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

Protease-Activated Receptor (PAR) (蛋白酶激活受体)

Protease activated receptors (PARs) are a family of G-protein-coupled receptors (GPCRs) that are irreversibly activated by proteolytic cleavage of the N terminus, which unmasks a tethered peptide ligand that binds and activates the transmembrane receptor domain, eliciting a cellular cascade in response to inflammatory signals and other stimuli. There are four members of the PAR family: PAR1, PAR2, PAR3 and PAR4. PARs have important functions in the vasculature, inflammation, and cancer and are important drug targets.

PARs are expressed on nearly all cell types in the blood vessel wall (ECs, fibroblasts, myocytes) and blood (platelets, neutrophils, macrophages, leukemic white cells) with exception of red blood cells. Thrombin-activated PAR-1, PAR-3, and PAR-4 are also expressed in epithelium, neurons, astrocytes, and immune cells. PAR-2, which is activated by trypsin-like serine proteases, is found in human vascular, intestinal, neuronal, and airway cells. Its expression increases in injured tissues or after stimulation by inflammatory mediators.

Protease-Activated Receptor (PAR) 相关产品 (27):

Cat. No. Product Name Effect Purity
  • HY-P0078
    TRAP-6 Agonist 99.74%
    TRAP-6 (PAR-1 agonist peptide),一种多肽片段,是选择性的蛋白酶激活受体 1 (PAR1) 激动剂。TRAP-6 通过凝血酶受体激活人血小板。TRAP-6 对 PAR4 无活性。
  • HY-112558
    AZ3451 Antagonist 99.54%
    AZ3451 是蛋白酶激活受体-2 (protease-activated receptor-2 (PAR2)) 拮抗剂,IC50 值为 23 nM。
  • HY-P1309A
    PAR-4 Agonist Peptide, amide TFA Agonist 99.97%
    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-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-14994
    SCH79797 dihydrochloride Antagonist ≥99.0%
    SCH79797 dihydrochloride 是一种高效的选择性非肽蛋白酶激活受体 1 (PAR1) 拮抗剂。SCH79797 dihydrochloride 抑制高亲和力的凝血酶受体激活肽与 PAR1 的结合,IC50 值为 70 nM,Ki 为 35 nM。SCH79797 dihydrochloride 以 IC50 为 3 μM 抑制凝血酶诱导的血小板凝集。SCH79797 dihydrochloride 具有抗增殖和促凋亡作用,并限制了大鼠心脏的心肌缺血/再灌注损伤。SCH79797 dihydrochloride 还可以有效地阻止血管平滑肌细胞,内皮细胞和星形胶质细胞中的 PAR1 活化。
  • 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-P1308
    SLIGRL-NH2 Agonist 99.66%
    SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) 是一种蛋白酶激活受体-2 (PAR-2) 激动剂。
  • HY-120528A
    GB-110 hydrochloride Agonist 99.94%
    GB-110 hydrochloride 是一种有效的,具有口服活性的,非肽类的 protease activated receptor 2 (PAR2) 激动剂。GB-110 hydrochloride 选择性诱导 PAR2 介导的 HT29 细胞内 Ca2+ 释放,EC50 值为 0.28 μM。
  • HY-P1314
    2-Furoyl-LIGRLO-amide Agonist 99.87%
    2-Furoyl-LIGRLO-amide 是一种有效的选择性蛋白酶激活受体2 (PAR2) 激动剂, 其 pD2 值为 7.0。
  • HY-14350
    AC-55541 Agonist 99.19%
    AC-55541是高选择性的蛋白酶激活受体 2 (PAR2) 激动剂 (pEC50=6.7),在其他 PAR 亚型或 30 种参与伤害感受和炎症的受体中没有活性。AC-55541 在 PI 水解测定和 Ca2+ 动态测定中的 pEC50 值为 5.9 和 6.6,并且在体内表现出伤害感受器活性。
  • HY-124748A
    ENMD-1068 hydrochloride Antagonist 98.18%
    ENMD-1068 hydrochloride 是一种具有抗血管生成和抗炎活性的选择性蛋白酶激活受体 2 (PAR2) 拮抗剂。ENMD-1068 hydrochloride 可通过抑制 TGF-β1/Smad 信号转导而减少星状细胞活化和胶原蛋白表达。
  • HY-P1260A
    FSLLRY-NH2 TFA Inhibitor 98.20%
    FSLLRY-NH2 TFA 是蛋白酶激活受体2 (PAR2)抑制剂。
  • HY-P0297
    Protease-Activated Receptor-4 Agonist 98.14%
    Protease-Activated Receptor-4 是转化生长因子受体 4 的激动剂。
  • HY-P1263A
    tcY-NH2 TFA Antagonist 99.84%
    tcY-NH2 TFA 是选择性的大鼠的 PAR4 肽类拮抗剂。tcY-NH2 TFA 抑制凝血酶和 AY-NH2 诱导的大鼠血小板聚集。
  • HY-P0226
    TFLLR-NH2 Agonist
    TFLLR-NH2是选择性的PAR1激动剂,EC50值为1.9 μM。
  • HY-18200
    Atopaxar Antagonist
    Atopaxar (E5555) 是一种高效、有口服活性活性的,选择性的,可逆的凝血酶受体蛋白酶激活受体-1 (PAR-1) 拮抗剂。Atopaxar 能干扰血小板信号。Atopaxar 可用于动脉粥样硬化血栓性疾病的研究。
  • HY-P2321
    TRAP-6 amide Agonist
    TRAP-6 amide 是一个 PAR-1 凝血酶受体的肽类激动剂。
  • HY-P1314A
    2-Furoyl-LIGRLO-amide TFA Agonist
    2-Furoyl-LIGRLO-amide TFA 是一种有效的选择性蛋白酶激活受体2 (PAR2) 激动剂, 其 pD2 值为 7.0。
  • HY-P1313A
    PAR 4 (1-6) (TFA) Agonist
    PAR 4 (1-6) TFA (GYPGQV TFA) 是一种六胜肽,它是蛋白酶激活受体 4 (PAR4) 的一个片段,并且能作为 PAR4 特异性的抑制剂。
  • HY-P1308A
    SLIGRL-NH2 TFA Agonist
    SLIGRL-NH2 TFA (Protease-Activated Receptor-2 Activating Peptide TFA) 是一种蛋白酶激活受体-2 (PAR-2) 激动剂。
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