gpvi

GPVI antagonist 2 (Compound 1) is a potential Glycoprotein VI (GPVI) antagonist, showing activity against collagen (IC50: 0.35 μM), CRP (IC50: 0.80 μM), convulxin (IC50: 195.2 μM), and thrombin (IC50: 81.38 μM), and is a promising anti-platelet agent.

GPVI antagonist 3 (Compound 2) is a promising antiplatelet agent that selectively inhibits the interaction between the Glycoprotein VI (GPVI) receptor and its ligands. It demonstrates potent inhibitory effects with IC50 values of 1.01 μM for collagen, 1.92 μM for CRP, 7.24 μM for convulxin, and 51.74 μM for thrombin, positioning it as a potential novel antithrombotic treatment [1].

GPVI antagonist 1 (compound 5) functions as an antagonist for the glycoprotein VI (GPVI) platelet receptor, effectively inhibiting collagen-induced platelet aggregation with an IC50 value of 25.3 μM [1].

Asebogenin is a compound fractionated from Salvia miltiorrhiza with antifungal activity, inhibition of GPVI-induced platelet reactions, and inhibition of NET formation induced by pro-inflammatory stimuli.

Adrenalone hydrochloride (Adrenalone HCl) is a dopamine β-oxidase inhibitor with a similar structure to the norepinephrine transporter (NET) ligand, with an IC50 of 36.9 μM. It is an adrenergic agonist that acts as a local vasoconstrictor and hemostatic agent.

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.

Glenzocimab (ACT017), a Fab fragment of a humanized anti-GPVI monoclonal antibody, demonstrated inhibition of collagen-induced platelet aggregation in an ischemic stroke model and has been studied in acute ischemic stroke and cerebral thrombosis.

Lanraplenib succinate inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans. Lanraplenib succinate is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases.

Lanraplenib monosuccinate inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans. Lanraplenib monosuccinate is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases.

OXSI-2 (Syk Inhibitor) is an inhibitor of Syk with an EC50 of 313 nM and an IC50 of 14 nM. OXSI-2 completely inhibits Adaptor protein LAT Y191 phosphorylation and Syk mediated events in platelets.

Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) being developed for treating inflammatory diseases. It inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.