PH-002
Based on 1 Customer Validation
PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells that could rescue impairments of mitochondrial motility and neurite outgrowth.
For research use only. We do not sell to patients.
- Purity: 98.48%
- CAS No.: 1311174-68-1
- Formula: C27H33N5O4
- Molecular Weight:491.58
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
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apoE |
PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells, with an IC50 of 116 nM in FRET[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1311174-68-1
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Appearance Solid
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Molecular Weight 491.58
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Formula C27H33N5O4
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Color White to off-white
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SMILES
O=C(N1CCN(CC2=CC=C(NC(CC3=NN(C)C(C4=C3C=CC=C4)=O)=O)C=C2)CC1)OC(C)(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : ≥ 75 mg/mL (152.57 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.09 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Protocol
Neuro-2a cells stably expressing apoE3 or apoE4 are seeded at 7500-8000 cells/well on PLlysine-coated 24-well plates containing Opti-MEM with either 0.03% DMSO (control) or DMSO plus compound PH-002 (100 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Brodbeck J, et al. Structure-dependent impairment of intracellular apolipoprotein E4 trafficking and its detrimental effects are rescued by small-molecule structure correctors. J Biol Chem. 2011 May 13;286(19):17217-26. [Content Brief]
[2]. Chen HK, et al. Small molecule structure correctors abolish detrimental effects of apolipoprotein E4 in cultured neurons. J Biol Chem. 2012 Feb 17;287(8):5253-66. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0343 mL | 10.1713 mL | 20.3426 mL | 50.8564 mL |
| 5 mM | 0.4069 mL | 2.0343 mL | 4.0685 mL | 10.1713 mL | |
| 10 mM | 0.2034 mL | 1.0171 mL | 2.0343 mL | 5.0856 mL | |
| 15 mM | 0.1356 mL | 0.6781 mL | 1.3562 mL | 3.3904 mL | |
| 20 mM | 0.1017 mL | 0.5086 mL | 1.0171 mL | 2.5428 mL | |
| 25 mM | 0.0814 mL | 0.4069 mL | 0.8137 mL | 2.0343 mL | |
| 30 mM | 0.0678 mL | 0.3390 mL | 0.6781 mL | 1.6952 mL | |
| 40 mM | 0.0509 mL | 0.2543 mL | 0.5086 mL | 1.2714 mL | |
| 50 mM | 0.0407 mL | 0.2034 mL | 0.4069 mL | 1.0171 mL | |
| 60 mM | 0.0339 mL | 0.1695 mL | 0.3390 mL | 0.8476 mL | |
| 80 mM | 0.0254 mL | 0.1271 mL | 0.2543 mL | 0.6357 mL | |
| 100 mM | 0.0203 mL | 0.1017 mL | 0.2034 mL | 0.5086 mL |