1338824-21-7

1338824-21-7 structure

Name: ML-224
Chemical Name: N-[4-({5-[3-(2-Furylmethyl)-4-oxo-1,2,3,4-tetrahydro-2-quinazolinyl]-2-methoxybenzyl}oxy)-3,5-dimethylphenyl]acetamide
CAS Number: 1338824-21-7
Molecular Formula: C₃₁H₃₁N₃O₅
Molecular Weight: 525.595
Catalog: Signaling Pathways GPCR/G Protein TSH Receptor
Create Date: 2018-04-29 16:50:25
Modify Date: 2024-01-01 23:16:29
ML224(NCGC00242364; ANTAG3) is a selective TSHR inverse agonist; inhibits TSH-stimulated cAMP production with an IC50 = 2.3 μM.IC50 value: 2.3 uM [1]Target: TSHR agonistin 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]. 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].

Name	N-[4-({5-[3-(2-Furylmethyl)-4-oxo-1,2,3,4-tetrahydro-2-quinazolinyl]-2-methoxybenzyl}oxy)-3,5-dimethylphenyl]acetamide
Synonyms	N-[4-({5-[3-(2-Furylmethyl)-4-oxo-1,2,3,4-tetrahydro-2-quinazolinyl]-2-methoxybenzyl}oxy)-3,5-dimethylphenyl]acetamide Acetamide, N-[4-[[5-[3-(2-furanylmethyl)-1,2,3,4-tetrahydro-4-oxo-2-quinazolinyl]-2-methoxyphenyl]methoxy]-3,5-dimethylphenyl]- ML-224 ML224

Description	ML224(NCGC00242364; ANTAG3) is a selective TSHR inverse agonist; inhibits TSH-stimulated cAMP production with an IC50 = 2.3 μM.IC50 value: 2.3 uM [1]Target: TSHR agonistin 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]. 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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> TSH Receptor Research Areas >> Endocrinology
References	[1]. Huang W, et al. Identification of Thyroid Stimulating Hormone Receptor Inverse Agonists. Probe Reports from the NIH Molecular Libraries Program [2]. Neumann S, et al. A selective TSH receptor antagonist inhibits stimulation of thyroid function in female mice. Endocrinology. 2014 Jan;155(1):310-4.