ML224
Based on 1 publication(s) in Google Scholar
ML224 (NCGC00242364) is a selective TSHR antagonist with an IC50 value of 2.1 µM. ML224 can be used in the study of Graves' disease and other thyroid disorders.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.18%
- No. CAS: 1338824-21-7
- Fòrmula: C31H31N3O5
- Peso molecular:525.59
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) ML224
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Actividad biológica
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TSHR 2.1 μM (IC50) |
LHR ＞30 μM (IC50) |
FSHR ＞30 μM (IC50) |
ML224 (0.001-100 μM; 20 min) exhibits half-maximal inhibitory doses of 2.1 μM for TSHR and greater than 30 μM for LH and FSH receptors in human embryonic kidney 293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human embryonic kidney 293 cells (stably expressing TSHRs, LHRs, or FSHRs)
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Concentration:0.001-100 µM
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Incubation Time:20 min
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Result:Showed the IC50 for stimulation by bovine TSH (1.8 nM) was 2.1 µM.
Showed inhibition of LH and FSH stimulation was less than 15% for LH (1 nM) and less than 30% for FSH (1 nM) at 30 µM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice (8 to 13-week-old; ~18.7 g)[1].
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Dosage:2 mg/mice
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Administration:Intraperitoneal injection via osmotic pump; single daily for 3 days
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Result:Lowered the levels of FT4 by 44%, and the levels of TPO and NIS mRNAs by 75% and 83%, respectively.
Chemical Information
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No. CAS 1338824-21-7
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Appearance Solid
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Peso molecular 525.59
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Fòrmula C31H31N3O5
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Color White to off-white
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SMILES
CC(NC1=CC(C)=C(OCC2=CC(C(N3CC4=CC=CO4)NC5=C(C=CC=C5)C3=O)=CC=C2OC)C(C)=C1)=O
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Synonyms
NCGC00242364; ANTAG3
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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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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J Immunother Cancer
2022 Jan;10(1):e004049. PMID: 35101946
Solvente y solubilidad
DMSO : 100 mg/mL (190.26 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (4.76 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.
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 (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9026 mL | 9.5131 mL | 19.0262 mL | 47.5656 mL |
| 5 mM | 0.3805 mL | 1.9026 mL | 3.8052 mL | 9.5131 mL | |
| 10 mM | 0.1903 mL | 0.9513 mL | 1.9026 mL | 4.7566 mL | |
| 15 mM | 0.1268 mL | 0.6342 mL | 1.2684 mL | 3.1710 mL | |
| 20 mM | 0.0951 mL | 0.4757 mL | 0.9513 mL | 2.3783 mL | |
| 25 mM | 0.0761 mL | 0.3805 mL | 0.7610 mL | 1.9026 mL | |
| 30 mM | 0.0634 mL | 0.3171 mL | 0.6342 mL | 1.5855 mL | |
| 40 mM | 0.0476 mL | 0.2378 mL | 0.4757 mL | 1.1891 mL | |
| 50 mM | 0.0381 mL | 0.1903 mL | 0.3805 mL | 0.9513 mL | |
| 60 mM | 0.0317 mL | 0.1586 mL | 0.3171 mL | 0.7928 mL | |
| 80 mM | 0.0238 mL | 0.1189 mL | 0.2378 mL | 0.5946 mL | |
| 100 mM | 0.0190 mL | 0.0951 mL | 0.1903 mL | 0.4757 mL |
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