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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 [1].
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 [1] .
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 [1] .
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 [1] .
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 [1] .
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 [1] .
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'.)
Q94 hydrochloride, a selective PAR1 antagonist (IC50=916 nM), can selectively block PAR1/Gαq interaction and signalling. Q94 hydrochloride blocks PAR1-mediated increases in both CCL2 mRNA and protein levels in a dose-dependent manner. Q94 hydrochloride also completely blocks thrombin-induced ERK1/2 and MLC phosphorylation [1].
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. [1] .
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.)
Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1(PAR1) with an IC50 of 0.26 μM [1]. 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 .
YFLLRNP is a biological active peptide. (a partial agonist of PAR-1. YFLLRNP selectively active G12/13 signaling pathway without activating Gq or Gi pathways at low concentrations. YFLLRNP (60 μM))
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 [1] .
iso-TRAP-6 (iso-SFLLRN) is a PAR-1 agonist that can activate platelets. iso-TRAP-6 is an analog of TRAP-6 (HY-P0078) that refers to the use of isoserine instead of serine as first amino acid [1].
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 [1] .
PAR-4 Agonist Peptide, amide (PAR-4-AP; AY-NH2) is a proteinase-activated receptor-4 (PAR-4) agonist, which has no effect on either PAR-1 or PAR-2 and whose effects are blocked by a PAR-4 antagonist.
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 [1].
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 [1].
PAR-4 Agonist Peptide, amide TFA (PAR-4-AP TFA; AY-NH2 TFA) is a proteinase-activated receptor-4 (PAR-4) agonist, which has no effect on either PAR-1 or PAR-2 and whose effects are blocked by a PAR-4 antagonist [1].
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[1] .
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[1] .
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 [1].
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 [1] .
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 [1] .
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 [1] .
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'.)
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.)
YFLLRNP is a biological active peptide. (a partial agonist of PAR-1. YFLLRNP selectively active G12/13 signaling pathway without activating Gq or Gi pathways at low concentrations. YFLLRNP (60 μM))
iso-TRAP-6 (iso-SFLLRN) is a PAR-1 agonist that can activate platelets. iso-TRAP-6 is an analog of TRAP-6 (HY-P0078) that refers to the use of isoserine instead of serine as first amino acid [1].
PAR-4 Agonist Peptide, amide (PAR-4-AP; AY-NH2) is a proteinase-activated receptor-4 (PAR-4) agonist, which has no effect on either PAR-1 or PAR-2 and whose effects are blocked by a PAR-4 antagonist.
PAR-4 Agonist Peptide, amide TFA (PAR-4-AP TFA; AY-NH2 TFA) is a proteinase-activated receptor-4 (PAR-4) agonist, which has no effect on either PAR-1 or PAR-2 and whose effects are blocked by a PAR-4 antagonist [1].
The thrombin receptor/PAR1 protein is a high-affinity receptor for activated thrombin that is coupled to G proteins to stimulate phosphoinositide hydrolysis. This signaling mechanism suggests its involvement in platelet activation, which is critical for hemostasis and thrombosis. Thrombin Receptor/PAR1 Protein, Human (HEK293, His) is the recombinant human-derived Thrombin Receptor/PAR1 protein, expressed by HEK293 , with C-His labeled tag. The total length of Thrombin Receptor/PAR1 Protein, Human (HEK293, His) is 81 a.a., with molecular weight of ~10.2 kDa.
MARK1 is an important serine/threonine protein kinase that critically regulates cell polarity and microtubule dynamics. It phosphorylates microtubule-associated proteins (DCX, MAP2, MAP4, MAPT/TAU), causing their dissociation and disassembly. MARK1 Protein, Human is the recombinant human-derived MARK1 protein, expressed by E. coli , with tag free. The total length of MARK1 Protein, Human is 751 a.a., .
MARK1 is an important serine/threonine protein kinase that critically regulates cell polarity and microtubule dynamics. It phosphorylates microtubule-associated proteins (DCX, MAP2, MAP4, MAPT/TAU), causing their dissociation and disassembly. MARK1 Protein, Human (His) is the recombinant human-derived MARK1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of MARK1 Protein, Human (His) is 751 a.a., .
NR1I2; Nuclear receptor subfamily 1 group I member 2; Orphan nuclear receptor PAR1; Orphan nuclear receptor PXR; Pregnane X receptor; Steroid and xenobiotic receptor; SXR
The PXR protein is a nuclear receptor that acts as a multifunctional transcription factor activated by a variety of endogenous and exogenous compounds. It regulates genes involved in the metabolism and secretion of substances, responding to ligands such as rifampicin, hypericin, gugulin, colupulone, isoflavones, pregnenolone and progesterone. PXR Protein, Human is the recombinant human-derived PXR protein, expressed by E. coli , with tag free. The total length of PXR Protein, Human is 305 a.a., .
NR1I2; Nuclear receptor subfamily 1 group I member 2; Orphan nuclear receptor PAR1; Orphan nuclear receptor PXR; Pregnane X receptor; Steroid and xenobiotic receptor; SXR
The PXR protein is a nuclear receptor that acts as a multifunctional transcription factor activated by a variety of endogenous and exogenous compounds. It regulates genes involved in the metabolism and secretion of substances, responding to ligands such as rifampicin, hypericin, gugulin, colupulone, isoflavones, pregnenolone and progesterone. PXR Protein, Human (His) is the recombinant human-derived PXR protein, expressed by E. coli , with N-6*His labeled tag. The total length of PXR Protein, Human (His) is 305 a.a., .
PAR1 Antibody is an unconjugated, approximately 42 kDa, rabbit-derived, anti-PAR1 polyclonal antibody. PAR1 Antibody can be used for: WB, ELISA, IHC-P, IHC-F, IF expriments in human, mouse, rat, background without labeling.
