[CAS NO. 1338824-21-7] ML224
PRODUCTS SPECIFICATIONS [1338824-21-7]
DESCRIPTION [1338824-21-7]
Overview
| 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 |
1 Publications Citing Use of MCE
Summary
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.
IC50 & Target
|
TSHR 2.1 μM (IC 50 ) |
LHR ＞30 μM (IC 50 ) |
FSHR ＞30 μM (IC 50 ) |
In Vitro
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. |
In Vivo
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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 190.26 mM ; Need ultrasonic)
Stock Solutions
| 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 |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution