Thrombin 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.

BMS 180742 is a thrombin exosite inhibitor. BMS 180742 does not inhibit arterial thrombosis.

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.

Hirudin (54-65) TFA is a fragment of Hirudin with anticoagulant effects. Hirudin is a thrombin inhibitor with blood anticoagulant property.

AT-1459 is a selective and orally active direct Thrombin inhibitor with a K_i value of 4.9 nM. AT-1459 exhibits excellent antithrombotic activity in both rat models of venous and arterial thrombosis. AT-1459 can be used for research on thrombosis-related diseases.

BCH-2763 is a potent and selective Thrombin inhibitor. BCH-2763 has a very high affinity for thrombin (K_i = 0.11 nM). BCH-2763 can effectively inhibit fibrin formation, platelet aggregation, and free thrombin activity. BCH-2763 can be used for the study of thrombosis.

Neutrophil elastase-IN-7 is a human neutrophil elastase inhibitor with an IC₅₀ of 0.54 μM. Neutrophil elastase-IN-7 also exhibits significant inhibitory activity against multiple coagulation proteins, with IC₅₀ values of 8.2, 12.7, 1.2 and 5.7 μM against thrombin, FXa, FXIa and FXIIIa, respectively. Neutrophil elastase-IN-7 can be used in the research of cardiopulmonary diseases and inflammatory diseases.

Ainsliaeasin C, a 7-hydroxycoumarin derivative, is an orally active anticoagulant agent that can be found in Ainsliaea fragrans. Ainsliaeasin C exerts anticoagulant activity both in vitro and in vivo. Ainsliaeasin C can be used for the research on thrombotic disorders.

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

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.

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).

Argatroban solution is mainly composed of Argatroban monohydrate (HY-B0375A). Argatroban monohydrate is a direct, selective thrombin inhibitor with anticoagulant properties, and can be used to alleviate motor paralysis caused by ischemic cerebral infarction.

LY 135305 is a thrombin activation inhibitor. LY 135305 inhibits spontaneous metastasis and increases animal survival.

RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with K_i of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.

Metolazone-d₇ is deuterium labeled Metolazone. Metolazone (SR-720-22) is primarily used to treat congestive heart failure and high blood pressure.

(21S)-Argatroban is an isomer of Argatroban (HY-B0375) and is a thrombin inhibitor. (21S)-Argatroban can prolong blood clotting time, reduces platelet adhesion and aggregation.

FXIIa-IN-1 hydrochloride is the hydrochloride of FXIIa-IN-1 (HY-149396). FXIIa-IN-1 (Compound 22) is a Factor XIIa inhibitor (K_i^app: 97.8 nM). FXIIa-IN-1 can be used for research of thrombosis.

Ro 09-1679 is a thrombin inhibitor, with an IC₅₀ of 33.6 μM. Ro 09-1679 inhibits the enzyme activities, with IC₅₀ values of 3.3, 0.04 and 0.0346 μM for factor Xa, trypsin and papain, respectively.

Ciraparantag (PER977) TFA is a thrombin and factor Xa inhibitor. Ciraparantag TFA 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.

Thrombin inhibitor 13 (Compound 13a) is a covalent and reversible inhibitor for thrombin (FIIa) with an IC₅₀ of 0.7 nM. Thrombin inhibitor 13 prolongs the activated partial thromboplastin time (aPTT) and prothrombin time (PT), exhibits antithrombotic and anticoagulant activities.