Phenserine
Based on 1 Customer Validation
Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine (HY-N6608) and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.55%
- CAS No.: 101246-66-6
- Formule: C20H23N3O2
- Masse moléculaire:337.42
-
Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
-
Neuronal Signaling Compound Library
HY-L013
-
Clinical Compound Library
HY-L026
-
Drug Repurposing Compound Library
HY-L035
-
Anti-Alzheimer's Disease Compound Library
HY-L069
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Protein-protein Interaction Inhibitor Library
HY-L109
-
Heterocyclic Compound Library
HY-L138
-
Membrane Protein-targeted Compound Library
HY-L149
-
Highly Selective Inhibitors Library
HY-L158
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
Activité biologique
|
AChE |
Phenserine (1-25 μM; 48 hours; CHO APP751SW cells) treatment CHO APP751SW cell shows 18.6% reduction in cells treated with 10 μM of Phenserine, while 25 μM concentration of Phenserine reduces APP level by 51.4%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:CHO APP751SW cells
-
Concentration:1 μM, 2.5 μM, 5 μM, 10 μM, 25 μM
-
Incubation Time:48 hours
-
Result:8.6% reduction in cells treated with 10 μM, while 25 μM concentration reduces APP level by 51.4%.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male Fischer-344 rats (5 months old) induced by scopolamine[3]
-
Dosage:1 mg/kg, 2 mg/kg, 4 mg/kg
-
Administration:Intraperitoneal injection; for 4 days
-
Result:Improved morris water maze performance of scopolamine-treated rats..
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 101246-66-6
-
Appearance Solid
-
Masse moléculaire 337.42
-
Formule C20H23N3O2
-
Color Off-white to yellow
-
SMILES
CN1[C@](N(C)CC2)([H])[C@]2(C)C3=C1C=CC(OC(NC4=CC=CC=C4)=O)=C3
-
Synonyms
(-)-Eseroline phenylcarbamate; (-)-Phenserine
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 200 mg/mL (592.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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)
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: ≥ 5 mg/mL (14.82 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (14.82 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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
-
Fiche technique (276 KB)
-
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)
- Portuguese - PT (393 KB)
-
Instruction de manipulation (2659 KB)
Références
[1]. Klein J. Phenserine. Expert Opin Investig Drugs. 2007 Jul;16(7):1087-97. [Content Brief]
[2]. Asuni AA, et al. Modulation of amyloid precursor protein expression reduces β-amyloid deposition in a mouse model. Ann Neurol. 2014 May;75(5):684-99. [Content Brief]
[3]. Janas AM, et al. The cholinesterase inhibitor, phenserine, improves Morris water maze performance of scopolamine-treated rats. Life Sci. 2005 Jan 21;76(10):1073-81. [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, 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 | 2.9637 mL | 14.8183 mL | 29.6367 mL | 74.0916 mL |
| 5 mM | 0.5927 mL | 2.9637 mL | 5.9273 mL | 14.8183 mL | |
| 10 mM | 0.2964 mL | 1.4818 mL | 2.9637 mL | 7.4092 mL | |
| 15 mM | 0.1976 mL | 0.9879 mL | 1.9758 mL | 4.9394 mL | |
| 20 mM | 0.1482 mL | 0.7409 mL | 1.4818 mL | 3.7046 mL | |
| 25 mM | 0.1185 mL | 0.5927 mL | 1.1855 mL | 2.9637 mL | |
| 30 mM | 0.0988 mL | 0.4939 mL | 0.9879 mL | 2.4697 mL | |
| 40 mM | 0.0741 mL | 0.3705 mL | 0.7409 mL | 1.8523 mL | |
| 50 mM | 0.0593 mL | 0.2964 mL | 0.5927 mL | 1.4818 mL | |
| 60 mM | 0.0494 mL | 0.2470 mL | 0.4939 mL | 1.2349 mL | |
| 80 mM | 0.0370 mL | 0.1852 mL | 0.3705 mL | 0.9261 mL | |
| 100 mM | 0.0296 mL | 0.1482 mL | 0.2964 mL | 0.7409 mL |
Powered by Bioz