<Suppliers Price>

ML-224

Names

[ CAS No. ]:
1338824-21-7

[ Name ]:
ML-224

[Synonym ]:
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

Biological Activity

[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.


[Related Small Molecules]

ML-109 | Org41841

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
752.3±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C31H31N3O5

[ Molecular Weight ]:
525.595

[ Flash Point ]:
408.8±32.9 °C

[ Exact Mass ]:
525.226379

[ LogP ]:
2.92

[ Vapour Pressure ]:
0.0±2.5 mmHg at 25°C

[ Index of Refraction ]:
1.626

[ Storage condition ]:
2-8℃

Related Compounds