Desethylamiodarone hydrochloride
Based on 1 Customer Validation
Desethylamiodarone hydrochloride (N-Desethylamiodarone hydrochloride; LB 33020 hydrochloride) is the major active metabolite of Amiodarone (HY-14187) generated via CYP3A4 metabolism. Desethylamiodarone hydrochloride downregulates p‑Akt, p‑Bad and Bcl‑2, upregulates Bax, promotes mitochondrial release of cytochrome c, activates caspase‑3 and cleaves PARP‑1, thereby inducing cell cycle arrest and apoptosis. Desethylamiodarone hydrochloride can be used in cervical cancer-related research.
For research use only. We do not sell to patients.
- Purity : 98.26%
- CAS No.: 96027-74-6
- Formula: C23H26ClI2NO3
- Molecular Weight:653.72
-
Storage:
-20°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]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
-
HY-130353R
Desethylamiodarone hydrochloride (Standard)Reference Standard -
HY-14187
AmiodaroneAntiarrhythmic Compound -
HY-14188
Amiodarone hydrochlorideAntiarrhythmic Agent -
HY-113147A
L-Palmitoylcarnitine chlorideKir6.2 Inhibitor -
HY-14188R
Amiodarone hydrochloride (Standard)Antiarrhythmic Agent -
HY-120358
L-6424T3R Inhibitor -
HY-124176
L-6355Phosphodiesterase Inhibitor -
HY-116478
L-3373 -
HY-W700643
Di-N-desethyl amiodarone hydrochlorideAmiodarone Metabolite -
HY-113147AR
L-Palmitoylcarnitine chloride (Standard)Kir6.2 Inhibitor
All Caspase Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
CYP3A4 |
Caspase-3 |
PARP-1 |
Bax |
Bcl-2 |
bad |
Akt |
In Vitro
Desethylamiodarone (DEA) (2.5-10 μM; 24-72 h) hydrochloride reduces the viability of human cervical cancer HeLa cells in a dose- and time-dependent manner[1].
Desethylamiodarone (0.5-2 μM; 7 days) hydrochloride inhibits colony formation of human cervical cancer HeLa cells in a dose-dependent manner[1].
Desethylamiodarone (2.5-5 μM; 24 h) hydrochloride inhibits the PI3K-Akt pathway in human cervical cancer HeLa cells in a dose-dependent manner by reducing the phosphorylation levels of Akt and its downstream target Bad; it also regulates the expression of apoptosis-related proteins in human cervical cancer HeLa cells in a dose-dependent manner: downregulating Bcl-2, upregulating Bax, inducing cytochrome c release, and activating the cleavage of caspase-3 and PARP-1[1].
Desethylamiodarone (5-10 μM; 24 h) hydrochloride induces apoptosis-related nuclear morphological changes (pyknosis and fragmentation) in human cervical cancer HeLa cells; it also induces apoptosis in human cervical cancer HeLa cells in a dose-dependent manner[1].
Desethylamiodarone (5 μM; 24 h) hydrochloride induces G0/G1 cell cycle arrest in human cervical cancer HeLa cells[1].
Desethylamiodarone (2.5-12.5 μg/mL; 1-4 days) hydrochloride exerts strong direct cytotoxicity against human thyroid cell line SGHTL-34 cultured in vitro, with an EC50 of 6.8 μg/mL at 24 h. It reduces cell numbers through cell destruction rather than decreasing cell adhesion, and induces vacuolization after 4 days of exposure[2].
Desethylamiodarone hydrochloride exhibits strong direct cytotoxicity against primary human retro-orbital fibroblasts in vitro, and a reduction in cell number is detected via protein content assay after 4 days of exposure[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 96027-74-6
-
Appearance Solid
-
Molecular Weight 653.72
-
Formula C23H26ClI2NO3
-
Color White to off-white
-
SMILES
O=C(C1=C(CCCC)OC2=CC=CC=C12)C3=CC(I)=C(OCCNCC)C(I)=C3.[H]Cl
-
Synonyms
N-Desethylamiodarone hydrochloride; LB 33020 hydrochloride
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 10 mg/mL (15.30 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 5 mg/mL (7.65 mM; Need ultrasonic and warming)
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)
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 (3.82 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Protocols
-
Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
-
TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
-
Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
-
Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
-
BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
-
Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
-
Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
Purity & Documentation
-
Data Sheet (285 KB)
-
SDS (704 KB)
- English - EN (704 KB)
- Français - FR (704 KB)
- Deutsch - DE (704 KB)
- Norwegian - NO (704 KB)
- Español - ES (704 KB)
- Swedish - SV (704 KB)
- Italian - IT (704 KB)
- Korean - KR (704 KB)
- Portuguese - PT (704 KB)
-
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 |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 1.5297 mL | 7.6485 mL | 15.2971 mL | 38.2427 mL |
| 5 mM | 0.3059 mL | 1.5297 mL | 3.0594 mL | 7.6485 mL | |
| DMSO | 10 mM | 0.1530 mL | 0.7649 mL | 1.5297 mL | 3.8243 mL |
| 15 mM | 0.1020 mL | 0.5099 mL | 1.0198 mL | 2.5495 mL |
Desethylamiodarone hydrochloride Related Classifications
HY-130353 Related Classifications
Powered by Bioz
Keywords
- Desethylamiodarone
- 96027-74-6
- N-Desethylamiodarone
- LB 33020
- LB33020
- LB-33020
- Drug Metabolite
- Cytochrome P450
- Akt
- Bcl-2 Family
- Caspase
- PARP
- Apoptosis
- phosphorylated Akt
- Bax
- proliferation
- HeLa human cervical cancer cells
- blood-brain barrier
- phosphorylated Bad
- apoptosis
- Bcl-2
- PI3K-Akt signaling
- SGHTL-34 human thyrocytes
- Inhibitor
- inhibitor
- inhibit