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

Thrombin

Thrombin

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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-14878
    (2R)-Atecegatran
    		Inhibitor
    (2R)-Atecegatran ((2R)-AZD-0837; (Ph(3-Cl)(5-OCHF2)-(R)CH(OH)C(O)-Aze-Pab)) is a thrombin inhibitor. (2R)-Atecegatran can be used in research related to thromboembolic disorders.
    (2R)-Atecegatran
  • HY-122542
    PPACK
    		Inhibitor
    PPACK is potent, selective and irreversible thrombin inhibitor. PPACK can be used an alternative anticoagulant to lithium heparin (LiHep) for blood gas and whole-blood electrolyte analyses. PPACK is also a plasminogen activator (rt-PA) inhibitor. PPACK can inhibit the binding of rt-PA to plasma protease inhibitors.
    PPACK
  • HY-12605
    SAR107375
    		Inhibitor
    SAR107375 is a potent and orally active dual thrombin and factor Xa inhibitor, with Ki values of 1 nM and 8 nM for factor Xa and thrombin, respectively.
    SAR107375
  • HY-P10293
    NQEQVSP
    		Inhibitor
    NQEQVSP, a fibrin-binding protein-derived peptide (FBP), is a factor XIIIa substrate. NQEQVSP can be recognized by factor XIII and is enzymatically conjugated into fibrin during polymerization.
    NQEQVSP
  • HY-162646
    FXIIa-IN-5
    		Inhibitor
    FXIIa-IN-5 (Compound 4J) is an orally active, selective inhibitor for factor XIIa (FXIIa), with IC50 of 21 nM. FXIIa-IN-5 inhibits the intrinsic coagulation pathways, and exhibits anti-inflammatory and antithrombotic activity in Carrageenan (HY-125474)-induced mice thrombosis models. FXIIa-IN-5 exhibits moderate pharmacokinetic characteristics and slightly toxicity (at 100 mg/kg).
    FXIIa-IN-5
  • HY-P6027
    H-D-CHA-Ala-Arg-pNA
    H-D-CHA-Ala-Arg-pNA is a chromogenic substrate for the amidolytic assay.
    H-D-CHA-Ala-Arg-pNA
  • 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-N16369
    1,2-Di-(9Z-hexadecenoyl)-sn-glycerol
    		Inhibitor
    1,2-Di-(9Z-hexadecenoyl)-sn-glycerol (Compound 2e) is a diacylglycerol derivative that can be isolated from the fungus Stereum Hirsutum. 1,2-Di-(9Z-hexadecenoyl)-sn-glycerol has potential thrombin-inhibiting activity and can be used in research related to antithrombotic drugs.
    1,2-Di-(9Z-hexadecenoyl)-sn-glycerol
  • 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>
Cat. No. Product Name / Synonyms Application Reactivity