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ML224 (NCGC00242364) is a TSHR antagonist for the treatment of Graves' orbital disease and Graves' hyperthyroidism.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $52 | - | In Stock | |
| 5 mg | $123 | - | In Stock | |
| 10 mg | $197 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $142 | - | In Stock |
| Description | ML224 (NCGC00242364) is a TSHR antagonist for the treatment of Graves' orbital disease and Graves' hyperthyroidism. |
| Targets&IC50 | FSHR:>30 μM, LHR:>30 μM, TSHR:2.1 μM, HEK293 cells:2.1 μM |
| In vitro | In human embryonic kidney 293 cells, ML224 exhibits a half-maximal inhibitory concentration (IC50) of 2.1 μM against TSHR after a 20-minute exposure, with a range of 0.001-100 μM. The half-maximal inhibitory concentrations against LH and FSH receptors exceed 30 μM[1]. |
| In vivo | ML224(ANTAG3) 2 mg per mouse; administered through intraperitoneal infusion pump; once daily for 3 days) reduces serum FT4 levels and thyroid mRNA of TPO and NIS in mice subjected to prolonged TRH stimulation[1]. |
| Synonyms | NCGC00242364, ANTAG3 |
| Molecular Weight | 525.59 |
| Formula | C31H31N3O5 |
| Cas No. | 1338824-21-7 |
| Smiles | COc1ccc(cc1COc1c(C)cc(NC(C)=O)cc1C)C1Nc2ccccc2C(=O)N1Cc1ccco1 |
| Relative Density. | 1.252 g/cm3 (Predicted) |
| Color | Red |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (152.21 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.28 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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