产品
编 号:F762431
分子式:C55H64N6O4
分子量:873.13
产品类型
结构图
CAS No: 2102347-47-5
联系客服
产品详情
生物活性:
LFHP-1c is an PGAM5 inhibitor with neuroprotective activity in brain ischemic stroke. LFHP-1c protects blood-brain barrier integrity from ischemia-induced injury. LFHP-1c binds to endothelial PGAM5 to inhibit the activity of PGAM5 phosphatase and the interaction of PGAM5 with NRF2. LFHP-1c exhibits in vitro and in vivo protection.
体内研究:
LFHP-1c (5 mg/kg;静脉注射;2 剂) 可防止大鼠大脑中动脉短暂性阻塞 (tMCAO) 后的 BBB 破坏。LFHP-1c (3 mg/kg,1 mL/kg;静脉注射;8 剂) 通过 PGAM5-NRF2 轴改善束状肌 tMCAO 模型的脑缺血损伤。Animal Model:Nonhuman primate Macaca fascicularis model with tMCAO
Dosage:3 mg/kg, 1 mL/kg
Administration:IV; at 4 h, 1, 2, 3, 4, 5, 6 and 7 days after tMCAO onset.
Result:Reduced infarct volume, brain edema and neurological deficits in Transient MCAO model in M. fascicularis.
Animal Model:SD rats (230-250 g)
Dosage:1 mg/kg, 5 mg/kg in 0.5 mL volume
Administration:IV; injected at 4 or 12 h after ischemia onset, and then injected another time at 24 h post-ischemia
Result:Dose-dependently protected rat brains against ischemia/reperfusion injury at 72 h after ischemia onset with a moderate therapeutic window.Prevented BBB disruption and attenuated endothelial inflammation in rat cerebral microvessels at 72 h after ischemia onset.
体外研究:
LFHP-1c (1、2 或 5 μmol/L;9 h) 先处理,然后再缺氧处理,在大鼠脑微血管内皮细胞 (rBMECs) 中增加了 NRF2 蛋白表达,促进 NRF2 的核易位。