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首页-小分子抑制剂&激动剂-GPCR-Thyrotropin Receptor-ML224
ML224

Chemical Structure : ML224

CAS No.: 1338824-21-7

ML224 (NCGC00242364, ANTAG3)

货号: PC-43013Not For Human Use, Lab Use Only.

ML224 (NCGC00242364, ANTAG3) is a potent selective thyroid stimulating hormone receptor (TSHR) inverse agonist, selectively inhibits TSH-stimulated cAMP production with IC50 of 2.3 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ML224 (NCGC00242364, ANTAG3) is a potent selective thyroid stimulating hormone receptor (TSHR) inverse agonist, selectively inhibits TSH-stimulated cAMP production with IC50 of 2.3 uM.
ML224 (NCGC00242364, ANTAG3) inhibits TSHR basal activity with IC50 of 6.0 uM, displays >20-fold selectivity over LHR and FSHR.
ML224 (NCGC00242364, ANTAG3) inhibits stimulation of thyroid function in female mice.
ML224 (NCGC00242364, ANTAG3) is a potential lead for development of drugs to treat TSHR-mediated hyperthyroidism caused by constitutively activating mutations or stimulating auto-antibodies associated with Graves’ disease.

物理化学性质&存储条件

分子量 525.5949
分子式 C31H31N3O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Acetamide, N-[4-[[5-[3-(2-furanylmethyl)-1,2,3,4-tetrahydro-4-oxo-2-quinazolinyl]-2-methoxyphenyl]methoxy]-3,5-dimethylphenyl]-

参考文献

1. Neumann S, et al. Endocrinology. 2014 Jan;155(1):310-4.

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