| Bioactivity | 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[1]. | ||||||||||||
| Invitro | 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[1]。 Immunofluorescence[1] Cell Line: | ||||||||||||
| In Vivo | 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[1]。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[1]。 Animal Model: | ||||||||||||
| Name | LFHP-1c | ||||||||||||
| CAS | 2102347-47-5 | ||||||||||||
| Formula | C55H64N6O4 | ||||||||||||
| Molar Mass | 873.13 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Gao C, et al. A novel PGAM5 inhibitor LFHP-1c protects blood-brain barrier integrity in ischemic stroke. Acta Pharm Sin B. 2021 Jul;11(7):1867-1884. |