Collagen-IN-1 (compound 3) is an ortho-carbonyl hydroquinone derivative exhibiting selective inhibition of collagen. It non-competitively inhibits agonist-induced platelet aggregation, with an IC50 value of 1.77 μM. Collagen-IN-1 effectively reduces the expression of P-selectin, activation of glycoproteinIIbIIIa, and release of adenosine triphosphate and CD63 from platelets. This compound holds promise for research into platelet-related thrombosis diseases [1].
Fradafiban binds to the human platelet GP IIbIIIa complex with a Kd value of 148 nM. Fradafiban is a non-polypeptide platelet glycoproteinIIbIIIa antagonist.
AR-H067637 is a rapid-binding, reversible and potent (inhibition constant K(i) = 2-4 nM), competitive inhibitor of thrombin, as well as of thrombin bound to fibrin (clot-bound thrombin) or to thrombomodulin. The total amount of free thrombin generated in
Variabilin, a novel inhibitor of human platelet aggregation, it is a potent RGD (Arg-Gly-Asp)-containing antagonist of the fibrinogen receptor glycoproteinIIb-IIIa (GPIIb-IIIa; αIIbβ3) and the vitronectin receptor αvβ3.Variabilin is also an antimicrobial furanosesterterpene. Variabilin is an inhibitor of human secretory and cytosolic phospholipase A2 (PLA2) activities that controls eicosanoid production in vitro and in vivo, inhibits neutrophil degranulation and superoxide generation in vitro and shows anti-inflammatory activity after topical or p.o. administration to mice.
Potent irreversible αVβ3 integrin antagonist (Ki = 0.27 nM). Disrupts attachment of osteoclasts to bone and inhibits bone reabsorption (IC50 = 0.1 nM). Prevents ADP-induced platelet aggregation via inhibition of glycoproteinIIbIIIa (GpIIbIIIa, αIIbβ3)