EBP-IN-1
Based on 1 Customer Validation
EBP-IN-1 is an orally active, blood-brain barrier-permeable inhibitor of emopamil binding protein (EBP). EBP-IN-1 has an IC50 of 8.2 μM against human ERG potassium channels (in CHO background). By inhibiting the sterol isomerase activity of EBP, EBP-IN-1 causes the accumulation of Zymostenol (HY-113345), and exhibits strong target binding in the brain after repeated administration in rodents. EBP-IN-1 also promotes oligodendrocyte formation in human cortical organoids and can be used in research related to multiple sclerosis.
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- Pureté: 99.77%
- CAS No.: 3034437-44-7
- Formule: C24H33N3O3
- Masse moléculaire:411.54
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
EBP-IN-1 induces zymostenol accumulation in mouse OPCs with an EC50 of 8 nM[1].
EBP-IN-1 induces zymostenol accumulation in human MSCs with an EC50 of 39 nM[1].
EBP-IN-1 (1 μM; up to 4 h) shows good metabolic stability in mouse, rat, and human hepatocytes, with projected hepatic clearances of 21, 11, and 1.4 mL/min/kg, respectively[1].
EBP-IN-1 (5 μM; 6 h) exhibits moderate plasma protein binding, with 36.4%, 30.0%, and 29.1% unbound in mouse, rat, and human plasma, respectively, at 5 μM[1].
EBP-IN-1 shows high brain tissue binding, with 92% bound[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, 6-9 weeks old, 25-35 g)[1]
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Dosage:0.02 mg/kg; 0.2 mg/kg; 2 mg/kg
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Administration:p.o.; daily; 7 days
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Result:Increased mean brain zymostenol total concentrations in a dose-dependent manner, reaching a 54-fold increase compared to vehicle controls at the 2 mg/kg dose.
Achieved free brain concentrations above the mouse GCMS EC50 (0.008 μM) at all tested doses.
Chemical Information
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CAS No. 3034437-44-7
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Appearance Solid
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Masse moléculaire 411.54
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Formule C24H33N3O3
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Color White to off-white
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SMILES
CCN1C(N(C2=CC=C(C3CC3)C=C2)C(C14CCN(CC5CCOCC5)CC4)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (242.99 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. 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. 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)
In Vivo:
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 (6.07 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 (6.07 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.
In Vivo Dissolution Calculator
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.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
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. 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 |
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| DMSO | 1 mM | 2.4299 mL | 12.1495 mL | 24.2990 mL | 60.7474 mL |
| 5 mM | 0.4860 mL | 2.4299 mL | 4.8598 mL | 12.1495 mL | |
| 10 mM | 0.2430 mL | 1.2149 mL | 2.4299 mL | 6.0747 mL | |
| 15 mM | 0.1620 mL | 0.8100 mL | 1.6199 mL | 4.0498 mL | |
| 20 mM | 0.1215 mL | 0.6075 mL | 1.2149 mL | 3.0374 mL | |
| 25 mM | 0.0972 mL | 0.4860 mL | 0.9720 mL | 2.4299 mL | |
| 30 mM | 0.0810 mL | 0.4050 mL | 0.8100 mL | 2.0249 mL | |
| 40 mM | 0.0607 mL | 0.3037 mL | 0.6075 mL | 1.5187 mL | |
| 50 mM | 0.0486 mL | 0.2430 mL | 0.4860 mL | 1.2149 mL | |
| 60 mM | 0.0405 mL | 0.2025 mL | 0.4050 mL | 1.0125 mL | |
| 80 mM | 0.0304 mL | 0.1519 mL | 0.3037 mL | 0.7593 mL | |
| 100 mM | 0.0243 mL | 0.1215 mL | 0.2430 mL | 0.6075 mL |
EBP-IN-1 Related Classifications
HY-162351 Related Classifications
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