Edonerpic maleate
Based on 1 Customer Validation
Edonerpic maleate is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ).
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- Purity: 99.02%
- CAS No.: 519187-97-4
- 화학식: C20H25NO6S
- 분자량:407.48
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Biological Activity
amyloid-β peptides[1]
Edonerpic maleate (T-817MA) treatment preserves the cortical neurons in the presence of Aβ(1-42). Twenty-four hours of pretreatment, followed by the continuous presence of Edonerpic maleate, prevents oxidative stress-induced neuronal death at 0.1 and 1 μM. Edonerpic maleate almost completely prevents GSH reduction at 0.1 and 1 μM. Hippocampal slices with 1 μM Edonerpic maleate treatment generate more and much longer neurites than control slices. Edonerpic maleate significantly increases the neurite length at 0.1 and 1 μM[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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 519187-97-4
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Appearance Solid
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분자량 407.48
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화학식 C20H25NO6S
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Color White to off-white
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SMILES
OC1CN(CCCOCCC2=CC=C3C(C=CS3)=C2)C1.O=C(O)/C=C\C(O)=O
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Synonyms
T-817 maleate; T-817MA
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : 100 mg/mL (245.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 100 mg/mL (245.41 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (6.14 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 140 mg/mL (343.58 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
A cortical neuron/glia coculture is prepared. Edonerpic maleate (T-817MA) is added to the cocultures at concentrations of 0 (control), 0.01, 0.1, and 1 μM, and the cells are subsequently incubated for 5 min or 24 h. H2O2 is then added to the coculture at a concentration of 100 μM, and the cells are incubated for another 24 h. For the normal group, the preparations are maintained in the medium with neither Edonerpic maleate nor H2O2. Neuronal cell viability is quantified by measuring the Monoclonal anti-microtubule-associated protein 2 (MAP2) immunoreactivity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Wistar rats (7 weeks, n=47) are used in this study. All rats are given food and water ad libitum in a clear cage and handled on three consecutive days before start of the experiments. The housing area is provided a temperature-controlled environment under a 12/12 h light cycle. These rats are divided into five groups: vehicle (n=11), Aβ infusion control (n=10), Aβ infusion+high-dose Edonerpic maleate (T-817MA) (8.4 mg/kg) (n=11), Aβ infusion+low-dose Edonerpic maleate (0.84 mg/kg) (n=9) and Aβ infusion+donepezil (0.5 mg/kg) (n=7)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Hirata K, et al. A novel neurotrophic agent, T-817MA [1-{3-[2-(1-benzothiophen-5-yl) ethoxy] propyl}-3-azetidinol maleate], attenuates amyloid-beta-induced neurotoxicity and promotes neurite outgrowth in rat cultured central nervous system neurons. J Pharmacol Exp Ther. 2005 Jul;314(1):252-9. [Content Brief]
[2]. Kimura T, et al. T-817MA, a neurotrophic agent, ameliorates the deficits in adult neurogenesis and spatial memory in rats infused i.c.v. with amyloid-beta peptide. Br J Pharmacol. 2009 Jun;157(3):451-63. [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 (sealed storage, away from moisture). 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 / H2O | 1 mM | 2.4541 mL | 12.2705 mL | 24.5411 mL | 61.3527 mL |
| 5 mM | 0.4908 mL | 2.4541 mL | 4.9082 mL | 12.2705 mL | |
| 10 mM | 0.2454 mL | 1.2271 mL | 2.4541 mL | 6.1353 mL | |
| 15 mM | 0.1636 mL | 0.8180 mL | 1.6361 mL | 4.0902 mL | |
| 20 mM | 0.1227 mL | 0.6135 mL | 1.2271 mL | 3.0676 mL | |
| 25 mM | 0.0982 mL | 0.4908 mL | 0.9816 mL | 2.4541 mL | |
| 30 mM | 0.0818 mL | 0.4090 mL | 0.8180 mL | 2.0451 mL | |
| 40 mM | 0.0614 mL | 0.3068 mL | 0.6135 mL | 1.5338 mL | |
| 50 mM | 0.0491 mL | 0.2454 mL | 0.4908 mL | 1.2271 mL | |
| 60 mM | 0.0409 mL | 0.2045 mL | 0.4090 mL | 1.0225 mL | |
| 80 mM | 0.0307 mL | 0.1534 mL | 0.3068 mL | 0.7669 mL | |
| 100 mM | 0.0245 mL | 0.1227 mL | 0.2454 mL | 0.6135 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Edonerpic maleate Related Classifications
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