| Identification | Back Directory | [Name]
[1,1'-Biphenyl]-2-carboxamide, N-[8-[[2-[1-(acetyloxy)pentyl]benzoyl]amino]octyl]-4'-[(1,4'-dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]- | [CAS]
2102347-47-5 | [Synonyms]
LFHP-1c
[1,1'-Biphenyl]-2-carboxamide, N-[8-[[2-[1-(acetyloxy)pentyl]benzoyl]amino]octyl]-4'-[(1,4'-dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]- | [Molecular Formula]
C55H64N6O4 | [MOL File]
2102347-47-5.mol | [Molecular Weight]
873.13 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
LFHP-1c (5 mg/kg; iv; 2 doses) prevents BBB disruption after transient middle cerebral artery occlusion (tMCAO) in rats[1].
LFHP-1c (3 mg/kg, 1 mL/kg; iv; 8 doses) ameliorates brain ischemic injury in tMCAO model of M. fascicularis through PGAM5–NRF2 axis[1].
| Animal Model: | Nonhuman primate Macaca fascicularis model with tMCAO[1] | | 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)[1] | | 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. |
| [References]
[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. DOI:10.1016/j.apsb.2021.01.008 |
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