Thrombin

Melagatran is an orally available, direct synthetic thrombin inhibitor that does not require endogenous cofactors other than thrombin and does not significantly interact with any other enzymes in the coagulation cascade or with the fibrinolytic enzymes.

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.

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

H-Gly-Arg-pNA dihydrochloride (H-Gly-Arg-Pna 2HCl) belongs to the class of peptides that bind to 1,2 thrombin and can be quantified by colorimetric detection at 405 nm as a measure 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).

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

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

Dabigatran etexilate (BIBR 1048) is a thrombin inhibitor that binds to thrombin, blocking its thrombogenic activity and preventing thrombus formation.

Thrombin (MW 37kDa) is an allosteric serine protease with trypsin-like activity.

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べーた (FIXa), with K i s of 6.00 μみゅーM and 41.7 μみゅーM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and is potential for thromboembolic diseases treatment [1] [2] [3].

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

Eltrombopag Olamine (Eltrombopag diethanolamine salt) is an orally active small-molecule, nonpeptide thrombopoietin receptor agonist that stimulates megakaryopoiesis. It binds to and activates the transmembrane domain of the platelet thrombopoietin receptor (TPO-R or CD110), promoting the proliferation and differentiation of megakaryocytic cells and enhancing platelet production.

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.

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.

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)

Rivaroxaban (BAY 59-7939) is an orally bioavailable oxazolidinone derivative and a direct inhibitor of coagulation factor Xa with anticoagulant activity. Upon administration, it selectively binds to both free factor Xa and factor Xa within the prothrombinase complex, interfering with the conversion of prothrombin (factor II) to thrombin and preventing cross-linked fibrin clot formation. Rivaroxaban does not affect existing thrombin levels.

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

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.

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.

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

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 (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.

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

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).

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

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.

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.

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

Naroparcil, an orally available thioglycoside analog of 4-methylumbelliferyl βべーた-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.

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.

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.

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.

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.

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 μみゅーM [1].

Thrombin inhibitor 1 is a potent inhibitor of thrombin [Ki: 0.66 nM, 2xaPTT=0.43 μみゅーM].

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).

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

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.

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

Metolazone (SR-720-22) is a quinazoline-sulfonamide derived diuretic that inhibits sodium chloride symporters.

OM-189 is a selective inhibitor of synthetic thrombin.

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