protease-activated receptor 2

AC-55541 (AOB2796) 是高选择性的蛋白酶激活受体 2(PAR2)激动剂，pEC50为6.7。它在 PI 水解测定和 Ca2+动态测定中的pEC50值为 5.9 和 6.6，在体内表现出伤害感受器活性。

Protease-Activated Receptor-1 antagonist 2 是一种选择性的、口服具有活力的蛋白酶激活受体-1 (PAR-1) 拮抗剂 (IC50: 7 nM)。Protease-Activated Receptor-1 antagonist 2 显示出良好的药代动力学特性，能够用于进行心血管疾病 (CVD) 的相关研究（如动脉粥样硬化和再狭窄）。

Protease-Activated Receptor-1 antagonist 2 是一种选择性蛋白酶激活受体-1 (PAR-1) 拮抗剂，口服活性，IC50值为7 nM。该化合物具有优良的药代动力学特性，适用于心血管疾病 (CVD) 如动脉粥样硬化和再狭窄的研究。

GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM. GB-110 is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist.

Protease-Activated Receptor-2, amide (SLIGKV-NH2) 是 PAR2 的激动剂，IC50为 10.4 M。

SLIGRL-NH2 TFA（Protease-Activated Receptor-2 Activating Peptide TFA）作为PAR-2（蛋白酶激活受体-2）的激动剂，具有高度特异性。

PAR-2 Activating Peptide acetate (SLIGRL-NH2 acetate)(171436-38-7 free base) 是 Protease-Activated Receptor-2 (PAR-2) 的激动剂。

Parmodulin 2 (ML 161) 是一种蛋白酶激活受体 1(PAR1) 变构抑制剂，IC50为 0.26 μM。它是蛋白酶激活受体 1 (PAR1) 介导的血小板活化的抑制剂，可以抑制体外血小板聚集和体内血小板血栓形成。

GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM. GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist.

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[1][2].

PAR-2-IN-2 (compound P-596) 是一种蛋白酶激活受体 2 (PAR-2) 抑制剂，其对 SLIGKV 的 IC50 为 10.79 μM，而对 Trypsin 的 IC50 大于 200 μM。

VKGILS-NH2 Acetate 是 SLIGKV-NH2 的反向氨基酸序列控制肽，SLIGKV-NH2 是一种蛋白酶激活受体 2 (PAR2) 激动剂。

LRGILS-NH2 is a reversed amino acid sequence control peptide for SLIGRL-NH2, a protease-activated receptor-2 (PAR2) agonist that facilitates gastrointestinal transit in vivo.

GB83 is a selective human protease activated receptor 2 (PAR2) antagonist.

PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1It binds to NCTC 2544 cells expressing human PAR2 (Ki= 9.64 μM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50= 0.075 μM).2PAR2 (1-6) amide (100 μM) reduces colony formation of A549 lung cancer cells.1It induces superoxide production and degranulation in isolated human eosinophils when used at a concentration of 500 μM.3PAR2 (1-6) amide (5 μmol kg) induces tear secretion in rats when used in combination with amastatin .4 1.Bohm, S.K., Kong, W., Bromme, D., et al.Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2Biochem. J.314(Pt 3)1009-1016(1996) 2.Kanke, T., Ishiwata, H., Kabeya, M., et al.Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2Br. J. Pharmacol.145(2)255-263(2005) 3.Miike, S., McWilliam, A.S., and Kita, H.Trypsin induces activation and inflammatory mediator release from human eosinophils through protease-activated receptor-2J. Immunol.167(11)6615-6622(2001) 4.Nishikawa, H., Kawai, K., Tanaka, M., et al.Protease-activated receptor-2 (PAR-2)-related peptides induce tear secretion in rats: Involvement of PAR-2 and non-PAR-2 mechanismsJ. Pharmacol. Exp. Ther.312(2)324-331(2005)

Protease-Activated Receptor-1 (PAR-1) Agonist TFA is a selective peptide that acts as an agonist for the proteinase-activated receptor-1 (PAR-1). Corresponding to the tethered ligand of PAR-1, this compound mimics the actions of thrombin through the PAR-1 receptor[1][2].

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 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis[1][2]. Proteinase-activated receptors (PARs) are a family of G protein-coupled receptors activated by the proteolytic cleavage of their N-terminal extracellular domain, exposing a new amino terminal sequence that functions as a tethered ligand to activate the receptors.RWJ56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM) while being quite selective relative to collagen and the thromboxane mimetic U46619 [1].RWJ-56110 dihydrochloride is fully inhibits thrombin-induced RASMC proliferation with an IC50 value of 3.5 μM. RWJ-56110 dihydrochloride shows blockade of thrombin's action with RASMC calcium mobilization (IC50=0.12 μM), as well as with HMVEC (IC50=0.13 μM) and HASMC calcium mobilization (IC50=0.17 μM)[1].RWJ56110 (0.1-10 μM; 24-96 hours) inhibits endothelial cell growth dose-dependently, with half-maximal inhibitory concentration of RWJ56110 is approximately 10 μM[2].RWJ56110 (0.1-10 μM; 6 hours) inhibits DNA synthesis of endothelial cells in a thymidine incorporation assays. Endothelial cells are in fast-growing state (50-60% confluence), RWJ56110 inhibits cell DNA synthesis in a dose-dependent manner, but when cells that are in the quiescent state (100% confluent), the inhibitory effect of PAR-1 antagonists is much less pronounced[2].RWJ56110 (0.1-10 μM; pretreatment for 15 min) inhibits thrombin-induced Erk1 2 activation in a concentration-dependent manner. However, when endothelial cells are stimulated by FBS (final concentration 4%), it reduces partially the activated levels of Erk1 2[2].RWJ56110 (30 μM; 24 hours) has an inhibitory effect on endothelial cell cycle progression. It reduces the percentage of cells in the S phase, while alterations in the percentages of G1 and G2 M cells are less pronounced[2]. Western Blot Analysis[2] Cell Line: Endothelial cells [1]. Andrade-Gordon, et al.Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. oc Natl Acad Sci U S A. 1999 Oct 26;96(22):12257-62. [2]. Panagiota Zania, et al. Blockade of angiogenesis by small molecule antagonists to protease-activated receptor-1: association with endothelial cell growth suppression and induction of apoptosis. J Pharmacol Exp Ther. 2006 Jul;318(1):246-54.

Protease-Activated Receptor-1, PAR-1 Agonist acetate 是一种选择性蛋白酶激活受体 1 (PAR-1) 激动剂肽。 它对应于 PAR1 栓系配体，可以选择性地模拟凝血酶通过该受体的作用。

AC-264613 是一种选择性蛋白酶激活受体 (PAR-2) 激动剂，pEC50为 7.5。

ENMD-1068 hydrochloride 是一种选择性的蛋白酶激活受体 2 (PAR2) 拮抗剂。ENMD-1068 hydrochloride 可通过抑制TGF-β1 Smad 信号转导而减少肝星状细胞的活化和胶原蛋白的表达。ENMD-1068 hydrochloride 还能抑制子宫内膜细胞的增殖，并诱导病灶中上皮细胞的凋亡。ENMD-1068 hydrochloride 可用于子宫内膜异位症、肝纤维化的研究。

I-191 是选择性有效的蛋白酶激活受体 2 拮抗剂。

GB-110 hydrochloride 是一种有效的，具有口服活性的，非肽类的 protease activated receptor2 (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。

TFLLR-NH2 是选择性的一种PAR1激动剂，EC50值为1.9 μM。

FSLLRY-NH2 TFA 是蛋白酶激活受体2(PAR2)抑制剂。