Search Result
Results for "
protease-activated receptor
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P2518
-
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Protease Activated Receptor (PAR)
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Inflammation/Immunology
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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 .
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-
-
- HY-P2519A
-
-
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- HY-P0283
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-
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- HY-P0297
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-
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- HY-P1308
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-
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- HY-P2518A
-
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Protease Activated Receptor (PAR)
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Cancer
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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 .
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- HY-143313
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Protease Activated Receptor (PAR)
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Cardiovascular Disease
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Protease-Activated Receptor-1 antagonist 1 (Compound 13) is a protease-activated receptor-1 (PAR-1) antagonist with the IC50 of 3 nM by FLIPR technology. Protease-Activated Receptor-1 antagonist 1 can be used for the research of thrombotic cardiovascular, myocardial infarction, and peripheral arterial disease .
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- HY-P2519
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-
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- HY-143315
-
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Protease Activated Receptor (PAR)
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Cardiovascular Disease
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Protease-Activated Receptor-1 antagonist 3 is a potent protease-activated receptor-1 antagonist with an IC50 value of 7 nM. Protease-Activated Receptor-1 antagonist 3 shows binding affinity for hERG K + channel with an IC50 value of 9 µM .
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- HY-143314
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Protease Activated Receptor (PAR)
|
Cardiovascular Disease
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Protease-Activated Receptor-1 antagonist 2 is an orally active protease-activated receptor-1 (PAR-1) antagonist, with an IC50 value of 7 nM. Protease-Activated Receptor-1 antagonist 2 has favorable pharmacokinetic properties which is useful in the research of cardiovascular disease (CVD), such as atherosclerosis and restenosis .
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- HY-P1308A
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-
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- HY-P1313A
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GYPGQV TFA
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Protease Activated Receptor (PAR)
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Others
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PAR 4 (1-6) TFA (GYPGQV TFA), a hexapeptide, is a fragment of protease-activated receptor 4 (PAR4). PAR 4 (1-6) TFA acts as a PAR4-specific agonist .
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- HY-150790
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-
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- HY-18200
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E5555; ER-172594-00
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Protease Activated Receptor (PAR)
JAK
Apoptosis
|
Cardiovascular Disease
Cancer
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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 .
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- HY-18200B
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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 .
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- HY-13965
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ML161
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
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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 .
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-
- HY-112558
-
-
-
- HY-P1260
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-
-
- HY-117793
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-
-
- HY-P1260A
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- HY-P4451
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- HY-14351
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- HY-138558
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- HY-18200A
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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 .
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- HY-P1313
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- HY-P1310
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- HY-10119
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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 .
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- HY-P10577
-
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
RAG8 peptide is an antagonist for protease-activated receptor 4 (PAR 4), which inhibits late-stage platelet activation, and reduces thrombosis without altering hemostasis or increasing bleeding risk. RAG8 peptide can be used for atherosclerosis research .
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- HY-10119A
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SCH 530348 sulfate
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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 .
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- HY-P1310A
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-
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- HY-162762
-
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Protease Activated Receptor (PAR)
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Cancer
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PAR-2 antagonist 1 (Compound 9a) is a protease-activated receptor 2 (PAR2) antagonist with an IC50 value of 0.9 μM. PAR-2 antagonist 1 can effectively inhibit the proliferation and migration of breast cancer cells .
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- HY-19837
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Protease Activated Receptor (PAR)
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Inflammation/Immunology
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BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects .
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- HY-10119S
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SCH 530348-d5
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Protease Activated Receptor (PAR)
Isotope-Labeled Compounds
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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 .
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- HY-10119R
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Protease Activated Receptor (PAR)
|
Cardiovascular Disease
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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 .
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- HY-128345
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Protease Activated Receptor (PAR)
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Cardiovascular Disease
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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) .
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- HY-14350
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Protease Activated Receptor (PAR)
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Others
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AC-55541 is a highly selective protease-activated receptor 2 (PAR2) agonist (pEC50=6.7), displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation. AC-55541 has pEC50 values of 5.9 and 6.6 in PI hydrolysis assays and Ca 2+ mobilization assays and exhibits pronociceptive activity in vivo .
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- HY-107146
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P1pal-7
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Cancer
|
PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects .
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- HY-124748A
-
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Protease Activated Receptor (PAR)
Apoptosis
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Inflammation/Immunology
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ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 hydrochloride reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 hydrochloride also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 hydrochloride can be used in the study of endometriosis and liver fibrosis .
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- HY-124748
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Protease Activated Receptor (PAR)
Apoptosis
|
Inflammation/Immunology
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ENMD-1068 is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 can be used in the study of endometriosis and liver fibrosis .
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- HY-P5875
-
|
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 .
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- HY-P5357
-
|
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.)
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- HY-P5875A
-
|
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 .
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- HY-P0078
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TRAP-6
4 Publications Verification
PAR-1 agonist peptide; Thrombin receptor Activator Peptide 6
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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 .
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- HY-120528
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-
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- HY-120528A
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-
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- HY-163341
-
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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 .
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- HY-162408
-
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Protease Activated Receptor (PAR)
|
Others
|
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 .
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- HY-162409
-
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Protease Activated Receptor (PAR)
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Others
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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 .
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- HY-161401
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Protease Activated Receptor (PAR)
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Cardiovascular Disease
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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 .
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- HY-14994
-
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Protease Activated Receptor (PAR)
Apoptosis
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Cardiovascular Disease
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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 .
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- HY-14993
-
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Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
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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 .
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- HY-P5372
-
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Protease Activated Receptor (PAR)
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Others
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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'.)
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P2518
-
|
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 .
|
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- HY-P2519A
-
-
- HY-P0283
-
-
- HY-P0297
-
-
- HY-P1308
-
-
- HY-P2518A
-
|
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 .
|
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- HY-P1260
-
-
- HY-P2519
-
-
- HY-P1308A
-
-
- HY-P1313A
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GYPGQV TFA
|
Protease Activated Receptor (PAR)
|
Others
|
PAR 4 (1-6) TFA (GYPGQV TFA), a hexapeptide, is a fragment of protease-activated receptor 4 (PAR4). PAR 4 (1-6) TFA acts as a PAR4-specific agonist .
|
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- HY-P1260A
-
-
- HY-P4451
-
-
- HY-P5060
-
|
Peptides
|
Others
|
PAR-1 (1-6) (mouse, rat) is a polypeptide fragment of protease-activated receptor 1 .
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- HY-P1312
-
|
Peptides
|
Others
|
LRGILS-NH2 is a reverse-sequence protease-activated receptor-2 (PAR-2)-inactive, negative control, and SLIGRL-NH2 is a PAR-2-activating peptide .
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- HY-P1313
-
-
- HY-P1312A
-
|
Peptides
|
Others
|
LRGILS-NH2 TFA is a reverse-sequence protease-activated receptor-2 (PAR-2)-inactive, negative control, and SLIGRL-NH2 is a PAR-2-activating peptide .
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- HY-P4004
-
|
Peptides
|
Inflammation/Immunology
|
PAR-4 (1-6) amide human is an N-terminal fragment of protease-activated receptor 4 (PAR4). PAR-4 (1-6) amide human induce platelet aggregation .
|
-
- HY-P1310
-
-
- HY-P10577
-
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
RAG8 peptide is an antagonist for protease-activated receptor 4 (PAR 4), which inhibits late-stage platelet activation, and reduces thrombosis without altering hemostasis or increasing bleeding risk. RAG8 peptide can be used for atherosclerosis research .
|
-
- HY-P1310A
-
-
- HY-107146
-
P1pal-7
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Cancer
|
PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects .
|
-
- HY-P5875
-
|
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 .
|
-
- HY-P5357
-
|
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.)
|
-
- HY-P5875A
-
|
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 .
|
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- 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 .
|
-
- HY-P5372
-
|
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'.)
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Chemical Structure |
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- HY-10119S
-
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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 .
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