ESP15228
Based on 1 Customer Validation
ESP15228 is a metabolite of Bempedoic acid (HY-12357). ESP15228 undergoes glucuronidation to form ESP15228-glucuronide. ESP15228 can form excretory ESP15228-taurine conjugate in feces. ESP15228-CoA is a selective hepatic ATP citrate lyase inhibitor. ESP15228 can be used in the research of hypercholesterolemia.
For research use only. We do not sell to patients.
- Purity : 98.0%
- CAS No.: 413624-71-2
- Formula: C19H34O5
- Molecular Weight:342.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hepatocyte | IC50 |
3 μM
Compound: 10g
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Concentration required for inhibition of lipid synthesis in primary cultures of rat hepatocytes
Concentration required for inhibition of lipid synthesis in primary cultures of rat hepatocytes
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[PMID: 15537362] |
In Vitro
ESP15228 (5 μM; 4 h) shows a plasma protein binding rate of 99.2% when tested at a concentration of 5 μM in an in vitro equilibrium dialysis assay[1].
ESP15228 (1-8 μM; 60 min) undergoes reversible conversion to Bempedoic acid (HY-12357) via an NADPH-dependent metabolic pathway and forms glucuronide conjugates via a UDPGA-dependent metabolic pathway in pooled liver microsomes; extremely low substrate conversion rates are observed after a 60-minute incubation at the tested concentrations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 413624-71-2
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Appearance Solid
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Molecular Weight 342.47
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Formula C19H34O5
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Color White to off-white
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SMILES
O=C(O)C(C)(C)CCCCCC(CCCCCC(C)(C)C(O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (292.00 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. 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 (7.30 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 (7.30 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.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9200 mL | 14.5998 mL | 29.1996 mL | 72.9991 mL |
| 5 mM | 0.5840 mL | 2.9200 mL | 5.8399 mL | 14.5998 mL | |
| 10 mM | 0.2920 mL | 1.4600 mL | 2.9200 mL | 7.2999 mL | |
| 15 mM | 0.1947 mL | 0.9733 mL | 1.9466 mL | 4.8666 mL | |
| 20 mM | 0.1460 mL | 0.7300 mL | 1.4600 mL | 3.6500 mL | |
| 25 mM | 0.1168 mL | 0.5840 mL | 1.1680 mL | 2.9200 mL | |
| 30 mM | 0.0973 mL | 0.4867 mL | 0.9733 mL | 2.4333 mL | |
| 40 mM | 0.0730 mL | 0.3650 mL | 0.7300 mL | 1.8250 mL | |
| 50 mM | 0.0584 mL | 0.2920 mL | 0.5840 mL | 1.4600 mL | |
| 60 mM | 0.0487 mL | 0.2433 mL | 0.4867 mL | 1.2167 mL | |
| 80 mM | 0.0365 mL | 0.1825 mL | 0.3650 mL | 0.9125 mL | |
| 100 mM | 0.0292 mL | 0.1460 mL | 0.2920 mL | 0.7300 mL |