gpvi

Adrenalone hydrochloride (Adrenalone HCl) 是一种多巴胺β氧化酶 (dopamine β oxidase) 抑制剂，结构与去甲肾上腺素转运蛋白 (NET) 配体相似，IC50=36.9 μM。它是一种肾上腺素能 (adrenergic) 激动剂，用作局部血管收缩剂和止血剂。

Glaucocalyxin A (Leukamenin F) 是来自日本黑纹病菌的一种对映型月桂基二萜，具有抗肿瘤作用。它通过调节PI3K Akt 信号通路抑制 GLI1 的核易位，诱导骨肉瘤凋亡。

Glenzocimab (ACT017) 是人源化抗 GPVI 单克隆抗体的 Fab 片段。Glenzocimab 在缺血性卒中模型对胶原诱导的血小板聚集显示出抑制作用。Glenzocimab 具有研究急性缺血性脑卒中和脑血栓。

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 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。

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 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].

Asebogenin 是从丹参中分离出来的化合物，具有抗真菌活性，对GPVI 诱导的血小板反应有抑制作用，抑制促炎刺激诱导的 NET 形成。

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) 是 Syk 的抑制剂，EC50 为 313 nM，IC50 为 14 nM。 OXSI-2 完全抑制适配器蛋白 LAT Y191 磷酸化和 Syk 介导的血小板聚集。