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ML224 (NCGC00242364) is a TSHR antagonist for the treatment of Graves' orbital disease and Graves' hyperthyroidism.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $52 | In Stock | |
5 mg | $123 | In Stock | |
10 mg | $197 | In Stock | |
25 mg | $383 | 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 | LHR:>30 μM, TSHR:2.1 μM, HEK293 cells:2.1 μM, FSHR:>30 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]. |
Alias | 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) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (152.21 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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