anti-thrombotic

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

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.

PSI-697 (P-Selectin Inhibitor) is an orally active P-selectin inhibitor with anti-inflammatory and anti-thrombotic effects, useful for studying cardiovascular diseases such as atherosclerosis.

α-Linolenic Acid (ALA) is an essential fatty acid that cannot be synthesized by the human body and is obtained by isolating it from seed oils. α-Linolenic acid has been shown to improve memory, inhibit thrombosis, and lower blood lipids.

Euchrestaflavanone A is a useful organic compound for research related to life sciences and the catalog number is T124187.

PAR4 antagonist8 (Compound 20f) is an effective oral and selective PAR4 antagonist with an IC50 of 15.32 nM, boasting favorable pharmacokinetic properties. It effectively inhibits human platelet aggregation induced by PAR4 agonists (IC50=6.39 nM) and also suppresses platelet aggregation in mice. PAR4 antagonist8 is utilized in anti-thrombotic research.

Imidazole-d4 is an isotope-labeled variant of imidazole, which is a heterocyclic aromatic compound. Imidazole molecules serve as inhibitors for acetylcholinesterase (AChEI) and xanthine oxidase (XO) and have been utilized as corrosion inhibitors. They display a range of biological activities, including antifungal, antitubercular, anti-inflammatory, antioxidant, and analgesic properties. Imidazole inhibits platelet microsomes from converting endoperoxides (PGG2 and PGH2) into thromboxane A2. Additionally, imidazole derivatives show inhibitory effects on the SARS-CoV-2 3CLpro enzyme, offering potential for research in Alzheimer’s disease, gout, COVID-19, and thrombotic disorders.

BCX-3607 is an orally active tissue factor/factor VIIa (TF-FVIIa) inhibitor with an IC50 of 4 nM. By inhibiting the TF-FVIIa complex, it effectively blocks the extrinsic coagulation pathway and significantly prolongs prothrombin time (PT). BCX-3607 exhibits higher selectivity for TF-FVIIa over other serine proteases like thrombin and FXa. It reduces thrombus weight and inflammation, offering dual anti-thrombotic and anti-inflammatory effects. BCX-3607 is applicable in research on thrombosis-related diseases.

BM 567 (compound 1) is a thromboxane A2 receptor (TXR) antagonist and thromboxane A2 synthase (TXS) inhibitor with anti-thrombotic effects, exhibiting IC₅₀ values of 1.1 and 12 nM respectively.

Protogracillin, a steroidal saponin isolated from Dioscorea zingiberensis Wright (DZW), may inhibit platelet aggregation (PAG) and thrombosis, potentially reducing the risk of cardiovascular diseases through its anti-thrombotic action.

12-HETE ((±)12-HETE) is a modulator of PGE2, with both anti-thrombotic and pro-thrombotic effects, inducing PGE2 release and COX-2 expression via phospholipase A2 (sPLA2-IIA) inducers. It is also a neuroregulator activating retinal cell endothelial dysfunction in diabetic retinopathy.

Liriope muscari baily saponins C has an anti-thrombotic activity due to down-regulation of the increased mRNA expression levels of TF and IL-6.

(1R,3S)-THCCA-Asn (4j) is a selective inhibitor of thrombin with an IC50 range of 0.07-0.14 μM and exhibits anti-thrombotic effects.

FXIa-IN-8, a potent and selective inhibitor of FXIa (IC50: 14.2 nM), exhibits anti-thrombotic effects without increasing the risk of bleeding or causing significant toxicity [1].

Mumefural, a bioactive compound found in the processed fruit of Prunus mume Sieb., inhibits platelet aggregation, exhibits anti-thrombotic properties, and ameliorates cognitive impairment [1] [2].

Caplacizumab (ALX-0681), a humanized anti-von Willebrand factor (vWF) nanobody, serves to impede vWF-mediated platelet adhesion, thereby averting additional microthrombi formation. This compound is utilized in the study of thrombotic thrombocytopenic purpura (TTP) [1].

6-Hydroxykaempferol 3-O-beta-D-glucoside has anti-thrombotic,and antioxidative activities.