1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Thrombin

Thrombin

Thrombin is a Na+-activated, serine protease which is activated by the enzymatic cleavage of two sites on prothrombin by activated Factor X. Thrombin exists in two allosteric forms, slow (S) and fast (F), target toward anticoagulant and procoagulant activities.

Thrombin is the main effector protease in primary hemostasis by activating platelets and plays a key role in secondary hemostasis. Besides its well-known functions in hemostasis, thrombin also plays a role in various non-hemostatic biological and pathophysiologic processes, predominantly mediated through activation of protease-activated receptors (PARs). PAR-1, PAR-3, and PAR-4 are cleaved by thrombin, whereas PAR-2 is cleaved by trypsin. Thrombin also plays a crucial role in the migration and metastasis of human cancer cells.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-151983
    Thrombin inhibitor 6
    Inhibitor
    Thrombin inhibitor 6 is a potent thrombin inhibitor (IC50: 1 nM). Thrombin inhibitor 6 has the function as an anticoagulant.
    Thrombin inhibitor 6
  • HY-19674
    SSR182289
    Inhibitor
    SSR182289 (SSR182289A free base) is a selective and potent orally active thrombin inhibitor. SSR182289 competitively and selectivity inhibits human thrombin (Ki=0.031 μM). SSR182289 demonstrates anticoagulant activity in vitro (thrombin time EC100=96 nM) and inhibits tissue factor-induced thrombin generation (IC50=0.15 μM) in human plasma. SSR182289 inhibits thrombin-induced aggregation of human platelets (IC50=32 nM), but has no effect on aggregation induced by other platelet agonists .
    SSR182289
  • HY-114603A
    Efegatran sulfate
    Inhibitor
    Efegatran (LY 294468) sulfate is an inhibitor for thrombin, which inhibits aggregation of platelets, and exhibits anticoagulant and antithrombotic activities.
    Efegatran sulfate
  • HY-151146
    (1R,3S)-THCCA-Asn
    Inhibitor
    (1R,3S)-THCCA-Asn (4j) is a selective thrombin inhibitor with the IC50 value in the range of 0.07 to 0.14 μM. ((1R,3S)-THCCA-Asn has antithrombotic activity.
    (1R,3S)-THCCA-Asn
  • HY-173207
    Antiplatelet agent 3
    Inhibitor
    Antiplatelet agent 3 (Compound K-10) is a compound with anti-platelet aggregation activity. The IC50 values for platelet aggregation induced by ADP, AA and COL are 2.55, 3.22 and 2.09 mg/mL, respectively. Antiplatelet agent 3 is expected to be used in the research of cardiovascular diseases.
    Antiplatelet agent 3
  • HY-P2021
    BMS 180742
    Inhibitor
    BMS 180742 is a thrombin exosite inhibitor. BMS 180742 does not inhibit arterial thrombosis.
    BMS 180742
  • HY-18660S
    Ciraparantag-d8 tetrahydrochloride diacetate
    Inhibitor
    Ciraparantag-d8 (PER977-d8) tetrahydrochloride diacetate is the deuterium labeled Ciraparantag (HY-18660). Ciraparantag is a thrombin and factor Xa inhibitor. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants. It is reported to antagonize the effects of all coagulants except VKAs and agratroban.
    Ciraparantag-d<sub>8</sub> tetrahydrochloride diacetate
  • HY-167924
    Ono 3307 free base
    Ono 3307 Free base is a novel synthetic protease inhibitor that exhibits protective effects against acute pancreatitis by preventing hyperamylasemia and pancreatic edema. Ono 3307 Free base also inhibits the redistribution of lysosomal enzymes in acinar cells and mitigates lactic dehydrogenase discharge. Ono 3307 Free base effectively reduces cathepsin B leakage from lysosomes in a dose-dependent manner. Ono 3307 Free base is able to target trypsin (Ki=48 nM), thrombin (Ki=0.18 μM), plasma kallikrein (Ki=0.29 μM), plasmin (Ki=0.31 μM), pancreatic kallikrein (Ki=3.6 μM), and chymotrypsin (Ki=47 μM).
    Ono 3307 free base
  • HY-123120
    SA-152
    SA-152 is an organophosphorus inhibitor. SA-152 modulates the fibrinogen coagulation and TAME esterase activity of bovine α-thrombin.
    SA-152
  • HY-W743984
    Melagatran-d11
    Melagatran-d11 is the deuterium labeled Melagatran (HY-129056). Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin. Melagatran does not require endogenous co-factors for its antithrombin effect and may help to alleviate some of the damaging effects of endotoxemia. Melagatran has the potential to provide a rational approach in the prevention of arterial occlusion.
    Melagatran-d<sub>11</sub>
  • HY-P1636A
    Hirudin (54-65) TFA
    Inhibitor
    Hirudin (54-65) TFA is a fragment of Hirudin with anticoagulant effects. Hirudin is a thrombin inhibitor with blood anticoagulant property.
    Hirudin (54-65) TFA
  • HY-114603B
    Efegatran di(hydrochloride)
    Inhibitor
    Efegatran (LY 294468) dihydrochloride is an inhibitor for thrombin, which inhibits aggregation of platelets, and exhibits anticoagulant and antithrombotic activities.
    Efegatran di(hydrochloride)
  • HY-10163S5
    Dabigatran-d7
    Dabigatran-d7 (BIBR 953-d7; BIBR 953ZW-d7) is the deuterium labeled Dabigatran (HY-10163). Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM).
    Dabigatran-d<sub>7</sub>
  • HY-P5371
    TFLLRNPNDK-NH2
    Activator
    TFLLRNPNDK-NH2 is a biological active peptide. (This peptide is a thrombin receptor activating peptide. This PAR-1 agonist peptide reversibly binds to PAR-1 mimicking the 'tethered ligand' that thrombin makes available through proteolytic cleavage of substrate. It is also known to cause increase in liquid and protein permeability much like thrombin.)
    TFLLRNPNDK-NH2
  • HY-12586
    AZD6564
    Inhibitor
    AZD6564 is an orally active inhibitor for fibrinolysis through disruption of plasma kinase-fibrin interaction. AZD6564 dissolves human plasma clot with an IC50 of 0.44 μM. AZD6564 ameliorates hemorrhage in rats with EC50 of 1.62 μM, and exhibits good pharmacokinetic characteristics in rats.
    AZD6564
  • HY-P4593
    Z-Gly-Pro-Arg-4MβNA
    Z-Gly-Pro-Arg-4MβNA is the cleavage of the substrate of thrombin to release free 4-methoxy-2-naphthylamine (4MβNA). Free 4MβNA can be captured by 5-nitrosalicylaldehyde to produce an insoluble yellow fluorescent and marks the site of thrombin activity.
    Z-Gly-Pro-Arg-4MβNA
  • HY-10163S3
    Dabigatran-13C,d3
    Inhibitor
    Dabigatran-13C,d3 is the 13C- and deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM).
    Dabigatran-<sup>13</sup>C,d<sub>3</sub>
  • HY-P5027
    Cbz-Lys-Arg-pNA
    Substrate
    Cbz-Lys-Arg-pNA is a peptide substrate containing pNA as the chromogenic group. Cbz-Lys-Arg-pNA is widely used in enzymatic analysis, including thrombin, plasmin, factor Xa and Kallikrein.
    Cbz-Lys-Arg-pNA
  • HY-120563
    LY135305
    Inhibitor
    LY 135305 is a thrombin activation inhibitor. LY 135305 inhibits spontaneous metastasis and increases animal survival.
    LY135305
  • HY-122542A
    PPACK dihydrochloride
    Inhibitor
    PPACK dihydrochloride is potent, selective and irreversible thrombin inhibitor. PPACK dihydrochloride can be used an alternative anticoagulant to lithium heparin (LiHep) for blood gas and whole-blood electrolyte analyses. PPACK dihydrochloride is also a plasminogen activator (rt-PA) inhibitor. PPACK dihydrochloride can inhibit the binding of rt-PA to plasma protease inhibitors.
    PPACK dihydrochloride
Cat. No. Product Name / Synonyms Application Reactivity