Epibestatin hydrochloride
Based on 1 Customer Validation
Epibestatin hydrochloride is an epimer of Bestatin (HY-B0134), a DPP4 inhibitor and protease inhibitor, with an IC50 of 17 μM against DPP4. As a stabilizer, Epibestatin hydrochloride binds to the cleft between 14-3-3 protein and plant proton pump PMA2, selectively stabilizing their interaction without affecting other 14-3-3 client proteins. Epibestatin hydrochloride triggers stomatal opening in leaf epidermis of Commelina communis. Epibestatin hydrochloride can be used in studies related to type 2 diabetes.
For research use only. We do not sell to patients.
- Purity: 98.43%
- CAS No.: 100992-60-7
- Formula: C16H25ClN2O4
- Molecular Weight:344.83
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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DPP-4 17 μM (IC50) |
Epibestatin (0.5-50 μM; 90 min) hydrochloride inhibits purified dipeptidyl peptidase 4 (DPP4) with an IC50 of 17 μM, showing dose-dependent inhibitory activity across concentrations from 0.5 to 50 μM, while its epimer bestatin shows no DPP4 inhibitory activity[1].
Epibestatin (50 μM) hydrochloride stabilizes the interaction between purified 14-3-3 protein and PMA2-CT52 with a KD of 1.8 μM, as measured via surface plasmon resonance[3].
Epibestatin (50 μM; 3 h) hydrochloride induces stomatal opening in isolated Commelina communis leaf epidermis to an average width of 3.2 μm after 3 hours of incubation[3].
Epibestatin hydrochloride does not stabilize the interaction between purified 14-3-3 protein and any of the tested alternative targets (Raf1, p53, Cdc25C, RNF11, Mlf1, AICD, Cby, YAP), demonstrating selectivity for the 14-3-3/PMA2 complex[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 100992-60-7
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Appearance Solid
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Molecular Weight 344.83
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Formula C16H25ClN2O4
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Color White to off-white
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SMILES
CC(C)C[C@@H](C(O)=O)NC([C@H](O)[C@H](N)CC1=CC=CC=C1)=O.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (290.00 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). 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). 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 (7.25 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.25 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.
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)
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.
Purity & Documentation
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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]. Kawaguchi M, et al. A time-resolved fluorescence probe for dipeptidyl peptidase 4 and its application in inhibitor screening. Chemistry (Weinheim an der Bergstrasse, Germany). 2010 Dec 03;16(45):13479-86. [Content Brief]
[3]. Rose R, et al. Identification and structure of small-molecule stabilizers of 14-3-3 protein-protein interactions. Angew Chem Int Ed Engl. 2010 Jun 1;49(24):4129-32. [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 | 1 mM | 2.9000 mL | 14.4999 mL | 28.9998 mL | 72.4995 mL |
| 5 mM | 0.5800 mL | 2.9000 mL | 5.8000 mL | 14.4999 mL | |
| 10 mM | 0.2900 mL | 1.4500 mL | 2.9000 mL | 7.2499 mL | |
| 15 mM | 0.1933 mL | 0.9667 mL | 1.9333 mL | 4.8333 mL | |
| 20 mM | 0.1450 mL | 0.7250 mL | 1.4500 mL | 3.6250 mL | |
| 25 mM | 0.1160 mL | 0.5800 mL | 1.1600 mL | 2.9000 mL | |
| 30 mM | 0.0967 mL | 0.4833 mL | 0.9667 mL | 2.4166 mL | |
| 40 mM | 0.0725 mL | 0.3625 mL | 0.7250 mL | 1.8125 mL | |
| 50 mM | 0.0580 mL | 0.2900 mL | 0.5800 mL | 1.4500 mL | |
| 60 mM | 0.0483 mL | 0.2417 mL | 0.4833 mL | 1.2083 mL | |
| 80 mM | 0.0362 mL | 0.1812 mL | 0.3625 mL | 0.9062 mL | |
| 100 mM | 0.0290 mL | 0.1450 mL | 0.2900 mL | 0.7250 mL |
Epibestatin hydrochloride Related Classifications
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