PAR-2

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

PAR-2-IN-1 (IUN76750) 是一种 PAR-​2 信号通路抑制剂，具有抗炎和抗癌作用。

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)

PAR2 (1-6) 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 mouse and rat PAR2. It also corresponds to residues 39-44 and 37-42 of the mouse and rat full-length sequences, respectively. PAR2 (1-6) induces relaxation in precontracted rat arteries in a concentration-dependent manner, an effect that can be reduced by the nitric oxide synthase inhibitor L-NNA . It inhibits keratinocyte growth in the presence and absence of growth factors. PAR2 (1-6) inhibits LPS-induced pulmonary neutrophil influx and increases in matrix metalloproteinase-2 (MMP-2) activity in mice.

LRGILS-NH2 acetate 是一种 PAR-2 失活的反向肽。

ENMD-1068 HCl (ENMD 1068) 是一种选择性蛋白酶激活受体（PAR-2）拮抗剂，具有抗血管生成和抗炎活性。

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

AZ3451 是蛋白酶激活受体 2 的变构拮抗剂，IC50值为 23 nM。

I-191 是选择性有效的蛋白酶激活受体 2 拮抗剂。

PAR-2 (1-6) (human) (SLIGKV) 是 PAR-2的多肽激动剂。

PAR-2 antagonist 1 (Compound 9a) 为一种针对蛋白酶激活受体 2 (PAR2) 的拮抗剂,展现出0.9 μM的IC50值.该化合物在抑制乳腺癌细胞的增殖和迁移方面表现出高效能.

GB-88 is an selective , oral non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 μM.

AY 77 (Unk-Cha-Chg-NH2)是一种有效的、具有选择性的 PAR2激动剂。AY 77对 Ca2+和 ERK1 2信号显示出选择性(Ca2+释放的ec50值为40 nM, ERK1 2磷酸化的ec50值为2 μM)。AY 77能够促进人乳腺癌细胞的体外迁移。

Trypsin 是一种可从鱼类分离出的丝氨酸蛋白酶，可水解赖氨酸或精氨酸羧基侧蛋白质。Trypsin 具有抗炎活性，可通过 PDCoV 的 S 糖蛋白与 pAPN 的相互作用诱导 PDCoV 感染的细胞膜融合，可激活 PAR2 和 PAR4，促进细胞增殖和分化。Trypsin 可用于促进伤口愈合和研究神经源性炎症。

SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) 为一种蛋白酶激活受体-2 (PAR-2) 激动剂，具有诱导非组胺能性瘙痒的功能。

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

2-Furoyl-LIGRLO-amide TFA(729589-58-6 free base) 是一种有效的选择性蛋白酶激活受体 2 (PAR2) 激动剂。

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。

FSLLRY-NH2 TFA(245329-02-6 free base) 是一种蛋白酶激活受体 2 (PAR2) 抑制剂。在 ICR 小鼠中逆转紫杉醇诱导的机械异常性疼痛、热痛觉过敏和 PKC 激活。阻断分离的心脏成纤维细胞中的 ERK 活化和胶原蛋白生成。还可以减轻皮肤癣菌相关瘙痒小鼠模型的症状。

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。

AY 254 is a potent PAR2 biased agonist. Selectively activates ERK1 2 signaling (EC50= 2 nM for ERK1 2 phosphorylation versus 80 nM for Ca2+release). Reduces cytoKi ne-induced caspase 3 8 activation, promotes scratch-wound healing, and induces IL-8 secretion, in human colorectal cancer (HT29) cellsin vitro.

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。

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.

TFLLR-NH2 2TFA(197794-83-5(free base)) 是 PAR1 (EC50 :1.9 μM) 的激动剂。