antithrombotic

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

Sulfinpyrazone (NSC-75925) is a uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties.

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).

Viquidil hydrochloride (Quinotoxine hydrochloride) is an isomer of Quinidine. Viquidil hydrochloride is an agent of cerebral vasodilator with antithrombotic activity.

Darexaban (Tanexaban, YM-150) is a direct inhibitor of Factor Xa.Darexaban and Darexaban glucuronide selectively and competitively inhibit FXA and inhibit prothrombin activity at the site of blood clot (thrombus) formation. This leads to a reduction in blood clot formation in a dose-dependent manner. Reducing clotting will reduce blockages in blood flow, which may reduce the risk of myocardial infarction, unstable angina, venous thrombosis, and ischemic stroke.

AZD1283 is an effective P2Y12 receptor antagonist (EC50: 3.0 ug/kg/min, binding IC50: 11 nM). AZD1283 dose-dependently induced increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 and 10 μg/kg/min, respectively. The doses induced the increase in bleeding time at 33 and 100 μg/kg/min for 3- and 13-fold, respectively. Thus, the therapeutic index (TI) was ≥10 for both compounds.

BPTU (BMS-646786) is an allosteric antagonist of P2Y1 (EC50 = 0.06-0.3 μM). Non-nucleotide ligand. Binds receptor outside of the helical bundle. Blocks inhibition of spontaneous contraction of rat and mouse colon induced by electrical field stimulation, nicotine and P2Y agonists. Antithrombotic; reduces platelet aggregation.

Tirofiban (L700462) (MK-383) is a selective palate GPIIb/IIIa antagonist which inhibits platelet aggregation with IC50 of 9 nM.

SC99 is a selective inhibitor of JAK2-STAT3 activation. SC99 downregulates the expression of STAT3-modulated genes.SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities

LCB-2853 is a potent thromboxane A2/prostaglandin H2 (TXA2/PGH2) receptor antagonist with antiplatelet aggregation, antivasospasm, and antithrombotic effects.

Trombodipine (PCA-4230) is a platelet aggregation inhibitor with antithrombotic activity and protection against Listeria monocytogenes.

Linotroban(CL-871502) is a potent selective thromboxane (TXA2) receptor antagonist with antithrombotic activity.

Fidexaban (CI1031) is a novel, potent, selective and orally active factor Xa inhibitor that has demonstrated antithrombotic activity in a variety of assays

LY 517717 is an orally active inhibitor of coagulation factor Xa with antithrombotic activity for the study of venous thromboembolism (VTE).

PCI-27483 is an activated coagulation factor VIIa inhibitor with antithrombotic effects in a baboon model of arterial thrombosis. It also inhibits the growth of BxPC3 xenografts by 42% and 85% at doses of 60 and 90 mg/kg, respectively.

Milvexian (BMS-986177) is a potent antithrombotic compound that inhibits human and rabbit factor XIa (FXIa) directly and reversibly. It is orally-bioavailable and exhibits a K i of 0.11 nM and 0.38 nM against human and rabbit FXIa, respectively.

BMS-986141(UDM-003183) is a selective and potent protease-activated receptor-4 (PAR-4) antagonist with oral activity and an IC50 value of 0.4 nM.BMS-98614 exhibits significant antithrombotic effects.

Iliparcil is an antithrombotic compound with oral activity.

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.

BMS-593214 is an active site-directed factor (F) VIIa inhibitor that exhibits antithrombotic and antihaemostatic properties. It acts as a direct competitive inhibitor of human FVIIa and a non-competitive inhibitor of FVIIa-activated substrate FX. Additionally, BMS-593214 effectively prevents electroinduced carotid artery thrombosis (AT) and wire-induced vena cava thrombosis (VT).

Nothofagin has antioxidant, and antithrombotic activities, it possesses anti-inflammatory activity by inhibiting hyperpermeability, expression of CAMs, and adhesion and migration of leukocytes, thereby endorsing its usefulness as a therapy for vascular inflammatory diseases.

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].

TRIA-662 (Nicotinamide Chloromethylate) is a niacin metabolite excreted via the urinary system.

Citronellal ((±)-Citronellal) is a monoterpene predominantly formed by the secondary metabolism of plants, producing antithrombotic, antiplatelet, and antihypertensive activities.