(Tos-GPR)2-[Rh110] – Fluorescent Peptides

Fluorogenic substrate for thrombin that when in its intact state does not fluoresce, however upon cleavage by thrombin in 2 successive steps, Rhodamine 110 is released to allow fluorescence. Thrombin is a multifunctional serine protease and is the principal enzyme of hemostasis. It catalyzes the conversion of fibrinogen to fibrin and activates procoagulant factors V, VIII, XI, and XIII. When bound to thrombomodulin, it activates protein C, an anticoagulant zymogen. Thrombin also activates platelets, regulates endothelial cell function, and has a host of direct actions on other cells. Thrombin has been found to act as a mediator of vascular dysfunction and inflammation in both the peripheral and the central nervous systems. Thrombin contributes to the development of cardiovascular disease, atherosclerosis and diabetes and promotes vascular dysfunction, inflammation, and neurodegeneration. Thrombin is elevated in the brains of people with Alzheimer’s disease (AD) and therefore may be a therapeutic target in AD.