Debutyldronedarone hydrochloride
Based on 2 publication(s) in Google Scholar
Debutyldronedarone hydrochloride (SR35021 hydrochloride) is a Cytochrome P450 enzyme inhibitor and a Thyroid Hormone Receptor inhibitor, and it is a metabolite of Dronedarone (HY-A0016). Debutyldronedarone hydrochloride inhibits the binding of T3 to TRα1 and TRβ1. Debutyldronedarone hydrochloride reduces the incidence of reperfusion-induced ventricular fibrillation in anesthetized rats, while decreasing their heart rate and blood pressure. Debutyldronedarone hydrochloride can be used in studies related to ventricular fibrillation and atrial fibrillation.
For research use only. We do not sell to patients.
- Purity: 98.32%
- CAS No.: 197431-02-0
- Formula: C27H37ClN2O5S
- Molecular Weight:537.11
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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)
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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
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Publications Citing Use of MedChemExpress (MCE) Debutyldronedarone hydrochloride
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Biological Activity
Debutyldronedarone (SR35021) hydrochloride inhibits the binding of T3 to human TRα1 (Ki = 59 μM) and TRβ1 (Ki = 280 μM) in vitro, with higher potency against the TRα1 subtype; it also inhibits multiple human CYP isozymes in vitro, with Ki values ranging from 4.37 μM (CYP2D6) to 56.9 μM (CYP2B6)[1].
Debutyldronedarone hydrochloride binds extensively to human plasma proteins (98.5%) and purified serum albumin (94.5-95.3%) in a non-saturable manner, whereas its binding to α1-acid glycoprotein is saturable and concentration-dependent[1].
Debutyldronedarone hydrochloride is metabolized by human CYP3A and CYP2D6 in vitro[1].
Debutyldronedarone (DBDron) (10-100 μM) hydrochloride potently and competitively inhibits the binding of [125I]T3 to chicken TRα1 with an IC50 of 59 μM; meanwhile, it only exerts weak inhibitory effects on the binding of [125I]T3 to human TRβ1, with an IC50 of 280 μM, demonstrating TRα1-selective antagonistic activity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Debutyldronedarone (DBDron) (formed in vivo from Dronedarone (HY-A0016); administration conditions: 50-100 mg/kg, p.o., once daily for 14 consecutive days) hydrochloride acts as a thyroid hormone receptor α1-selective inhibitor. It prolongs the QTc interval to approximately 0.028 msec via TRα1 mediation, reduces plasma T3 levels, and does not affect TRβ1-mediated hepatic lipid metabolism endpoints[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 197431-02-0
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Appearance Solid
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Molecular Weight 537.11
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Formula C27H37ClN2O5S
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Color White to light yellow
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SMILES
O=C(C1=C(CCCC)OC2=C1C=C(NS(=O)(C)=O)C=C2)C3=CC=C(C=C3)OCCCNCCCC.Cl
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Synonyms
SR35021 hydrochloride
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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)
Publications (2)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : ≥ 100 mg/mL (186.18 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (4.65 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 (4.65 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 (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 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 (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 | 1.8618 mL | 9.3091 mL | 18.6182 mL | 46.5454 mL |
| 5 mM | 0.3724 mL | 1.8618 mL | 3.7236 mL | 9.3091 mL | |
| 10 mM | 0.1862 mL | 0.9309 mL | 1.8618 mL | 4.6545 mL | |
| 15 mM | 0.1241 mL | 0.6206 mL | 1.2412 mL | 3.1030 mL | |
| 20 mM | 0.0931 mL | 0.4655 mL | 0.9309 mL | 2.3273 mL | |
| 25 mM | 0.0745 mL | 0.3724 mL | 0.7447 mL | 1.8618 mL | |
| 30 mM | 0.0621 mL | 0.3103 mL | 0.6206 mL | 1.5515 mL | |
| 40 mM | 0.0465 mL | 0.2327 mL | 0.4655 mL | 1.1636 mL | |
| 50 mM | 0.0372 mL | 0.1862 mL | 0.3724 mL | 0.9309 mL | |
| 60 mM | 0.0310 mL | 0.1552 mL | 0.3103 mL | 0.7758 mL | |
| 80 mM | 0.0233 mL | 0.1164 mL | 0.2327 mL | 0.5818 mL | |
| 100 mM | 0.0186 mL | 0.0931 mL | 0.1862 mL | 0.4655 mL |
Debutyldronedarone hydrochloride Related Classifications
HY-12753A Related Classifications
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