Itanapraced
Based on 1 publication(s) in Google Scholar
Itanapraced (CHF5074) is an orally active γ-secretase modulator and a non-steroidal anti-inflammatory derivative. Itanapraced reduces Aβ42 and Aβ40 secretion with IC50 values of 3.6 and 18.4 μM, respectively. Itanapraced inhibits cell apoptosis of hippocampal neurons induced by oxygen and glucose deprivation (OGD). Itanapraced can be used for the research of Alzheimer's disease.
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- Pureza: 99.37%
- No. CAS: 749269-83-8
- Fòrmula: C16H11Cl2FO2
- Peso molecular:325.16
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Itanapraced
More
Actividad biológica
IC50 value: 3.6 μM (Aβ42), 18.4 μM (Aβ40)[1]
Itanapraced (0.03-100 μM) inhibits Aβ secretion in human neuroglioma cells (H4swe) expressing APPswe with IC50 values of 3.6 and 18.4 μM for Aβ42 and Aβ40, respectively[1]. Itanapraced (5-200 μM) inhibits Notch processing in HEK293swe cells with concentrations over 15 μM[1]. Itanapraced (0-1000 μM; 30 min) dose-dependently inhibits the action potential with an IC50 value of 106 μM[2]. Itanapraced (30-100 μM) dose-dependently inhibits excitatory synaptic transmission[2]. Itanapraced (1-10 μM) significantly reduces cell apoptosis in hippocampal neurons induced by oxygen and glucose deprivation (OGD)[2].
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.
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Animal Model:Male and female Tg2576 transgenic mice expressing Swedish mutated form of human APP (APPswe)[1]
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Dosage:375 ppm
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Administration:Oral administration; 375 ppm in the diet for 17 weeks
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Result:Reduced total brain Aβ42 and Aβ40 levels, and brain plaque burden in aged Tg2576 mice. Caused no COX-mediated toxic effects in the gastrointestinal tract and Notch-mediated cell differentiation abnormalities in the ileum.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 749269-83-8
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Appearance Solid
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Peso molecular 325.16
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Fòrmula C16H11Cl2FO2
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Color White to off-white
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SMILES
OC(C1(CC1)C(C=C2)=CC(F)=C2C3=CC=C(Cl)C(Cl)=C3)=O
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Synonyms
CHF5074; CSP-1103
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Sci Rep
2022 Apr 23;12(1):6672. PMID: 35461337
Solvente y solubilidad
DMSO : 100 mg/mL (307.54 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, 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 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (7.69 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. 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.
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.
Pureza y Documentación
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Ficha de datos (274 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Imbimbo BP, et al. 1-(3',4'-Dichloro-2-fluoro[1,1'-biphenyl]-4-yl)-cyclopropanecarboxylic acid (CHF5074), a novel gamma-secretasemodulator, reduces brain beta-amyloid pathology in a transgenic mouse model of Alzheimer's disease withoutcausing peripheral toxicity. J Pharmacol Exp Ther. 2007 Dec;323(3):822-830. [Content Brief]
[2]. Mango D, et al. Electrophysiological and metabolic effects of CHF5074 in the hippocampus: protection against in vitro ischemia. Pharmacol Res. 2014 Mar;81:83-90. [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 | 3.0754 mL | 15.3770 mL | 30.7541 mL | 76.8852 mL |
| 5 mM | 0.6151 mL | 3.0754 mL | 6.1508 mL | 15.3770 mL | |
| 10 mM | 0.3075 mL | 1.5377 mL | 3.0754 mL | 7.6885 mL | |
| 15 mM | 0.2050 mL | 1.0251 mL | 2.0503 mL | 5.1257 mL | |
| 20 mM | 0.1538 mL | 0.7689 mL | 1.5377 mL | 3.8443 mL | |
| 25 mM | 0.1230 mL | 0.6151 mL | 1.2302 mL | 3.0754 mL | |
| 30 mM | 0.1025 mL | 0.5126 mL | 1.0251 mL | 2.5628 mL | |
| 40 mM | 0.0769 mL | 0.3844 mL | 0.7689 mL | 1.9221 mL | |
| 50 mM | 0.0615 mL | 0.3075 mL | 0.6151 mL | 1.5377 mL | |
| 60 mM | 0.0513 mL | 0.2563 mL | 0.5126 mL | 1.2814 mL | |
| 80 mM | 0.0384 mL | 0.1922 mL | 0.3844 mL | 0.9611 mL | |
| 100 mM | 0.0308 mL | 0.1538 mL | 0.3075 mL | 0.7689 mL |
Itanapraced Related Classifications
HY-14399 Related Classifications
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