1. GPCR/G Protein
  2. 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 oseltamivir-resistant 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 (12):

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 99.13%
    AZ3451是蛋白酶激活受体-2 (protease-activated receptor-2 (PAR2)) 拮抗剂。
  • 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-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-P1309
    PAR-4 Agonist Peptide, amide Agonist
    PAR-4 Agonist Peptide, amide 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-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-19837
    BMS-986120 Antagonist
    BMS-986120 是 PAR4 的一个拮抗剂,其在人类和猴子血液中的 IC50 值分别为 9.5, 2.1 nM。
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