Chemical Structure : Org 274179-0
CAS No.:
1421683-12-6
Org 274179-0
(Org274179-0)
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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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480.53
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Formula
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C28H27F3N2O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. van Koppen CJ, et al. Br J Pharmacol. 2012 Apr;165(7):2314-24.
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