Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10081 | Thrombin inhibitor 1 | Thrombin | Proteases/Proteasome |
Thrombin inhibitor 1 is a potent inhibitor of thrombin (Ki: 0.66 nM, 2xaPTT=0.43 μM). | |||
T7625 |
TRAP-6
PAR-1 agonist peptide,Thrombin Receptor Activator Peptide 6,TRAP-6(2TFA) |
Protease-activated Receptor | GPCR/G Protein |
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。 | |||
T1986 |
Atopaxar
E5555,ER-172594-00 |
Protease-activated Receptor | GPCR/G Protein |
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。 | |||
T5519 |
Bivalirudin
BG-8967,比伐卢定,Hirulog-1 |
Thrombin | Proteases/Proteasome |
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。 | |||
T8917 |
PAR-2-IN-1
IUN76750,8-(叔丁基)-6-氯咪唑并[1,2-B]吡啶-2-羧酸甲酯 |
Protease-activated Receptor | GPCR/G Protein |
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。 | |||
T10951 |
Dabigatran ethyl ester hydrochloride
N-[[2-[[[4-(氨基亚氨甲基)苯基]氨基]甲基]-1-甲基-1H-苯并咪唑-5-基]羰基]-N-(2-吡啶基)-BETA-丙氨酸乙酯盐酸盐 |
Others; Thrombin | Others; Proteases/Proteasome |
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。 | |||
T1986L |
Atopaxar Hydrobromide
|
Protease-activated Receptor | GPCR/G Protein |
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。 | |||
T9845 | Thrombin inhibitor 5 | ||
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。 | |||
T9892 |
JAMM protein inhibitor 2
Acetamide, 2-(2-ethylphenoxy)-N-[2-methyl-4-(1-pyrrolidinyl)phenyl]- |
Others | Others |
JAMM protein inhibitor 2 (Acetamide, 2-(2-ethylphenoxy)-N-[2-methyl-4-(1-pyrrolidinyl)phenyl]-) 是 JAMM 蛋白酶的抑制剂,可用于抗癌的研究。 对thrombin、Rpn11 和 MMP2 的 IC50 分别为 10 μM、46 μM 和 89 μM。 | |||
T1893 |
Parmodulin 2
ML 161 |
Protease-activated Receptor | GPCR/G Protein |
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。 | |||
T2368L |
Edoxaban
Lixiana,依杜沙班 |
Factor Xa; Thrombin | Metabolism; Proteases/Proteasome |
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。 | |||
T72448 |
Thrombin inhibitor 6
|
||
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。 | |||
T80097 |
Hirullin P18
|
Thrombin | Proteases/Proteasome |
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。 | |||
T36777 |
Thrombin Receptor Agonist Peptide (trifluoroacetate salt)
|
||
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... | |||
T77221 | Benzenecarboximidamide, hydrochloride, hydrate (1:1:x) | ||
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。 | |||
T11100 |
DS-1040 Tosylate
|
Others | Others |
DS-1040 Tosylate is an oral active, selective thrombolytic inhibitor with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa, is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM | |||
T80738 |
Z-FK-ck
Z-Phe-Lys-2,4,6-Trimethylbenzoyloxy-methylketone |
||
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。 | |||
T73751 |
Lepirudin
|
||
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。 | |||
T82286 |
Glycylglycylcysteine
|
||
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。 | |||
T75242 |
Bivalirudin TFA
|
||
Bivalirudin TFA 是20个氨基多肽,可逆地抑制凝血酶。 | |||
T9670 | Patamostat | ||
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。 | |||
T36717 |
RWJ-56110 dihydrochloride
|
||
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 ap... |