LFHP-1c
Based on 3 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.01%
- No. CAS: 2102347-47-5
- Fòrmula: C55H64N6O4
- Peso molecular:873.13
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) LFHP-1c
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Actividad biológica
Descripciòn
In Vitro
LFHP-1c (1, 2, or 5 μmol/L; 9 h) treatment, and followed by hypoxic treatment, increases NRF2 protein expression and facilitates nuclear translocation of NRF2 in primary rat brain microvascular endothelial cells (rBMECs)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Primary rat brain microvascular endothelial cells (rBMECs)
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Concentration:2 μmol/L
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Incubation Time:1 h
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Result:Bound to PGAM5, to facilitate nuclear translocation of NRF2.
In Vivo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nonhuman primate Macaca fascicularis model with tMCAO[1]
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Dosage:3 mg/kg, 1 mL/kg
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Administration:IV; at 4 h, 1, 2, 3, 4, 5, 6 and 7 days after tMCAO onset.
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Result:Reduced infarct volume, brain edema and neurological deficits in Transient MCAO model in M. fascicularis.
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Animal Model:SD rats (230-250 g)[1]
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Dosage:1 mg/kg, 5 mg/kg in 0.5 mL volume
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Administration:IV; injected at 4 or 12 h after ischemia onset, and then injected another time at 24 h post-ischemia
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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.
Chemical Information
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No. CAS 2102347-47-5
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Appearance Solid
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Peso molecular 873.13
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Fòrmula C55H64N6O4
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Color White to off-white
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SMILES
O=C(C)OC(CCCC)C1=C(C(NCCCCCCCCNC(C2=C(C3=CC=C(CN4C5=CC(C6=NC7=C(N6C)C=CC=C7)=CC(C)=C5N=C4CCC)C=C3)C=CC=C2)=O)=O)C=CC=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Nature
2026 Mar;651(8105):451-461. PMID: 41535474
LFHP-1c purchased from MedChemExpress. Usage Cited in: Nature. 2026 Mar;651(8105):451-461. [Abstract]
WT and KO OT-I T cells were activated and cultured for 3 days in vitro, then treated with DMSO or the PGAM5 inhibitor LFHP-1c (P5i, 2 μM) for another 3 days before analysis. Immunoblotting of Mfn2, Opa1, Drp1, p-Drp1S637, PGAM5, and Actin.
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Free Radic Biol Med
Targeting PGAM5 attenuates airway inflammation in asthma by inhibiting HMGB1 release in bronchial epithelium. [Abstract]2025 Feb 16:228:207-220. PMID: 39756489 -
Cancers (Basel)
2025 May 6;17(9):1573. PMID: 40361499
LFHP-1c purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2025 May 6;17(9):1573. [Abstract]
Treatment of the hepatoma and hepatocellular carcinoma cell lines, HepG2 and HuH7, respectively, with the novel PGAM5 inhibitor LFHP-1c (0-10 μM, 0-25 h) inhibited cell growth after 24 h at all concentrations tested.
LFHP-1c purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2025 May 6;17(9):1573. [Abstract]
Twenty-four-hour exposure to LFHP-1c (0-10 μM) significantly attenuated viability in both cell lines at all concentrations tested compared to DMSO-treated control cells.
LFHP-1c purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2025 May 6;17(9):1573. [Abstract]
In HepG2 cells, NRF2 expression significantly decreased after a 24 h exposure to LFHP-1c at 2 μM.
LFHP-1c purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2025 May 6;17(9):1573. [Abstract]
NRF2 protein expression in HuH7 cells treated with DMSO (0 μM) or LFHP-1c (2 µM) for 3, 6, 9, 12, or 24 h was determined by immunoblot.
LFHP-1c purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2025 May 6;17(9):1573. [Abstract]
HepG2 and HuH7 cells were treated with LFHP-1c (0, 2, 4, 6, 8, or 10 μM) at 0 h. ROS was quantified at 24 h. Values were normalized to the 0 h measurement.
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (114.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 20% HS-15 70% Saline
Solubility: 2.5 mg/mL (2.86 mM); Suspended solution; Need ultrasonic
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1453 mL | 5.7265 mL | 11.4530 mL | 28.6326 mL |
| 5 mM | 0.2291 mL | 1.1453 mL | 2.2906 mL | 5.7265 mL | |
| 10 mM | 0.1145 mL | 0.5727 mL | 1.1453 mL | 2.8633 mL | |
| 15 mM | 0.0764 mL | 0.3818 mL | 0.7635 mL | 1.9088 mL | |
| 20 mM | 0.0573 mL | 0.2863 mL | 0.5727 mL | 1.4316 mL | |
| 25 mM | 0.0458 mL | 0.2291 mL | 0.4581 mL | 1.1453 mL | |
| 30 mM | 0.0382 mL | 0.1909 mL | 0.3818 mL | 0.9544 mL | |
| 40 mM | 0.0286 mL | 0.1432 mL | 0.2863 mL | 0.7158 mL | |
| 50 mM | 0.0229 mL | 0.1145 mL | 0.2291 mL | 0.5727 mL | |
| 60 mM | 0.0191 mL | 0.0954 mL | 0.1909 mL | 0.4772 mL | |
| 80 mM | 0.0143 mL | 0.0716 mL | 0.1432 mL | 0.3579 mL | |
| 100 mM | 0.0115 mL | 0.0573 mL | 0.1145 mL | 0.2863 mL |
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