Cas No.: | 1338824-21-7 |
Chemical Name: | NCGC00242364,ANTAG3,ML-224,ML 224 |
Synonyms: | NCGC00242364,ANTAG3,ML-224,ML 224 |
SMILES: | C1=C(NC(=O)C)C=C(C)C(OCC2=C(OC)C=CC(C3NC4C=CC=CC=4C(=O)N3CC3=CC=CO3)=C2)=C1C |
Formula: | C31H31N3O5 |
M.Wt: | 525.59 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | ML224(NCGC00242364; ANTAG3) is a selective TSHR inverse agonist; inhibits TSH-stimulated cAMP production with an IC50 = 2.3 μM. |
In Vivo: | In mice treated with TRH, ANTAG3 lowered serum free T4 by 44% and lowered mRNAs for sodium-iodide cotransporter and thyroperoxidase by 75% and 83%, respectively. In mice given M22, ANTAG3 lowered serum free T4 by 38% and lowered mRNAs for sodium-iodide cotransporter and thyroperoxidase by 73% and 40%, respectively [2]. |
In Vitro: | ANTAG3 was selective for TSHR inhibition; half-maximal inhibitory doses were 2.1 μM for TSHR and greater than 30 μM for LH and FSH receptors [2]. |