Thrombin Inhibitor

Atecegatran TFA (AR-H067637 TFA) is an anticoagulant with selective direct thrombin inhibitory activity. Atecegatran TFA is commonly used to inhibit cardiovascular diseases. The biotransformation product of Atecegatran TFA, AR-H067637, is its active form and participates in the anticoagulation process.

CVS-1123 is an orally active direct thrombin inhibitor. CVS-1123 inhibits in vitro platelet aggregation of γ-thrombin and prolongs activated partial thromboplastin time. CVS-1123 alters the thrombotic response to deep vessel wall damage in arterial and venous circulation. CVS-1123 can be used in antithrombotic studies

DS-1040 is a low-molecular-weight imidazole derivative. DS-1040 is an inhibitor of the activated thrombin-activatable fibrinolysis (TAFIa). DS-1040 can promote fibrinolysis through suppressing TAFIa activity. DS-1040 can be studied in thrombolytic disease research.

Hirudin (55-65) (sulfated) is a fragment of Hirudin with anticoagulant effects. Hirudin is a thrombin inhibitor with blood anticoagulant property.

Argatroban-¹³C₆ hydrochloride is ¹³C labeled Argatroban (HY-B0375). Argatroban (MD-805) is a direct, selective thrombin 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.

PPACK is a potent, peptidic inhibitor targeting thrombin and granzyme GZMK. PPACK specifically blocks the activities of thrombin and GZMK, thereby inhibiting thrombin-mediated PAR-1 cleavage, as well as downstream inflammatory and procoagulant signaling pathways. Through stabilizing IκB proteins, blocking NF-κB activation and reducing systemic levels of proinflammatory/procoagulant biomarkers, PPACK exerts multiple effects including anti-inflammatory, antithrombotic, barrier repair, and inhibition of atherosclerotic plaque progression. PPACK binds to platelets without interference from kininogen, effectively limiting acute thrombus growth and reducing eosinophil infiltration and goblet cell hyperplasia in asthma models. PPACK is an important tool molecule for investigating the mechanisms of atherosclerosis, asthma and related thromboinflammatory diseases.

S-18326 is an orally active direct thrombin inhibitor. S-18326 inhibits thrombus formation by reversibly and with high affinity binding to the active site of thrombin, directly preventing the conversion of fibrinogen to fibrin. S-18326 effectively prolongs various clotting times in human plasma. S-18326 has demonstrated antithrombotic efficacy in multiple animal models without causing thrombocytopenia. S-18326 can be used in research on thromboembolic diseases.

SAR107375 is a potent and orally active dual thrombin and factor Xa inhibitor, with K_i values of 1 nM and 8 nM for factor Xa and thrombin, respectively.

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.

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).

Thrombin inhibitor 6 is a potent thrombin inhibitor (IC₅₀: 1 nM). Thrombin inhibitor 6 has the function as an anticoagulant.

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.

SSR182289 (SSR182289A free base) is a selective and potent orally active thrombin inhibitor. SSR182289 competitively and selectivity inhibits human thrombin (K_i=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 .

DPC423 free base is a selective and orally active factor Xa inhibitor with a K_is of 0.15 (human) and 0.3 (rabbit) nM. DPC423 free base exhibits K_is of 60, 61 and 6000 nM against human trypsin, plasma kallikrein and thrombin. DPC423 free base blocks the formation of prothrombinase complex, reduces thrombin production, inhibits fibrin formation and platelet activation. DPC423 free base can be used for the study of anticoagulation of arterial thrombosis.

Napsagatran (Ro 46-6240) is a potent thrombin inhibitor. Napsagatran exhibits anticoagulant effects in vitro and in vivo. Napsagatran can be used in antithrombotic research^[1][2].

Rovunaptabin sodium (ARC 183 sodium) is a DNA aptamer, which is a single-stranded DNA molecule consisting of 15 deoxynucleotides that forms well-defined three-dimensional configuration, allowing it to bind to thrombin with high affinity and specificity.

Efegatran (LY 294468) sulfate is an inhibitor for thrombin, which inhibits aggregation of platelets, and exhibits anticoagulant and antithrombotic activities.

(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.

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.