par-1

TRAP-6 (Thrombin Receptor Activator Peptide 6) 是一种多肽片段，是选择性的蛋白酶激活受体 1 (PAR1) 激动剂，通过凝血酶受体激活人血小板。

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。

SCH79797 dihydrochloride 是一种有效的特异性蛋白酶激活受体 1 (PAR1) 拮抗剂，IC50 为 70 nM，Ki 为 35 nM。SCH79797 dihydrochloride 具有抗增殖和促凋亡作用。

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].

Protease-Activated Receptor-1 (PAR-1) Agonist, a selective peptide, activates the PAR-1 receptor by mimicking the specific actions of thrombin. It corresponds to the PAR1 tethered ligand, facilitating selective activation of this receptor.

Atopaxar hydrobromide 是可口服的，高效选择性的可逆凝血酶受体蛋白酶激活受体-1 拮抗剂。它是一种抗血小板剂，能干扰血小板信号，用于动脉粥样硬化血栓性疾病的研究。

Vorapaxar (MK-5348) 是抗血小板药物，是一种选择性、口服活性和竞争性的凝血酶受体蛋白酶激活受体(PAR-1)拮抗剂，Ki 值为 8.1 nM。它靠剂量依赖性抑制凝血酶受体激活肽 (TRAP) 诱导的血小板聚集。

iso-TRAP-6(iso-SFLLRN)是一个由异丝氨酸代替丝氨酸后的六肽，是一种蛋白酶激活受体 1 (PAR1) 激动剂，可通过 PAR-1 激活血小板。iso-TRAP-6 抵抗血浆氨基肽酶降解的能力比TRAP-6 强。

Atopaxar (E5555) 是一种高效、可口服的，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。它是一种抗血小板剂，能干扰血小板信号，可用于动脉粥样硬化血栓性疾病的研究。

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

Thrombin Receptor Activator for Peptide 也称为凝血因子 II 受体 (1-5) 或蛋白酶激活受体 1 (1-5)，用于研究冠心病 (CHD)。

Vorapaxar sulfate (Zontivity) 是一种选择性、口服活性和竞争性的凝血酶受体蛋白酶激活受体(PAR-1)拮抗剂，Ki 值为 8.1 nM。它剂量依赖性抑制凝血酶受体激活肽 (TRAP) 诱导的血小板聚集，是抗血小板药物。

Thrombin Receptor Activator for Peptide 5 (TRAP-5) 也称为凝血因子 II 受体 (1-5) 或蛋白酶激活受体 1 (1-5)，用于研究冠心病 (CHD)。

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

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。

Fidaxomicin (Tiacumicin B) 是一种大环RNA 聚合酶抑制剂，具有窄谱活性。它选择性地根除致病性艰难梭菌，对构成正常健康肠道菌群的多种细菌影响很小。

Cerdulatinib hydrochloride (PRT2070 hydrochloride) 是一种选择性可逆，具有口服活性、 ATP 竞争性的 SYK 和 JAK 的双重抑制剂，抑制 JAK1、2、3、SYK 和 Tyk2的 IC50值分别为12、6、8、32 和 0.5 nM。它可用于研究自身免疫性疾病和B 细胞恶性肿瘤。

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 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。

Protease-activated receptor 1 antagonist

protease-activated receptor-1 (PAR1) antagonist

Cerdulatinib (PRT2070) 是一种选择性 Tyk2抑制剂，IC50为 0.5 nM。它是 JAK 和 SYK 的双抑制剂，抑制JAK1、2、3 和SYK 的IC50分别为12、6、8 和 32。

LPAR1 antagonist2 (example 76) 作为LPAR1拮抗剂，其平均IC50值达到130 nM。