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Protease-activated Receptor

Protease-activated receptors (PAR) are a subfamily of related G protein-coupled receptors that are activated by cleavage of part of their extracellular domain. They are highly expressed in platelets, and also on endothelial cells, myocytes and neurons.

Vorapaxar
T7013618385-01-6
Vorapaxar (MK-5348) (SCH 530348) is an effective and orally active thrombin receptor (PAR-1) antagonist (Ki: 8.1 nM).
  • $68
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AY 77
T411901835734-92-3In house
AY 77 (Unk-Cha-Chg-NH2) is a potent and selective PAR2 agonist. AY 77 showed selectivity for Ca2+ and ERK1/2 signaling (ec50 value of Ca2+ release was 40 nM and ec50 value of ERK1/2 phosphorylation was 2 μM). AY 77 can promote migration of human breast cancer cells in vitro.
  • $412
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Vorapaxar sulfate
T3098705260-08-8
Vorapaxar sulfate (Zontivity) is a potent and orally active thrombin receptor (PAR-1) antagonist.
  • $32
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ENMD-1068 HCl
T27267789488-77-3
ENMD-1068 HCl (ENMD 1068) is a PAR-2 antagonist. ENMD-1068 HCl inhibits the development of endometriosis in a mouse model.
  • $50
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TRAP-6
T7625141136-83-6
TRAP-6 (Thrombin Receptor Activator Peptide 6)(2TFA) is an agonist of protease-activated receptor 1 (PAR1).
  • $34
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2-Furoyl-LIGRLO-amide TFA(729589-58-6 free base)
TP1378
2-Furoyl-LIGRLO-amide TFA(729589-58-6 free base) is a potent and selective protease-activated receptor 2 (PAR2) agonist.
  • $50
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PAR-2 Activating Peptide acetate
TP1046L
PAR-2 Activating Peptide acetate (SLIGRL-NH2 acetate) is an agonist of Protease-Activated Receptor-2 (PAR-2).
  • $78
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Trypsin
TN68729002-07-7
Trypsin is a serine protease that can be isolated from fish to hydrolyze lysine or arginine carboxy-side proteins. With the anti-inflammatory activity, Trypsin could induce the cell membrane fusion of PDCoV-infected cells through the interaction between the S glycoprotein of PDCoV and pAPN, activate PAR2 and PAR4, and promote cell proliferation and differentiation. Trypsin can be used to promote wound healing and study neurogenic inflammation.
  • $39
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I-191
T71371690172-25-8
I-191 is a potent antagonist of protease-activated receptor 2 (PAR2), inhibits multiple signaling functions in human cancer cells.
  • $82
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Protease-Activated Receptor-2, amide
T7513190383-13-2
Protease-Activated Receptor-2, amide (SLIGKV-NH2) is an agonist of PAR2 with an IC50 of 10.4 M.
  • $48
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PAR-4 Agonist Peptide, amide TFA
TP10651228078-65-6
PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA)), is a selective activator of the proteinase-activated receptor-4 (PAR-4) that does not affect PAR-1 or PAR-2, and its activity can be inhibited by a PAR-4 antagonist.
  • $30
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Protease-Activated Receptor-1, PAR-1 Agonist acetate
T38836L
Protease-Activated Receptor-1, PAR-1 Agonist acetate is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist acetate corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor[1][2].
  • $133
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AZ3451
TQ00122100284-59-9
AZ3451 is an allosteric antagonist of protease-activated receptor-2 (PAR2, IC50: 23 nM).
  • $38
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TFLLR-NH2 2TFA(197794-83-5(free base))
T7573L
TFLLR-NH2 2TFA(197794-83-5(free base)) is an agonist of PAR1 (EC50 :1.9 μM).
  • $133
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tcY-NH2 TFA(327177-34-4 free base)
TP1925L
tcY-NH2 TFA is a selective PAR4 antagonist peptide. Inhibits endostatin release and platelet aggregation induced by thrombin.
  • $106
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PAR-2-IN-1
T89171690176-75-0
PAR-2-IN-1 (IUN76750) is a PAR- 2 signaling pathway inhibitor with anti-inflammatory and anticancer effects.
  • $30
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LRGILS-NH2 acetate
T22933L
LRGILS-NH2 acetate is a PAR-2-inactive reversed peptide.
  • $35
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Atopaxar
T1986751475-53-3In house
Atopaxar (E5555), a reversible PAR-1 thrombin receptor antagonist, interferes with platelet signaling. Atopaxar has been investigated for the treatment of Coronary Artery Disease and Acute Coronary Syndrome.
  • $67
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FSLLRY-NH2 TFA(245329-02-6 free base)
TP1904L
FSLLRY-NH2 TFA is a is a protease-activated receptor 2 (PAR2) inhibitor. Reverses taxol-induced mechanical allodynia, heat hyperalgesia and PKC activation in ICR mice. Blocks ERK activation and collagen production in isolated cardiac fibroblasts. Also reduces symptoms in a mouse model of dermatophyte-associated itch.
  • $98
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Protease-Activated Receptor-4 diTFA
T7740
Protease-Activated Receptor-4 diTFA,2454 is the proteinase-activated receptor-4 (PAR4)agonist
  • $40
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SCH79797 dihydrochloride
T128701216720-69-2
SCH79797 dihydrochloride is an effective and selective antagonist of protease activated receptor 1 (PAR1) with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects.
  • $32
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Parmodulin 2
T1893423735-93-7
Parmodulin 2 (ML 161) is the inhibitor of protease-activated receptor 1 (PAR1)-mediated platelet activation (IC50: 0.26 μM for the inhibition of platelet P-selectin expression on human platelets). It also inhibits thrombin-induced platelet activation.
  • $30
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iso-TRAP-6
T78099150242-29-8
iso-TRAP-6 (iso-SFLLRN), a hexapeptide derived from the substitution of isoserine for serine, is a protease-activated receptor 1 (PAR1) agonist that activates platelets via PAR-1. iso-TRAP-6 is more resistant to degradation by plasma aminopeptidases than iso-TRAP-6.
  • $40
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Thrombin Receptor Activator for Peptide
T7674
Thrombin Receptor Activator for Peptide is also called Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), used in the research of coronary heart disease (CHD).
  • $39
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TRAP-6 amide acetate
T38852L
TRAP-6 amide acetate is a PAR-1 thrombin receptor agonist peptide[1].
  • $89
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BMS-986141
T639661478711-48-6In house
BMS-986141(UDM-003183) is a selective and potent protease-activated receptor-4 (PAR-4) antagonist with oral activity and an IC50 value of 0.4 nM.BMS-98614 exhibits significant antithrombotic effects.
  • $787
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VKGILS-NH2 Acetate
T21699L
VKGILS-NH2 Acetate is a reversed amino acid sequence control peptide for SLIGKV-NH2, a protease-activated receptor 2 (PAR2) agonist.
  • $29
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AC-55541
T2370916170-19-9
AC-55541 (AOB2796) is a novel PAR2 agonist; activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 200 to 1000 nM.
  • $29
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ML-354
T2190189159-60-4
ML-354 (VU0099704) is a selective and potent PAR4 antagonist for the study of cardiovascular disease.
  • $50
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SLIGRL-NH2
TP1046171436-38-7
SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) is a PAR-2 agonist that induces non-histaminergic pruritus.
  • $99
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PAR-4 Agonist Peptide, amide
T7623352017-71-1
PAR-4 Agonist Peptide, amide (AY-NH2), is an agonist of proteinase-activated receptor-4 (PAR-4).
  • $47
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Atopaxar Hydrobromide
T1986L474550-69-1
Atopaxar, a reversible PAR-1 thrombin receptor antagonist, interferes with platelet signaling. Atopaxar has been investigated for the treatment of Coronary Artery Disease and Acute Coronary Syndrome.
  • $257
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Protease-Activated Receptor-4
T7380245443-52-1
Protease-Activated Receptor-4 (PAR4) is a proteinase-activated receptor-4 agonist used in antiplatelet therapy.
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    Thrombin Receptor Activator for Peptide 5 (TRAP-5)
    T7496141685-53-2
    Thrombin Receptor Activator for Peptide 5 (TRAP-5), also known as Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), is utilized in coronary heart disease (CHD) research.
    • $71
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    TFLLR-NH2
    T7573197794-83-5
    TFLLR-NH2(2TFA) is an agonist of PAR1 (EC50 :1.9 μM).
    • $970
    35 days
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    PAR-4 Agonist Peptide, amide acetate
    T7623L
    PAR-4 Agonist Peptide, amide acetate is an agonist of proteinase-activated receptor-4 (PAR-4).
    • $98
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    AC-264613
    T41861051487-82-1
    AC-264613 is an agonist of the GPCR protease-activated receptor 2 (PAR2). AC-264613(AC264613) suppresses interferon regulatory factor 5 and decreases interleukin-12p40 production by lipopolysaccharide-stimulated macrophages. AC-264613(AC264613) activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 30 to 100 nM.
    • $93
    35 days
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