1. Metabolic Enzyme/Protease
  2. Phospholipase
  3. LFHP-1c

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.

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LFHP-1c Chemical Structure

LFHP-1c Chemical Structure

CAS No. : 2102347-47-5

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1 mg USD 140 In-stock
5 mg USD 350 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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 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.

Immunofluorescence[1]

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.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

873.13

Formula

C55H64N6O4

CAS No.
Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1453 mL 5.7265 mL 11.4530 mL
5 mM 0.2291 mL 1.1453 mL 2.2906 mL
View the 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.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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.

  • Protocol 1

    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

  • Protocol 2

    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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 98.07%

References

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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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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LFHP-1c
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HY-139598
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