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| ln Vitro |
In rat brain microvascular endothelial cells (rBMECs), treatment with LFHP-1c (1, 2 or 5 μmol/L; 9 h) followed by hypoxia enhanced NRF2 protein expression and encouraged NRF2 nuclear translocation [1].
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| ln Vivo |
In rats, LFHP-1c (5 mg/kg; i.v.; 2 doses) inhibits disruption of the blood brain barrier after temporary middle cerebral artery occlusion (tMCAO)[1]. Through the PGAM5-NRF2 axis, LFHP-1c (3 mg/kg, 1 mL/kg; intravenous injection; 8 doses) reduces cerebral ischemia damage in the fascicularis tMCAO model[1].
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| Cell Assay |
Immunofluorescence[1]
Cell Types: Primary rat brain microvascular endothelial cells (rBMECs) Tested Concentrations: 2 μmol/L Incubation Duration: 1 h Experimental Results: Bound to PGAM5, to facilitate nuclear translocation of NRF2. |
| Animal Protocol |
Animal/Disease Models: Nonhuman primate Macaca fascicularis model with tMCAO[1]
Doses: 3 mg/kg, 1 mL/kg Route of Administration: IV; at 4 h, 1, 2, 3, 4, 5, 6 and 7 days after tMCAO onset. Experimental Results: decreased infarct volume, brain edema and neurological deficits in Transient MCAO model in M. fascicularis. Animal/Disease Models: SD rats (230-250 g)[1] Doses: 1 mg/kg, 5 mg/kg in 0.5 mL volume Route of Administration: IV; injected at 4 or 12 h after ischemia onset, and then injected another time at 24 h post-ischemia Experimental Results: 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.
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| Molecular Formula |
C55H64N6O4
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|---|---|
| Molecular Weight |
873.13
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| CAS # |
2102347-47-5
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (114.53 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (2.86 mM) in 10% DMSO 20% HS-15 70% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1145 mL | 0.5727 mL | 1.1453 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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