LFHP-1c

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LFHP-1c 是一种 PGAM5 抑制剂，在缺血性脑卒中中具有神经保护活性。LFHP-1c 保护血脑屏障完整性免受缺血损伤。LFHP-1c 与内皮细胞 PGAM5 结合，抑制 PGAM5 磷酸酶活性，抑制 PGAM5 与 NRF2 的相互作用。LFHP-1c 具有体外和体内保护作用。

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.

Immunofluorescence Cell Line:Primary rat brain microvascular endothelial cells (rBMECs)Concentration:2 μmol/L Incubation Time:1 h Result:Bound to PGAM5, to facilitate nuclear translocation of NRF2.

Animal Model:Nonhuman primate Macaca fascicularis model with tMCAODosage:3 mg/kg, 1 mL/kgAdministration: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.

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Metabolic Enzyme/Protease

Phosphatase

Phosphatase

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2102347-47-5

873.13

C55H64N6O4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (114.53 mM; 超声助溶 )

O=C(OC(C=1C=CC=CC1C(=O)NCCCCCCCCNC(=O)C=2C=CC=CC2C=3C=CC(=CC3)CN4C5=CC(=CC(=C5N=C4CCC)C)C6=NC=7C=CC=CC7N6C)CCCC)C

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(-20℃)

With Ice Pack

≥ 2 years