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首页-小分子抑制剂&激动剂-GPCR-Thyrotropin Receptor-Org 274179-0
Org 274179-0

Chemical Structure : Org 274179-0

CAS No.: 1421683-12-6

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Org 274179-0 (Org274179-0)

货号: PC-20861Not For Human Use, Lab Use Only.

Org 274179-0 is a highly potent, allosteric antagonist of the thyroid-stimulating hormone receptor (TSH receptor), inhibits bTSH-, hTSH- and M22-mediated CRE-luciferase transactivation in the CHO cell line.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Org 274179-0 is a highly potent, allosteric antagonist of the thyroid-stimulating hormone receptor (TSH receptor), inhibits bTSH-, hTSH- and M22-mediated CRE-luciferase transactivation in the CHO cell line.
Org 274179-0 potently inhibits bTSH- and M22-mediated cAMP formation in FRTL-5 cells with IC50 of 5 and 2 nM, respectively.
Org 274179-0 exhibits equipotent, full antagonist activity at the human FSH receptor with IC50 of 17 nM.
Org 274179-0 does not inhibit TSH receptor activation by acting in a receptor-independent manner, downstream from the TSH receptor.
Org 274179-0 reduces basal cAMP synthesis of the wild-type TSH receptor in wild-type TSH receptor transiently expressed in the CHO cells with IC50 of 22 nM.H receptor transiently expressed in the CHO cells with IC50 of 22 nM.

物理化学性质&存储条件

分子量 480.53
分子式 C28H27F3N2O2
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

O=C(NC1=CC2=C(N(C(C)=O)CC[C@@]2(C)C3=CC=CC=C3)C=C1)CCC4=CC=CC(C(F)(F)F)=C4

参考文献

1. van Koppen CJ, et al. Br J Pharmacol. 2012 Apr;165(7):2314-24.

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