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Catalog: | HY-12381 |
Brand: | MCE |
CAS: | 1338824-21-7 |
MDL | - |
---|---|
Molecular Weight | 525.59 |
Molecular Formula | C31H31N3O5 |
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 |
ML224 (NCGC00242364) is a selective TSHR antagonist with an IC 50 value of 2.1 µM. ML224 can be used in the study of Graves' disease and other thyroid disorders.
TSHR 2.1 μM (IC 50 ) |
LHR >30 μM (IC 50 ) |
FSHR >30 μM (IC 50 ) |
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
Cell Line: | Human embryonic kidney 293 cells (stably expressing TSHRs, LHRs, or FSHRs) |
Concentration: | 0.001-100 µM |
Incubation Time: | 20 min |
Result: |
Showed the IC
50
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. |
ANTAG3 (2 mg/mice; i.p. via osmotic pump; single daily for 3 days) lowers serum FT4 levels and thyroidal mRNAs for TPO and NIS in mice continuously stimulated by TRH [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | Female BALB/c mice (8 to 13-week-old; ~18.7 g) [1] . |
Dosage: | 2 mg/mice |
Administration: | Intraperitoneal injection via osmotic pump; single daily for 3 days |
Result: | Lowered the levels of FT4 by 44%, and the levels of TPO and NIS mRNAs by 75% and 83%, respectively. |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 100 mg/mL ( 190.26 mM ; Need ultrasonic)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 1.9026 mL | 9.5131 mL | 19.0262 mL |
5 mM | 0.3805 mL | 1.9026 mL | 3.8052 mL |
10 mM | 0.1903 mL | 0.9513 mL | 1.9026 mL |
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution
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