BRI-50460
Based on 1 Customer Validation
BRI-50460 is a brain-penetrant selective cPLA2 inhibitor with an IC50 of 0.88 nM. BRI-50460 inhibits cPLA2 to modulate downstream inflammatory lipid signaling pathways, attenuating Aβ42 oligomer-induced synaptic loss and tau hyperphosphorylation, thereby exerting effects of modulating neuroinflammation and restoring lipid homeostasis. BRI-50460 can be used in research in the fields of Alzheimer's disease and other neurodegenerative diseases.
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- Pureté : 99.62%
- Formule: C21H18N2O4S
- Masse moléculaire:394.44
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
cPLA2 0.88 nM (IC50) |
In Vitro
BRI-50460 (up to 1 μM) shows no cytotoxicity in HEK293 and HMC3 cells[1].
BRI-50460 (up to 50 μM; 10-30 min) shows no inhibitory activity against the non-target enzyme iPLA2 in biochemical assays of lysates from cells expressing iPLA2 (demonstrating extremely high cPLA2 selectivity, with a selectivity window of > 100-fold)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human iPSC-derived astrocytes (APOE ε3/ε3)
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Concentration:0.1, 1 μM (BRI-50460); 2.5 μM (Aβ42O)
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Incubation Time:30 min (BRI-50460 pre-incubation); 72 h (Aβ42O)
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Result:Reduced Aβ-related increases in cPLA2 levels and caused a reduction in phosphorylated cPLA2 at 1 μM.
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Cell Line:human iPSC-derived neuron/astrocyte mixed culture (APOE3/3)
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Concentration:1 μM (BRI-50460); 2.5 μM (Aβ42O)
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Incubation Time:72 h
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Result:Reduced Aβ42O-induced increases in phospho-cPLA2α(Ser505) and phospho-tau (Ser202/Thr205) in human neurons.
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Cell Line:human iPSC-derived neuron/astrocyte mixed culture (APOE4/4)
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Concentration:1 μM (BRI-50460); 2.5 μM (Aβ42O)
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Incubation Time:72 h
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Result:Protected the cells from Aβ42O-induced reductions of synaptic puncta stained by synapsin and dendritic density (occupied area) stained by CamKIIα and MAP2.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Masse moléculaire 394.44
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Formule C21H18N2O4S
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Color White to off-white
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SMILES
O=C(CC1)NC2=C1C=CC(NS(C3=CC=CC(OC4=CC=CC=C4)=C3)(=O)=O)=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (253.52 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.34 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
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.
Pureté et documentation
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Fiche technique (280 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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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 2.5352 mL | 12.6762 mL | 25.3524 mL | 63.3810 mL |
| 5 mM | 0.5070 mL | 2.5352 mL | 5.0705 mL | 12.6762 mL | |
| 10 mM | 0.2535 mL | 1.2676 mL | 2.5352 mL | 6.3381 mL | |
| 15 mM | 0.1690 mL | 0.8451 mL | 1.6902 mL | 4.2254 mL | |
| 20 mM | 0.1268 mL | 0.6338 mL | 1.2676 mL | 3.1690 mL | |
| 25 mM | 0.1014 mL | 0.5070 mL | 1.0141 mL | 2.5352 mL | |
| 30 mM | 0.0845 mL | 0.4225 mL | 0.8451 mL | 2.1127 mL | |
| 40 mM | 0.0634 mL | 0.3169 mL | 0.6338 mL | 1.5845 mL | |
| 50 mM | 0.0507 mL | 0.2535 mL | 0.5070 mL | 1.2676 mL | |
| 60 mM | 0.0423 mL | 0.2113 mL | 0.4225 mL | 1.0563 mL | |
| 80 mM | 0.0317 mL | 0.1585 mL | 0.3169 mL | 0.7923 mL | |
| 100 mM | 0.0254 mL | 0.1268 mL | 0.2535 mL | 0.6338 mL |
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