1. Signaling Pathways
  2. GPCR/G Protein
  3. Protease-Activated Receptor (PAR)

Protease-Activated Receptor (PAR)

Protease activated receptors (PARs) are a family of four G-protein-coupled receptors (PAR1, PAR2, PAR3, and PAR4) that are self-activated by tethered peptide ligands exposed by proteolytic cleavage of the extracellular amino terminus. PAR1, PAR3, and PAR4 are activated by thrombin, whereas PAR2 and, to a lesser degree, PAR4, are activated by trypsin.

PAR1 is a thrombin-activated receptor that contributes to inflammatory responses at mucosal surfaces. PAR1 antagonism might be explored as a treatment for influenza, including that caused by highly pathogenic H5N1 and H1N1 viruses.

PAR2 receptors have been implicated in numerous physiological processes necessitating therapeutic intervention, especially pain and inflammation and syndromes with a strong inflammatory component, including colitis, gastritis, pancreatitis, asthma and pulmonary disease, and arthritis.

Protease-Activated Receptor (PAR) 相关产品 (16):

Cat. No. Product Name Effect Purity
  • HY-10119
    Vorapaxar Antagonist 99.91%
    Vorapaxar是一种蛋白酶激活受体 (PAR-1)拮抗剂,可抑制凝血酶诱导的血小板活化。
  • HY-P0078
    TRAP-6 Agonist 99.84%
    TRAP-6 是蛋白酶激活受体1 (PAR1) 的激动剂。
  • HY-112558
    AZ3451 Antagonist 99.33%
    AZ3451 是蛋白酶激活受体-2 (protease-activated receptor-2 (PAR2)) 拮抗剂,IC50 值为 23 nM。
  • HY-14350
    AC-55541 Agonist 99.35%
    AC-55541 是 Protease-activated receptor 2 (PAR2) 新型小分子激动剂,能激活PAR2的信号转导,EC50 值为 200-1000nM。
  • HY-P0283
    Protease-Activated Receptor-2, amide Agonist 98.33%
    Protease-Activated Receptor-2, amide (SLIGKV-NH2) 是一种高效的蛋白酶活化受体-2 (PAR2) 活化肽。
  • HY-P1309A
    PAR-4 Agonist Peptide, amide TFA Agonist 99.93%
    PAR-4 Agonist Peptide, amide TFA (PAR-4-AP TFA; AY-NH2 TFA) 是一种蛋白酶激活受体-4 (PAR-4) 激动剂,对 PAR-1 或 PAR-2 都没有作用,且其作用会被 PAR-4 拮抗剂阻断。
  • HY-128345
    UDM-001651 Antagonist
    UDM-001651 是一种有效选择性的、口服生物可利用的蛋白酶激活受体 4 (PAR4) 拮抗剂 (IC50=4 nM;Kd=1.4 nM)。UDM-001651 在 γ-凝血酶诱导的富含血小板的血浆聚集测定 (γ-Thr PRP) 中显示抗血小板活性 (IC50=25 nM)。
  • HY-120261
    GB-88 Inhibitor
    GB-88 是一种口服、选择性的非肽类 PAR2 拮抗剂,可抑制 PAR2 介导的 Ca2+ 的释放,IC50 值为 2 µM。
  • HY-P0226A
    TFLLR-NH2(TFA) Agonist 99.29%
    TFLLR-NH2 (TFA) 是选择性的 PAR1 激动剂,EC50 值为 1.9 μM。
  • HY-P0297
    Protease-Activated Receptor-4 Agonist 98.35%
    Protease-Activated Receptor-4 是转化生长因子受体 4 的激动剂。
  • HY-P0226
    TFLLR-NH2 Agonist
    TFLLR-NH2是选择性的PAR1激动剂,EC50值为1.9 μM。
  • HY-19837
    BMS-986120 Antagonist
    BMS-986120 是具有一流的口服活性的蛋白酶激活受体 4 (PAR4) 的可逆拮抗剂,在人类和猴子血液中的 IC50 值分别为 9.5 nM 和 2.1 nM。BMS-986120 具有有效选择性的抗血小板作用。
  • HY-P1536
    Thrombin Receptor Activator for Peptide 5 TRAP-5
    Thrombin Receptor Activator for Peptide 5 (TRAP-5) 又叫作凝血因子 II 受体 (1-5) 或蛋白酶激活受体 1 (1-5) (Proteinase Activated Receptor 1 (1-5)),可用于冠心病的研究。
  • HY-P1309
    PAR-4 Agonist Peptide, amide Agonist
    PAR-4 Agonist Peptide, amide (PAR-4-AP; AY-NH2) 是一种蛋白酶激活受体-4 (PAR-4) 激动剂,对 PAR-1 或 PAR-2 都没有作用,且其作用会被 PAR-4 拮抗剂阻断。
  • HY-P1308
    Protease-Activated Receptor-2 Activating Peptide Agonist
    Protease-Activated Receptor-2 Activating Peptide 是一种蛋白酶激活受体-2 (PAR-2) 激动剂。
  • HY-117793
    I-191 Antagonist
    I-191 是一种有效的蛋白酶激活受体 2 (PAR2) 拮抗剂。
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