Ertiprotafib
Based on 2 publication(s) in Google Scholar
Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
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- Pureza: 98.13%
- No. CAS: 251303-04-5
- Fòrmula: C31H27BrO3S
- Peso molecular:559.51
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) Ertiprotafib
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Actividad biológica
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PTP1B 1.6 μM (IC50) |
IKK-β 400 nM (IC50) |
PPARα ~1 μM (EC50) |
PPARβ ~1 μM (EC50) |
Ertiprotafib is a potent inhibitor of IKK-β, with an IC50 value of 400±40 nM, which is much lower than that required for the half-maximal inhibition of the p-nitrophenyl phosphatase activity of PTP1B. The reported IC50 value of Ertiprotafib against PTP1B ranges from 1.6 to 29 μM depending on the assay conditions[2]. Ertiprotafib is at least a dual PPARα and PPARβ agonist with EC50 values for transactivation of 1 μM. Such activities readily explain the observations with suprapharmacologic doses of these[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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No. CAS 251303-04-5
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Appearance Solid
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Peso molecular 559.51
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Fòrmula C31H27BrO3S
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Color Light yellow to yellow
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SMILES
OC([C@@H](CC1=CC=CC=C1)OC2=C(C)C=C(C3=C(C(C)=C(C)S4)C4=C(Br)C5=CC=CC=C53)C=C2C)=O
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Synonyms
PTP 112
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (2)
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Journal Impact Factor
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Most Recent
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Acta Pharm Sin B
Activatable PROTAC nanoassembly for photodynamic PTP1B proteolysis enhances glioblastoma immunotherapy. [Abstract]2025 Sep;15(9):4886-4899. PMID: 41049728 -
Spectrochim Acta A Mol Biomol Spectrosc
A novel fluorescent probe with Aggregation-Induced emission characteristics for PTP1B activity sensing and inhibitor screening. [Abstract]2025 Feb 15:327:125394. PMID: 39520822
Solvente y solubilidad
DMSO : 100 mg/mL (178.73 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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: 2.5 mg/mL (4.47 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
Protocolo
Mice, Rats[2]
Male Ob/ob mice and Zucker fa/fa rats are used. They are kept on a 12-h/12-h light/dark cycle and fed Rodent Diet 5001 (for mice and rats) from Purina Mills. Compounds are dosed orally by gavage in an aqueous suspension of 2% Tween 80 and 0.5% methylcellulose. Whole blood (5 μL) is used for glucose readings via tail nick for measurement using the Ascensia Elite XL glucometer and glucose strips by preloading a strip into the meter and touching the end to a small drop of blood on each tail. Insulin levels are quantified by enzyme-linked immunosorbent assay[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (282 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Shrestha S, et al. PTP1B inhibitor Ertiprotafib is also a potent inhibitor of IkappaB kinase beta (IKK-beta). Bioorg Med Chem Lett. 2007 May 15;17(10):2728-30. Epub 2007 Mar 3. [Content Brief]
[2]. Erbe DV, et al. Ertiprotafib improves glycemic control and lowers lipids via multiple mechanisms. Mol Pharmacol. 2005 Jan;67(1):69-77. [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 and light). 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 | 1.7873 mL | 8.9364 mL | 17.8728 mL | 44.6820 mL |
| 5 mM | 0.3575 mL | 1.7873 mL | 3.5746 mL | 8.9364 mL | |
| 10 mM | 0.1787 mL | 0.8936 mL | 1.7873 mL | 4.4682 mL | |
| 15 mM | 0.1192 mL | 0.5958 mL | 1.1915 mL | 2.9788 mL | |
| 20 mM | 0.0894 mL | 0.4468 mL | 0.8936 mL | 2.2341 mL | |
| 25 mM | 0.0715 mL | 0.3575 mL | 0.7149 mL | 1.7873 mL | |
| 30 mM | 0.0596 mL | 0.2979 mL | 0.5958 mL | 1.4894 mL | |
| 40 mM | 0.0447 mL | 0.2234 mL | 0.4468 mL | 1.1170 mL | |
| 50 mM | 0.0357 mL | 0.1787 mL | 0.3575 mL | 0.8936 mL | |
| 60 mM | 0.0298 mL | 0.1489 mL | 0.2979 mL | 0.7447 mL | |
| 80 mM | 0.0223 mL | 0.1117 mL | 0.2234 mL | 0.5585 mL | |
| 100 mM | 0.0179 mL | 0.0894 mL | 0.1787 mL | 0.4468 mL |
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