα12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in mice and can be used for inflammation/immunology research.
  • HY-108556A
    RWJ-56110 dihydrochloride
    		Inhibitor 99.54%
    RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by?both?SFLLRN-NH2?(IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective?relative to U46619 (HY-108566). RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.
  • HY-162409
    PAR4 antagonist 4
    		Inhibitor
    PAR4 antagonist 4 (Compound 37) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 14.2 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 42.5 min.
  • HY-124663
    CBK289001
    		Inhibitor
    CBK289001 is a tartrate-resistant acid phosphatase (TRAP/ACP5) inhibitor. CBK289001 inhibits TRAP 5bMV, TRAP 5bOX and TRAP 5aOX with IC50s of 125 µM, 4.21 µM and 14.2 µM, respectively.
  • HY-162408
    PAR4 antagonist 3
    		Inhibitor
    PAR4 antagonist 3 (Compound 36) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 26.1 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 97.6 min.
  • HY-108556
    RWJ-56110
    		Inhibitor
    RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by?both?SFLLRN-NH2?(IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective?relative to U46619 (HY-108566). RWJ-56110 inhibits angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 induces cell apoptosis.
  • HY-146333
    TRAP-6-IN-1
    		Inhibitor
    TRAP-6-IN-1 (Compound 8) is a dual collagen and TRAP-6 inhibitor with IC50 values of 17.12 µM and 11.88 µM against collagen and TRAP-6, respectively. TRAP-6-IN-1 inhibits agonist-induced platelet aggregation in a non-competitive manner.