antithrombotic

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.

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

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

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.

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).

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

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

Iliparcil is an antithrombotic compound with oral activity.

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

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.

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).

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

Octacosanoic acid has antiplatelet and antithrombotic effects.

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].

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.

1. Glaucocalyxin A (Leukamenin F)-SBE-β-CD could be useful with a better solubility and sustained function in drug delivery. 2. Glaucocalyxin A activates caspase-3, decreases BAD phosphorylation, and reduces the expression of X-linked inhibitor of apoptosis protein. 3. Glaucocalyxin A inhibits Akt phosphorylation, suppresses proliferation, and promotes apoptosis in a dose-dependent manner, but not in normal glial cells. 4. Glaucocalyxin A inhibits collagen-stimulated tyrosine phosphorylation of Syk, LAT, and phospholipase Cγ2, the signaling events in collagen receptor GPⅥ pathway. 5. Glaucocalyxin A could potentially be developed as an antiplatelet and antithrombotic agent, can inhibit platelet p-selectin secretion and integrin activation by convulxin, is a GPVI selective ligand.

Salvianolic acid B (Dan Shen Suan B), a natural product from Salvia miltiorrhiza, is a water-soluble antioxidant. Salvianolic acid B has antiplatelet aggregation, anticoagulant, and antithrombotic effects, and is commonly used in the study of microcirculatory disorders.

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.

NP-313 (NSC-4264) is a potent antithrombotic agent that inhibits platelet aggregation and activation by inhibiting thromboxane A 2 synthesis and selectively inhibiting SOCC-mediated Ca2+ efflux.

Bupranolol is an antagonist of β2-adrenergic receptor and has been used for angina pectoris, hypertension, glaucoma, cardiac arrhythmia and as an antithrombotic.

Nitroaspirin (NCX 4016) is a nitric oxide donor and a nitro-derivative of Aspirin that inhibits cyclooxygenase. It induces cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells by down-regulating EGFR PI3K STAT3 signaling and modulating Bcl-2 family proteins. Additionally, Nitroaspirin possesses antithrombotic and antiplatelet properties and acts as a direct and irreversible inhibitor of COX-1.

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

Betrixaban maleate is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa.