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Chemical Structure : Org 274179-0
Catalog No.: 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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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.
| M.Wt | 480.53 | |
| Formula | C28H27F3N2O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. van Koppen CJ, et al. Br J Pharmacol. 2012 Apr;165(7):2314-24.
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