thrombin inhibitor 1

Thrombin inhibitor 1 is a potent inhibitor of thrombin (Ki: 0.66 nM, 2xaPTT=0.43 μM).

Thrombin inhibitor13 (Compound 13a) 是一种针对凝血酶 (thrombin, FIIa) 的共价可逆抑制剂，IC50为0.7 nM。Thrombin inhibitor13 能延长活化部分凝血活酶时间 (aPTT) 和凝血酶原时间 (PT)，显示出抗血栓和抗凝活性。

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。

Edoxaban (Lixiana) (DU-176) 是一种选择性的，口服有效的 factor Xa (FXa)抑制剂。Edoxaban 对游离 FXa 和凝血酶原的 Ki 分别为 0.561 nM 和 2.98 nM。Edoxaban 是一种抗凝剂，可用于预防中风。Edoxaban 还是一种凝血酶和凝血因子 IXaβ (FIXa) 的弱抑制剂，Ki 值分别为 6.00 μM 和 41.7 μM，对 FXa 的选择性超过 10000 倍。由于具有抗血栓形成的特性，Edoxaban 可用于预防血栓栓塞性疾病的研究。

Patamostat (E-3123)是一种有效的蛋白酶抑制剂，对胰蛋白酶、纤溶酶和凝血酶具有显著抑制效果，其IC50值分别为39 nM、950 nM和1.9 μM。Patamostat可能在急性胰腺炎的发病机制和发展中发挥抑制作用。

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。

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。

Bivalirudin (BG-8967) 是一种直接凝血酶(thrombin)抑制剂，是一种肽类抗凝剂，可在侵入性心脏病，特别是在经皮冠状动脉介入中用于抗凝。

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。

Thrombin inhibitor 5 (compound 385) 是一种凝血酶抑制剂，IC50范围为 0.1 μM~1 μM，可用于静脉血栓栓塞的研究。

Dabigatran ethyl ester hydrochloride 是一种核糖基二氢烟酰胺脱氢酶抑制剂，IC50=0.8 μM，也是一种凝血酶的抑制剂。

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。

C1s-IN-1 trihydrochloride (Compound A1) 是 C1s 蛋白酶 (C1s protease) 的特异性抑制剂，Ki 为 5.8 μM。该化合物能够抑制 C1s 对 C2 的裂解，IC50 为 85 μM，并抑制经典途径的激活，其 IC50 为 22 μM。此外，C1s-IN-1 trihydrochloride 也是凝血酶 (thrombin) 的竞争性抑制剂，Ki 为 51.2 μM。

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。

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.

Thrombin receptor agonist peptide (TRAP-14) is a 14-amino acid peptide agonist of the α-thrombin receptor. It induces aggregation of washed platelets as well as platelets in citrated and hirudin plasma. TRAP-14 (100 μM) increases the cytosolic calcium concentration in isolated guinea pig pulmonary smooth muscle cells 5-fold over baseline. It increases pulmonary arterial pressure in isolated guinea pig lung when used at a concentration of 1 μM, which is comparable to the effect induced by 10 nM α-thrombin. TRAP-14 also induces contraction of isolated rat aortic rings and increases endothelin-1 (ET-1) levels in a dose-dependent manner, an effect that is reversed by the ETA antagonist BQ-123 and the nitric oxide synthase (NOS) inhibitor L-NNA .

Thrombin inhibitor6为高效的凝血酶抑制剂，IC50值为1 nM，表现出显著的抗凝作用。

Lepirudin为高效的不可逆凝血酶抑制剂，同时是重组水蛭素，主要在肝素诱导的血小板减少症（HIT）中发挥抗凝作用。

Bivalirudin TFA 是20个氨基多肽，可逆地抑制凝血酶。

Benzenecarboximidamide, hydrochloride, hydrate (1:1:x) (Benzamidine hydrochloride hydrate) 是一种可逆的竞争性胰蛋白酶样丝氨酸蛋白酶 (trypsin-like serine proteases) 抑制剂，对 Tryptase、Trypsin、uPA、Factor Xa、Thrombin 和 tPA 的Ki 值分别为 20、21、97、110、320 和 750 μM。

Pyr-Arg-Thr-Lys-Arg-AMC TFA为AMC肽类化合物，其结构由十肽组成，可经由特异性水解反应由如胰蛋白酶及凝血酶等蛋白酶作用下分解。该肽用于评估蛋白酶活性及酶抑制剂功效的检测。

Hirullin P18 作为一种高效的凝血酶抑制剂，展现出显著的抗凝作用。

Z-FK-ck (Z-Phe-Lys-2,4,6-Trimethylbenzoyloxy-methylketone) 作为一种选择性gingipain-K抑制剂，具有在剂量和时间依赖性的方式上延长血浆凝血酶时间 (TT) 的特性。

Glycylglycylcysteine是一种TAFI抑制剂，其Ki值0.99μM，IC50值为9.4μM，在TAFI底物测定中有效性得以体现。TAFI为一种碱性羧肽酶，通过裂解部分降解纤维蛋白末端的赖氨酸，起到抑制纤维蛋白溶解的功能。