TES-1025
Based on 3 publication(s) in Google Scholar
TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC50 of 13 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.39%
- CAS. Nr.: 1883602-21-8
- Formel: C18H13N3O3S2
- Molecular Weight:383.44
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Metabolism/Protease Compound Library
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Publications Citing Use of MedChemExpress (MCE) TES-1025
More
Biologische Aktivität
IC50: 13±3 nM (human ACMSD)[1]
TES-1025 is a low nanomolar human ACMSD inhibitor, which increases NAD+ levels in cellular systems[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. Nr. 1883602-21-8
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Appearance Solid
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Molecular Weight 383.44
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Formel C18H13N3O3S2
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Color White to yellow
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SMILES
O=C1C(C#N)=C(C2=CC=CS2)N=C(SCC3=CC=CC(CC(O)=O)=C3)N1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Biomed Pharmacother
Adult zebrafish as an in vivo drug testing model for ethanol induced acute hepatic injury. [Abstract]2020 Dec;132:110836. PMID: 33035832 -
Toxicol Lett
Modulation of NAD+ biosynthesis activates SIRT1 and resists cisplatin-induced ototoxicity. [Abstract]2021 Oct 1:349:115-123. PMID: 34089817
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (260.80 mM; Need warming; 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (6.52 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 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.
Protokoll
Recombinant hACMSD is expressed in Pichia pastoris and purified. Its enzyme activity is assayed by a coupled spectrophotometric assay. Briefly, in a pre-assay mixture, the ACMS substrate is generated from 10 μM 3-hydroxyanthranilic acid by recombinant 3-hydroxyanthranilate 3,4-dioxigenase from Ralstonia metallidurans. ACMS formation is monitored at 360 nm, and after the reaction is complete, an appropriate amount of ACMSD is added. Activity is calculated from the initial rate of the absorbance decrease subtracted from that of a control reaction mixture in the absence of ACMSD. The effects of the various compounds (e.g., TES-1025) on the enzyme activity are tested by adding the compounds to the assay mixture along with ACMSD. For the IC50 evaluations for each compound, a serial dilution from a stock solution prepared in DMSO is tested, maintaining a DMSO concentration in all the reaction mixtures of 1.0%. One unit is defined as the amount of enzyme that consume 1 μmol of ACMS per minute at 37°C[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Male CD-1 mice are used.The study is conducted in 3 phases. Phase 1: 18 mice receive an oral administration of TES-1025 at a target dose level of 5 mg/kg. Blood, brain and liver are collected at intervals up to 8 h after dose administration (n=3 animals per each time point). Phase 2: 3 mice receive each an intravenous administration of TES-1025 at a target dose of 0.5 mg/kg. Blood samples are collected from the lateral tail vein at intervals up to 24 h after dose administration. Phase 3: 3 mice receive a single intravenous administration of Elacridar (5 mg/kg) shortly before an oral administration of TES-1025 at a target dose of 5 mg/kg. Blood and brain samples are collected 0.5 h after dose administration. Brain, liver and kidney are collected from all animals of the study[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (277 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)
Verweise
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 | 2.6080 mL | 13.0398 mL | 26.0797 mL | 65.1992 mL |
| 5 mM | 0.5216 mL | 2.6080 mL | 5.2159 mL | 13.0398 mL | |
| 10 mM | 0.2608 mL | 1.3040 mL | 2.6080 mL | 6.5199 mL | |
| 15 mM | 0.1739 mL | 0.8693 mL | 1.7386 mL | 4.3466 mL | |
| 20 mM | 0.1304 mL | 0.6520 mL | 1.3040 mL | 3.2600 mL | |
| 25 mM | 0.1043 mL | 0.5216 mL | 1.0432 mL | 2.6080 mL | |
| 30 mM | 0.0869 mL | 0.4347 mL | 0.8693 mL | 2.1733 mL | |
| 40 mM | 0.0652 mL | 0.3260 mL | 0.6520 mL | 1.6300 mL | |
| 50 mM | 0.0522 mL | 0.2608 mL | 0.5216 mL | 1.3040 mL | |
| 60 mM | 0.0435 mL | 0.2173 mL | 0.4347 mL | 1.0867 mL | |
| 80 mM | 0.0326 mL | 0.1630 mL | 0.3260 mL | 0.8150 mL | |
| 100 mM | 0.0261 mL | 0.1304 mL | 0.2608 mL | 0.6520 mL |
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