glycoprotein vi

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.

Lanraplenib (GS-9876) 是高效的、选择性的、口服具有活力的 SYK 抑制剂 (IC50=9.5 nM) ，能够用于炎症性疾病的研究。它通过糖蛋白 VI (GPVI) 受体抑制血小板中的 SYK 活性，而不会延长猴子或人类的出血时间 (BT)。

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

GPVI antagonist 3 (Compound 2) is a potential antagonist that shows promising antiplatelet activity by selectively inhibiting 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. GPVI is a major collagen receptor on platelets, making it an ideal target for safe and effective antithrombotic treatment. Therefore, GPVI antagonist 3 holds potential as a novel antiplatelet agent [1].

GPVI antagonist 2 (Compound 1) 是一种潜在的 Glycoprotein VI (GPVI) 拮抗剂，能够作用于胶原蛋白 (IC50: 0.35 μM)、CRP (IC50: 0.80 μM)、convulxin (IC50: 195.2 μM)、凝血酶 (IC50: 81.38 μM)。其中糖蛋白 VI (GPVI) 是一种血小板主要胶原受体，是有效的、安全的抗血栓研究靶点。GPVI antagonist 2 是一种很有前途的抗血小板药物。

pep-10L peptide 是一种糖蛋白 VI (Glycoprotein VI, GPVI) 拮抗剂，其对 CPR、GPO-1 和 Type1collagen 的 Ki 值分别为 180、225 和 179 μM。pep-10L peptide 展示了抗血栓形成的作用。