Thrombin

Flovagatran (TGN 255) is an orally active, potent, and selective inhibitor of thrombin and parenteral direct factor II.Flovagatran is used to study venous thromboembolism.

Melagatran, a direct and orally active thrombin inhibitor, specifically inhibits thrombin without affecting other enzymes in the coagulation cascade or fibrinolytic enzymes. It does not rely on endogenous co-factors to exert its antithrombin effect, and may alleviate the harmful effects of endotoxemia. As a result, Melagatran offers a promising strategy for the prevention of arterial occlusion.

AEBSF hydrochloride (Pefabloc SC) is an irreversible inhibitor of serine proteases, such as chymotrypsin, kallikrein, thrombin, plasmin, and trypsin.

Heparin sodium is a sulfated polysaccharide, which belongs to the family of glycosaminoglycans. It is utilized as an anticoagulant and interacted with diverse proteins for numerous important biological activities.Heparin sodium salt (Sodium heparinate) significantly inhibits exosome-cell interactions.

RS-601 is a potent dual leukotriene D4/thromboxane A2 inhibitor that inhibits antigen-induced airway hyperresponsiveness (AHR) and shows asthmatic effects in a guinea pig model of asthma.

Pirodomast is a thromboxane A (TXA2) synthase inhibitor. Pirodomast inhibits leukotriene (LT) D4, C4, E4 formation and thromboxane B2 (TXB2) activity, but is weakly or ineffectively antagonistic to guinea pig bronchospasm induced by histamine, methacholine, serotonin, LTC4, or platelet-activating factor. Pirodomast is a potential antiallergic compound. Pirodomast had only weak relaxant activity on guinea pig trachea in vitro. Pirodomast is a potential antiallergic compound that inhibits the protein hydrolyzing activity of trypsin in vitro, prevents antigen-induced immediate and late asthmatic responses in allergic sheep in vivo, and inhibits antigen-induced airway hyperresponsiveness to histamine and carbachol in allergic sheep.

Efegatran sulfate (LY294468 sulfate) is a potent thrombin inhibitor used in the treatment of thrombotic disorders.

Menadione (Vitamin K3) is a synthetic naphthoquinone without the isoprenoid side chain and biological activity, but can be converted to active vitamin K2, menaquinone, after alkylation in vivo.

Bivalirudin (BG-8967) is a reversible inhibitor of α- and ζ-thrombin (Kis = 2.56 and 1.84 nM, respectively), enzymes that exhibit high fibrinogen-clotting activities.

Heparin (Adomiparin) is a mucopolysaccharide sulfate often used as an anticoagulant in clinical medicine.Heparin has shown partial anti-inflammatory activity in in vivo experiments.

Ozagrel hydrochloride (OKY-046 HCl) is a selective thromboxane A(2) synthetase inhibitor used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

Metolazone (SR-720-22) is a quinazoline-sulfonamide derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.

Succinyl-(Pro58,D-Glu65)-Hirudin (56-65) (sulfated) is a hirugen-like peptide with greater thrombin affinity than Hirugen, exhibiting a dissociation constant (K D) of less than 100 nM. This compound acts as an antithrombotic agent, effectively inhibiting thrombin-induced fibrin clot formation with an inhibitory concentration (IC 50) of 0.087 μM [1].

NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion. NFPS is a selective and non-competitive glycine transporter-1 (GlyT1) inhibitor (IC50s: 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively).

Eltrombopag Olamine (Eltrombopag diethanolamine salt) is the orally active ethanolamine salt of eltrombopag, a small-molecule, nonpeptide thrombopoietin receptor agonist with megakaryopoiesis-stimulating activity. Eltrombopag binds to and stimulates the transmembrane domain of the platelet thrombopoietin receptor (TPO-R or CD110), a member of the hematopoietin receptor superfamily. Activation of TPO-R leads to the proliferation and differentiation of cells in the megakaryocytic lineage and an increase in platelet production.

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

Lusutrombopag (Mulpleta) is an orally bioavailable, small molecule thrombopoietin (TPO) receptor agonist for chronic liver disease (CLD) patients with thrombocytopenia prior to elective invasive surgery.

Dabigatran Etexilate Mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI, Ki: 4.5 nM).

Proflavine Hemisulfate (3,6-Diaminoacridine hemisulfate) is the hemisulfate salt form of proflavine, an acridine-derived fluorescent contrast and disinfectant agent that can potentially be used for cellular imaging and antiseptic purposes.

Ozagrel (Domenan) is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

Avatrombopag (YM477) is a new oral thrombopoietin (TPO) receptor agonist, activating TPO receptor and increasing megakaryocytic proliferation differentiation and platelet production.

Odiparcil is an orally active beta-d-thioxyloside analog. Odiparcil is an indirect thrombin inhibitor that exerts its anticoagulant effect through activation of antithrombin II (heparin cofactor II). It also has an antithrombotic activity associated with a reduced risk of adverse bleeding events.

Thrombin (MW 37kDa) is a trypsin-like allosteric serine protease.

Naroparcil, an orally available thioglycoside analog of 4-methylumbelliferyl β-D-xyloside, showed antithrombotic effects in the Wessler sludge model of venous thrombosis (jugular vein).Naroparcil enhanced the formation of the thrombin heparin cofactor II complex, induced dermatophyte sulfate-like substances in plasma from treated rabbits appearance, but reduced the formation of thrombin antithrombin III complexes in plasma incubated with (125I)-human alpha-thrombin.

Dabigatran (BIBR 953ZW) is a THROMBIN inhibitor which acts by binding and blocking thrombogenic activity and the prevention of thrombus formation. It is used to reduce the risk of stroke and systemic EMBOLISM in patients with nonvalvular atrial fibrillation.

TFLLRNPNDK-NH2 is a biologically active peptide and a thrombin receptor activating peptide (TRAP). As a PAR-1 agonist, it reversibly binds to PAR-1, mimicking the 'tethered ligand' created by thrombin through proteolytic substrate cleavage. It also induces increased liquid and protein permeability, similar to thrombin's effect.

Thrombin receptor peptide ligand, a thrombin receptor antagonist, serves as an antithrombotic agent [1].

OM-189 is a selective inhibitor of synthetic thrombin.

Imitrodast is a small molecule thromboxane A2 synthase (TXA2 synthase) inhibitor for the treatment of immune system disorders, respiratory disorders, and cardiovascular diseases, and can be used in studies of arterial thrombosis, asthma, and coronary vasospasm.

Rivaroxaban (BAY 59-7939) is an orally bioavailable oxazolidinone derivative and direct inhibitor of the coagulation factor Xa with anticoagulant activity. Upon oral administration, rivaroxaban selectively binds to both free factor Xa and factor Xa bound in the prothrombinase complex. This interferes with the conversion of prothrombin (factor II) to thrombin and eventually prevents the formation of cross-linked fibrin clots. Rivaroxaban does not affect existing thrombin levels.

Argatroban Monohydrate is a specific thrombin inhibitor, which is a non-heparin anticoagulant, prevents the formation of thrombi.

Protamine sulfate is a polycationic peptide that serves as an antiheparin agent. This compound can neutralize the anticoagulant action of heparin and enhance lipid-mediated gene transfer.

Dabigatran ethyl ester (Dabigatran (ethyl ester)) is an emerging oral anticoagulant and it also is a direct inhibitor of thrombin activity.

Eltrombopag (SB-497115-GR), an orally active thrombopoietin receptor agonist with megakaryopoiesis stimulating activity, binds to and stimulates the platelet thrombopoietin receptor (TPO-R or CD110).

(S)-(+)-Ibuprofen (Dexibuprofen) , is a non-steroidal anti-inflammatory drug (NSAID), inhibiting cyclooxygenase (COX).

Argatroban (MCI-9038), a specific thrombin inhibitor, which is a non-heparin anticoagulant, prevents the formation of thrombi.

Edoxaban (Lixiana) (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with K i s of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and is able to be used for stroke prevention. Edoxaban is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with K i s of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and is potential for thromboembolic diseases treatment [1] [2] [3].

RWJ-445167 is a thrombin and factor Xa dual inhibitor(Ki of 4.0 nM and 230 nM, respectively), with potent antithrombotic activity.

Ximelagatran (H 376-95), a direct thrombin inhibitor, can be taken orally and acts solely by inhibiting the actions of thrombin. Ximelagatran is converted to the active agent melagatran in vivo.

p-Hydroxycinnamic acid (NSC-59260) can inhibit platelet activity, with IC50s of 371 μM, 126 μM for thromboxane B2 production and lipopolysaccharide-induced prostaglandin E2 generation, respectively.

Dabigatran ethyl ester hydrochloride is an effective inhibitor of ribosyl dihydronicotinic acid amide dehydrogenase (NQO2) with an IC50 value of 0.8 μM and is a thrombin inhibitor.

NQ301, an antithrombotic agent, inhibits collagen-challenged rabbit platelet aggregation (IC50: 10 mg/mL).

Z-Gly-Pro-Arg-4MβNA is a thrombin substrate that, upon cleavage by thrombin, releases 4-methoxy-2-naphthylamine (4MβNA). This liberated 4MβNA reacts with 5-nitrosalicylaldehyde to form an insoluble yellow fluorescent product, indicating the site of thrombin activity [1].

Hirullin P18 is a potent thrombin inhibitor with anticoagulant properties [1].

Edoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention.

Enoxaparin sodium is a low-molecular-weight heparin (LMWH) that has recently been approved by the US FDA for use in patients with medically managed ST-segment myocardial infarction (STEMI), or STEMI with subsequent percutaneous coronary intervention (PCI)

Dabigatran etexilate (BIBR 1048) is a thrombin inhibitor, which acts by binding and blocking thrombogenic activity and the prevention of thrombus formation.