Elunetirom
Based on 1 Customer Validation
Elunetirom (MA-JD21) is an orally active, blood-brain barrier-permeable prodrug of LL-340001. Elunetirom employs fatty acid amide hydrolase (FAAH)-dependent prodrug technology to enhance the brain delivery of LL-340001, a potent thyroid hormone receptor agonist with 15-fold higher selectivity for TRβ over TRα. Elunetirom induces T3-regulated gene expression, including that of ABCD2. Elunetirom drives neuroplasticity and bioenergetic changes, and induces neurogenesis, neuritogenesis, and synaptogenesis. Elunetirom is applicable to research related to major depressive disorder and X-linked adrenoleukodystrophy.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.24%
- No. CAS: 2156649-32-8
- Fòrmula: C19H21Cl2NO3
- Peso molecular:382.28
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
In Vitro
Elunetirom (0.3 nM-1 μM; 24-72 h) induces robust neuritogenic and synaptogenic effects in mature E17 Wistar rat hippocampal neurons, with effects comparable to BDNF (50 ng/mL)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Hypothyroid cohort[2]
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Dosage:13 μg/kg
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Administration:p.o.
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Result:Enhanced delivery of LL-340001 to the brain by 30-fold.
Induced T3-dependent gene expression in the brain and liver.
Increased Abcd2 expression in the brain, spinal cord, and liver.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2156649-32-8
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Appearance Solid
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Peso molecular 382.28
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Fòrmula C19H21Cl2NO3
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Color White to off-white
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SMILES
O=C(COC1=CC(Cl)=C(CC2=CC=C(C(C(C)C)=C2)O)C(Cl)=C1)NC
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Synonyms
MA-JD21; ABX-002
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (261.59 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.54 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.
Pureza y Documentación
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Ficha de datos (279 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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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.6159 mL | 13.0794 mL | 26.1588 mL | 65.3971 mL |
| 5 mM | 0.5232 mL | 2.6159 mL | 5.2318 mL | 13.0794 mL | |
| 10 mM | 0.2616 mL | 1.3079 mL | 2.6159 mL | 6.5397 mL | |
| 15 mM | 0.1744 mL | 0.8720 mL | 1.7439 mL | 4.3598 mL | |
| 20 mM | 0.1308 mL | 0.6540 mL | 1.3079 mL | 3.2699 mL | |
| 25 mM | 0.1046 mL | 0.5232 mL | 1.0464 mL | 2.6159 mL | |
| 30 mM | 0.0872 mL | 0.4360 mL | 0.8720 mL | 2.1799 mL | |
| 40 mM | 0.0654 mL | 0.3270 mL | 0.6540 mL | 1.6349 mL | |
| 50 mM | 0.0523 mL | 0.2616 mL | 0.5232 mL | 1.3079 mL | |
| 60 mM | 0.0436 mL | 0.2180 mL | 0.4360 mL | 1.0900 mL | |
| 80 mM | 0.0327 mL | 0.1635 mL | 0.3270 mL | 0.8175 mL | |
| 100 mM | 0.0262 mL | 0.1308 mL | 0.2616 mL | 0.6540 mL |
Elunetirom Related Classifications
HY-160207 Related Classifications
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Keywords
- Elunetirom
- 2156649-32-8
- MA-JD21
- ABX-002
- ABX002
- ABX 002
- ABX-002
- Drug Intermediate
- FAAH
- Thyroid Hormone Receptor
- oligodendrocyte progenitor cell
- TR-α
- TR-β
- x-linked adrenoleukodystrophy
- bipolar depression
- major depressive disorder
- ABCD2
- E17 Wistar rat hippocampal neurons
- thyroid hormone receptor beta
- demyelinating disease models
- Inhibitor
- inhibitor
- inhibit