Welcome to Raystarbio!Focus On Forefront Bioactive Compounds.
Find Your Distributors

Select Your Country or Region

$ USD

You are here:Home-Research Areas-Cardiovascular Disease-Thrombosis

Request The Product List ofThrombosis Thrombosis

    Thrombosis is a crucial hemostatic process for maintaining blood volume (hemostasis) following injury, yet aberrant thrombosis can trigger pathological conditions including myocardial infarction and stroke. Therefore the initiation of thrombosis is tightly controlled under physiological conditions.

    Mechanisms of Thrombosis and Hemostasis

    Platelets are a central component of thrombosis and exhibit a rapid, exponential activation in the event of tissue damage. Produced in the bone marrow, platelets are anucleate cell fragments of megakaryocytes. Despite having no nucleus, platelets possess two different types of granules within the cytoplasm - alpha granules and dense granules - and also express a number of different receptors on their plasma membranes. Both alpha and dense granules contain a variety of bioactive mediators including ADP, calcium and 5-HT as well as growth factors such as platelet-derived growth factor (PDGF), insulin-like growth factor-1 (IGF-1) and transforming growth factor (TGF) β1. Upon activation, platelets undergo degranulation; this releases granule contents into the surrounding environment and promotes the activation and aggregation of neighboring platelets.

    Receptors present on the platelet plasma membrane include the purinergic (P2X) receptors P2X1, P2Y1 and P2Y12; the 5-HT receptor 5-HT2A; the thromboxane A2 (TXA2) receptor TP; and the protease-activated receptorsPAR1 and PAR4. Platelet signaling may also be activated by exposure to collagen via the glycoprotein receptor, GPVI. Key downstream mediators of these receptors include the plasma membrane phospholipid phosphatidylinositol 4,5-bisphosphate (PIP2), which is cleaved by phospholipase C to form inositol triphosphate (IP3) and diacylglycerol (DAG). IP3 receptor (InsP3R) activation triggers the efflux of calcium ions from intracellular calcium stores such as the endoplasmic reticulum, leading to a rise in intracellular calcium and subsequent platelet aggregation through the activation of integrin receptors.


    Agonist stimulation of platelets also initiates the production of arachidonic acid from membrane phospholipids in a reaction catalyzed by cytosolic phospholipase A2 (cPLA2). Arachidonic acid can be utilized by both cyclooxygenases (COX) to form prostaglandin H2 (PGH2), and also by lipoxygenases (LOX) to form the lipid mediator hydroperoxyeicosatetraenoic acid (HPETE). PGH2 is further metabolized to form prothrombotic eicosanoids including TXA2.

Cat. No. Product Name CAS No. Information
GY04359

Edoxaban tosylate monohydrate

1229194-11-9

A potent and orally active Factor Xa inhibitor with Ki of 0.561 nM; also inhibits prothrombinase (Ki=2.98 nM), weakly inhibits thrombin and FIXa (Ki=6.0 uM, and 41.7 uM); exhibits >10,000-fold selectivity for Fxa over FVIIa/sTF, FXIa, tPA, aPC, trypsin, plasmin and chymotrypsin; inhibits thrombus formation in rat and rabbit thrombosis models.

GY06541

BCX-1470

217099-43-9

BCX-1470 is a serine protease inhibitor that inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM); displays 3.4-fold and 200-fold bette than that of trypsin, respectively; inhibits esterolytic activity translates into potent inhibition of the proteolytic activity of C1s, factor D, and consequently of the classical and alternative pathway-mediated hemolysis of target RBC (IC50=46 nM and 330 nM, respectively); blocks the reverse passive Arthus (RPA) reaction in rats.

GY06540

BCX-1470 methanesulfonate

217099-44-0

BCX-1470 methanesulfonate is a serine protease inhibitor that inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM); displays 3.4-fold and 200-fold bette than that of trypsin, respectively; inhibits esterolytic activity translates into potent inhibition of the proteolytic activity of C1s, factor D, and consequently of the classical and alternative pathway-mediated hemolysis of target RBC (IC50=46 nM and 330 nM, respectively); blocks the reverse passive Arthus (RPA) reaction in rats.

GY05433

UK-396082

400044-47-5

UK-396082 is a potent and selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (activated TAFI; TAFIa) with Ki of 10 nM; displays excellent selectivity over plasma carboxypeptidase N (>1,000-fold); exhibits antithrombotic efficacy in a rabbit model of venous thrombosis, yet has no effect on surgical bleeding in the rabbit; possesses excellent preclinical and clinical pharmacokinetic profile, and shows potential for the treatment of thrombosis and other fibrin-dependent diseases in humans.

GY05211

Otamixaban

193153-04-7

A potent and selective factor Xa (FXa) inhibitor with Ki of 0.4 nM; shows >1,000-fold selectivity over thrombin, activated protein C (aPC), plasmin, and tissue-plasminogen activator (t-PA); dose-dependently prolongs the time to vessel occlusion and inhibits thrombus formation in canine models of thrombosis.

GY04201

Edoxaban

480449-70-5

A potent and orally active Factor Xa inhibitor with Ki of 0.561 nM; also inhibits prothrombinase (Ki=2.98 nM), weakly inhibits thrombin and FIXa (Ki=6.0 uM, and 41.7 uM); exhibits >10,000-fold selectivity for Fxa over FVIIa/sTF, FXIa, tPA, aPC, trypsin, plasmin and chymotrypsin; inhibits thrombus formation in rat and rabbit thrombosis models.

GY04197

Vorapaxar

618385-01-6

A potent, selective and orally active thrombin receptor PAR-1 antagonist with Ki of 8.1 nM; displays no activity against e PAR-2, PAR-3 and PAR-4, and no CYP450 enzyme inhibition potential; inhibits thrombin (10 nM) induced human platelet aggregation with IC50 of 47 nM; inhibits haTRAP-induced platelet aggregation in vivo.

GY04066

Tirofiban

144494-65-5

A potent, selective inhibitor of the platelet fibrinogen receptor GPIIb/IIIa with IC50 of 9 nM, inhibition of platelet aggregation; displays > 24,000-fold over human umbilical vein endothelial cell fibrinogen receptors; inhibits ex vivo platelet aggregation induced by ADP in anesthetized dogs.

GY05344

AZD-8165

1201686-72-7

AZD-8165 is a potent, selective and oral thrombin inhibitor for treatment of thrombosis.

GY05285

BMS-962212

1430114-34-3

BMS-962212 is a potent, highly selective and reversible small molecule coagulation Factor XIa (FXIa) inhibitor with Ki of 0.7 nM; displays an excellent protease selectivity profile, including thrombin, Factor Xa/VIIa/IXa/XIIa, plasma or tissue kallikrein; shows excellent preclinical efficacy in thrombosis models and aqueous solubility suitable for intravenous administration.

Request The Product List

* Indicates a Required FieldYour information is safe with us.

  • *Product List:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Country:
  • Additional Information:
© Copyright 2020 RayStarBio. All Rights Reserved. Products are only for research use