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.
Odiparcil is an orally active beta-d-thioxyloside analog. Odiparcil is an indirect thrombin inhibitor that exerts its anticoagulant effect through activation of antithrombin II (heparin cofactor II). It also has an antithrombotic activity associated with a reduced risk of adverse bleeding events.
1,2,3,4,7,8-Hexachlorodibenzo-p-dioxin 是一种多氯二苯并二恶英 (PCDD) 同源物。在最高剂量 (10,000 μg kg) 下,该化合物可导致 H W 和 A 系大鼠肝脏苍白 (脂肪肝)、胃肠道出血和早期死亡。此外,1,2,3,4,7,8-Hexachlorodibenzo-p-dioxin 还会引起肝窦扩张,甚至导致 B 系大鼠严重紫癜。
Gemeprost, an analog of prostaglandin E1, is used for the treatment of obstetric bleeding. It is used to terminate pregnancy up to 24 weeks gestation together with mifepristone.
MRS2179 is a competitive P2Y1 receptor antagonist (Kb = 100 nM) with no appreciable activity at P2Y2, P2Y4, or P2Y6 at concentrations up to 30 µM, or at P2Y12 and P2Y13. It inhibits ADP-induced platelet shape change and aggregation (pA2 = 6.55) in vitro a
Onapristone, a progesterone receptor antagonist, is used potentially for the treatment of breast cancer, advanced prostate cancer, and inducer of vaginal bleeding.
R-1663 is a factor Xa inhibitor. R-1663 prolonged clotting times, inhibited thrombin generation (peak height and endogenous thrombin potential [ETP]) and anti-factor Xa activity in a concentration-dependent manner without increasing bleeding time. Pharmac
Aspalatone is an anti-platelet aggregator (IC50 = 180 μM, in vitro) that prolongs bleeding time significantly in a rodent model of thromboembolism. Additionally at a minimal effective dose of 24 mg/kg, aspalatone generates antioxidant and neuroprotective effects against kainic acid-induced epilepsy in rat hippocampus.