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Thrombin receptors

" in MedChemExpress (MCE) Product Catalog:

41

Inhibitors & Agonists

1

Biochemical Assay Reagents

22

Peptides

1

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P2518
    Protease-Activated Receptor-1, PAR-1 Agonist

    		Protease Activated Receptor (PAR) Inflammation/Immunology
    Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor .
    Protease-Activated Receptor-1, PAR-1 Agonist
  • HY-P0078
    TRAP-6
    4 Publications Verification

    PAR-1 agonist peptide; Thrombin Receptor Activator Peptide 6

    		 Protease Activated Receptor (PAR) Inflammation/Immunology
    TRAP-6 (PAR-1 agonist peptide), a peptide fragment, is a selective protease activating receptor 1 (PAR1) agonist. TRAP-6 activates human platelets via the thrombin receptor. TRAP-6 shows no activity at PAR4 .
    TRAP-6
  • HY-150790
    BMS-986141

    		Protease Activated Receptor (PAR) Cardiovascular Disease
    BMS-98614 is an orally active, selective thrombin receptor protease-activated receptor-4 (PAR-4) antagonist with an IC50 value of 0.4 nM. BMS-98614 has excellent antithrombotic effect .
    BMS-986141
  • HY-18200
    Atopaxar

    E5555; ER-172594-00

    		 Protease Activated Receptor (PAR) JAK Apoptosis Cardiovascular Disease Cancer
    Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar, an antiplatelet agent, interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease .
    Atopaxar
  • HY-P1000
    TRAP-14

    SFLLRNPNDKYEPF

    		 Thrombin Cardiovascular Disease
    TRAP-14 (SFLLRNPNDKYEPF) is a synthetic thrombin receptor agonist peptide.
    TRAP-14
  • HY-10119
    Vorapaxar
    Maximum Cited Publications
    10 Publications Verification

    SCH 530348

    		 Protease Activated Receptor (PAR) Cardiovascular Disease
    Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
    Vorapaxar
  • HY-18200B
    Atopaxar hydrobromide

    E5555 hydrobromide; ER 172594-06

    		 Protease Activated Receptor (PAR) JAK Apoptosis Cardiovascular Disease Cancer
    Atopaxar (E5555) hydrobromide is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar hydrobromide, an antiplatelet agent, interferes with platelet signaling. Atopaxar hydrobromide can be used for the research of atherothrombotic disease .
    Atopaxar hydrobromide
  • HY-18200A
    Atopaxar hydrochloride

    E5555 hydrochloride; ER-172594-00 hydrochloride

    		 Protease Activated Receptor (PAR) JAK Apoptosis Cardiovascular Disease Cancer
    Atopaxar hydrochloride (E5555 hydrochloride) is the hydrochloride salt form of Atopaxar (HY-18200). Atopaxar hydrochloride is an orally active, selective and reversible antagonist for thrombin receptor protease-activated receptor-1 (PAR-1). Atopaxar hydrochloride is the inhibitor for Janus kinase 1 (JAK1) and JAK2, which inhibits the JAK-STAT with EC50 of 5.90 μM in A549. Atopaxar hydrochloride inhibits the cell viability of A549 (IC50=7.02 μM), arrests the cell cycle at G1 phase and induces apoptosis. Atopaxar hydrochloride exhibits antiplatelet and antitumor activities. Atopaxar hydrochloride can be used for the research of atherothrombotic disease .
    Atopaxar hydrochloride
  • HY-P5889
    Thrombin receptor peptide ligand

    		Thrombin Cardiovascular Disease
    Thrombin receptor peptide ligand is a thrombin receptor antagonist peptide that can be used as an antithrombotic agent .
    Thrombin receptor peptide ligand
  • HY-114164B
    Human γ-Thrombin

    Human Gamma Thrombin

    		 Thrombin Cardiovascular Disease
    Human γ-Thrombin (Human Gamma Thrombin) is a variant of an enzyme that is further hydrolyzed from Thrombin. Human γ-Thrombin is produced by the hydrolysis of α-thrombin by factor X (fXa) or other plasma proteases such as hydrolases and plasmin, and can selectively activate platelets through specific receptors. Human γ-Thrombin can be used in the research of antithrombotic drugs .
    Human γ-Thrombin
  • HY-10119A
    Vorapaxar sulfate
    Maximum Cited Publications
    10 Publications Verification

    SCH 530348 sulfate

    		 Protease Activated Receptor (PAR) Cardiovascular Disease
    Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
    Vorapaxar sulfate
  • HY-P2321
    TRAP-6 amide

    		Protease Activated Receptor (PAR) Inflammation/Immunology
    TRAP-6 amide is a PAR-1 thrombin receptor agonist peptide .
    TRAP-6 amide
  • HY-P5371
    TFLLRNPNDK-NH2

    		Thrombin Others
    TFLLRNPNDK-NH2 is a biological active peptide. (This peptide is a thrombin receptor activating peptide. This PAR-1 agonist peptide reversibly binds to PAR-1 mimicking the 'tethered ligand' that thrombin makes available through proteolytic cleavage of substrate. It is also known to cause increase in liquid and protein permeability much like thrombin.)
    TFLLRNPNDK-NH2
  • HY-P2321A
    TRAP-6 amide TFA

    		Protease Activated Receptor (PAR) Inflammation/Immunology
    TRAP-6 amide TFA is a PAR-1 thrombin receptor agonist peptide .
    TRAP-6 amide TFA
  • HY-108555
    FR-171113

    		Protease Activated Receptor (PAR) Cardiovascular Disease
    FR171113 is a specific and non-peptide thrombin receptor antagonist. FR171113 exhibits the antithrombotic effects of a PAR1 antagonist. FR171113 inhibits thrombin-induced platelet aggregation with an IC50 of 0.29 μM. .
    FR-171113
  • HY-10119S
    Vorapaxar-d5

    SCH 530348-d5

    		 Protease Activated Receptor (PAR) Isotope-Labeled Compounds Cardiovascular Disease
    Vorapaxar-d5 is deuterated labeled Vorapaxar (HY-10119). Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
    Vorapaxar-d5
  • HY-10119R
    Vorapaxar (Standard)

    		Protease Activated Receptor (PAR) Cardiovascular Disease
    Vorapaxar (Standard) is the analytical standard of Vorapaxar. This product is intended for research and analytical applications. Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
    Vorapaxar (Standard)
  • HY-P1261
    Parstatin(mouse)

    		Protease Activated Receptor (PAR) Cardiovascular Disease Inflammation/Immunology
    Parstatin(mouse), a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis .
    Parstatin(mouse)
  • HY-P1262
    Parstatin(human)

    		Protease Activated Receptor (PAR) Cardiovascular Disease Inflammation/Immunology
    Parstatin(human), a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis .
    Parstatin(human)
  • HY-P1262A
    Parstatin(human) TFA

    		Protease Activated Receptor (PAR) Cardiovascular Disease Inflammation/Immunology
    Parstatin(human) TFA, a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis .
    Parstatin(human) TFA
  • HY-P1261A
    Parstatin(mouse) TFA

    		Protease Activated Receptor (PAR) Cardiovascular Disease Inflammation/Immunology
    Parstatin(mouse) TFA, a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis .
    Parstatin(mouse) TFA
  • HY-P1536
    Thrombin Receptor Activator for Peptide 5 (TRAP-5)

    		Protease Activated Receptor (PAR) Cardiovascular Disease
    Thrombin Receptor Activator for Peptide 5 (TRAP-5) 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).
    Thrombin Receptor Activator for Peptide 5 (TRAP-5)
  • HY-P0316
    TP508

    		Thrombin NO Synthase Cardiovascular Disease
    TP508 is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 activates endothelial cells and stem cells to revascularize and regenerate tissues .
    TP508
  • HY-P0316A
    TP508 TFA

    		Thrombin NO Synthase Cardiovascular Disease
    TP508 TFA is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 TFA activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 TFA activates endothelial cells and stem cells to revascularize and regenerate tissues .
    TP508 TFA
  • HY-P5372
    Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2

    		Protease Activated Receptor (PAR) Others
    Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biological active peptide. (Protease activated receptor 1 (PAR-1) belongs to a subfamily of G-protein coupled receptors and is known to mediate the cellular effects of thrombin. This peptide is a PAR-1 selective agonist displaying a high level of specificity to PAR-1 over PAR-2. The specificity of peptide was evaluated in cell-based calcium signaling assay using HEK293 cells. PAR-1 selective agonists can be used to study PAR-1 activation in vivo. In addition to its varied cellular effects of thrombin, PAR-1 has also been shown to coordinate with PAR-4 and regulate thrombin-induced hepatocellular carcinoma harboring thrombin formation within the tumor environment classified as 'coagulation type'.)
    Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2
  • HY-P2518A
    Protease-Activated Receptor-1, PAR-1 Agonist TFA

    		Protease Activated Receptor (PAR) Cancer
    Protease-Activated Receptor-1, PAR-1 Agonist TFA is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist TFA corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor .
    Protease-Activated Receptor-1, PAR-1 Agonist TFA
  • HY-14994
    SCH79797 dihydrochloride
    2 Publications Verification

    		 Protease Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
    SCH79797 dihydrochloride
  • HY-14993
    SCH79797
    2 Publications Verification

    		 Protease Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
    SCH79797
  • HY-P3267
    Transferrins
    1 Publications Verification

    		 Transferrin Receptor Others
    Transferrin, a blood-plasma glycoprotein, is a target ligand for transferrin receptor. Transferrins can bind to and mediate the transport of iron .
    Transferrins
  • HY-P4987
    TRAP-7

    		Protease Activated Receptor (PAR) Cardiovascular Disease
    TRAP-7 is a thrombin receptor (PAR) activating peptide. TRAP-7 stimulates total inositol phosphate (IP) accumulation and phosphorylation of a specific endogenous substrate for activated PKC. TRAP-7 can be used in cardiovascular disease research .
    TRAP-7
  • HY-P5357
    SFNGGP-NH2

    		Protease Activated Receptor (PAR) Others
    SFNGGP-NH2 is a biological active peptide. (PAR-3 is a high-affinity thrombin receptor. PAR-3 mRNA is expressed in the cutaneous mast cells of humans. Protease-Activated Receptors (PARs) have been studied for their roles in itch and their itch-associated response through histamine-dependent/independent pathways have been reported. PAR-3 has been shown not to induce itching alone but possibly in conjunction with PAR-4. Co-expression of PAR-3 and PAR-4 enhances thrombin action suggesting that PAR-3 alone does not mediate transmembrane signaling but instead functions as a cofactor to activate PAR-4.)
    SFNGGP-NH2
  • HY-W006069
    H-Phe(3,5-DiF)-OH

    		Protease Activated Receptor (PAR) Others
    H-Phe(3,5-DiF)-OH is a difluorophenylalanines in the L-configuration [L-(F2)Phe]. H-Phe(3,5-DiF)-OH can be incorporated into the thrombin receptor-tethered ligand peptide SFLLRNP to identify the phenyl hydrogens of the Phe-2 residue involved in the CH/π receptor interaction .
    H-Phe(3,5-DiF)-OH
  • HY-163341
    PAR4 antagonist 1

    		Protease Activated Receptor (PAR) Cardiovascular Disease
    PAR4 antagonist 1 (Compound 48) is a protease activated receptor 4 (PAR4) antagonist with an IC50 of 1.8 nM. PAR4 antagonist 1 has an IC50 of 2 nM against γ-thrombin-activated PAR4 in platelet-rich plasma (PRP). PAR4 antagonist 1 can be used in antithrombotic research .
    PAR4 antagonist 1
  • HY-161401
    PAR4 antagonist 2

    		Protease Activated Receptor (PAR) Cardiovascular Disease
    PAR4 antagonist 2 (Compound 31) is a protease activated receptor 4 (PAR4) antagonist, with IC50 values of 95 nM and 367 nM for human PAR4 and mouse PAR4. PAR4 antagonist 2 is active against PAR4 activation by the native protease thrombin cleavage but not the synthetic PAR4 agonist peptide AYPGKF .
    PAR4 antagonist 2
  • HY-128345
    UDM-001651

    		Protease Activated Receptor (PAR) Cardiovascular Disease
    UDM-001651 is a potent, selective, and orally bioavailable protease-activated receptor 4 (PAR4) antagonist (IC50=4 nM; Kd=1.4 nM). UDM-001651 shows antiplatelet potency (IC50=25 nM) in a γ-thrombin-induced platelet-rich plasma aggregation assay (γ-Thr PRP) .
    UDM-001651
  • HY-107613
    R 59-022
    1 Publications Verification

    DKGI-I; Diacylglycerol kinase inhibitor I

    		 PKC 5-HT Receptor Inflammation/Immunology
    R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils .
    R 59-022
  • HY-107613A
    R 59-022 hydrochloride
    1 Publications Verification

    DKGI-I hydrochloride; Diacylglycerol kinase inhibitor I hydrochloride

    		 PKC 5-HT Receptor Infection Inflammation/Immunology Cancer
    R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils .
    R 59-022 hydrochloride
  • HY-115911
    GPVI antagonist 2

    		Glycoprotein VI Cardiovascular Disease
    GPVI antagonist 2 (Compound 1) is a potential antagonist of Glycoprotein VI (GPVI). IC50 values of GPVI antagonist 2 are, respectively, 0.35 μM for collagen, 0.80 μM for CRP, 195.2 μM for convulxin and 81.38 μM for thrombin. Glycoprotein VI (GPVI) is a platelet major collagen receptor and a target for potent and safe antithrombotic research. GPVI antagonist 2 is a promising antiplatelet agent .
    GPVI antagonist 2
  • HY-115912
    GPVI antagonist 3

    		Glycoprotein VI Cardiovascular Disease
    GPVI antagonist 3 (Compound 2) is a potential antagonist of Glycoprotein VI (GPVI). IC50 values of GPVI antagonist 3 are, respectively, 1.01 μM for collagen, 1.92 μM for CRP, 7.24 μM for convulxin and 51.74 μM for thrombin. Glycoprotein VI (GPVI) is a platelet major collagen receptor and a target for potent and safe antithrombotic research. GPVI antagonist 3 is a promising antiplatelet agent .
    GPVI antagonist 3
  • HY-P5875
    P4pal10

    		Protease Activated Receptor (PAR) Cardiovascular Disease Inflammation/Immunology
    P4pal10 is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 ameliorates the injury in mice myocardial ischemia/reperfusion (I/R) models .
    P4pal10
  • HY-P5875A
    P4pal10 TFA

    		Protease Activated Receptor (PAR) Cardiovascular Disease Inflammation/Immunology
    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 .
    P4pal10 TFA

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