1421683-12-6
Chemical Structure
Org 274179-0
- CAS No.: 1421683-12-6
- Formula:C28H27F3N2O2
- Molecular Weight:480.52
IUPAC Name: (S)-N-(1-acetyl-4-methyl-4-phenyl-1,2,3,4-tetrahydroquinolin-6-yl)-3-(3-(trifluoromethyl)phenyl)propanamide
InChIKey: IOEFWCOWBKDSQX-MHZLTWQESA-N
SMILES: C[C@]1(C2=CC=CC=C2)C3=CC(NC(CCC4=CC(C(F)(F)F)=CC=C4)=O)=CC=C3N(CC1)C(C)=O
Biological Activity: Org 274179-0 is a low-molecular-weight allosteric thyrotropin receptor (TSH Receptor) antagonist with equipotent follicle-stimulating hormone receptor antagonistic activity and selectivity for the luteinizing hormone receptor. Org 274179-0 binds to the transmembrane domain of the thyrotropin receptor, stabilizes the receptor's inactive state, and blocks agonist-induced and constitutive signaling through the adenylyl cyclase/cAMP and phospholipase C pathways. Org 274179-0 can be used for research on Graves' disease and Graves' ophthalmopathy[1][2][3].
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Org 274179-0 | 98.63% | Org 274179-0 is a low-molecular-weight allosteric thyrotropin receptor (TSH Receptor) antagonist with equipotent follicle-stimulating hormone receptor antagonistic activity and selectivity for the luteinizing hormone receptor. Org 274179-0 binds to the transmembrane domain of the thyrotropin receptor, stabilizes the receptor's inactive state, and blocks agonist-induced and constitutive signaling through the adenylyl cyclase/cAMP and phospholipase C pathways. Org 274179-0 can be used for research on Graves' disease and Graves' ophthalmopathy. | ||||||||||||||||||||
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References
- [1]. van Koppen CJ, et al. Mechanism of action of a nanomolar potent, allosteric antagonist of the thyroid-stimulating hormone receptor. British journal of pharmacology. 2012 Apr;165(7):2314-24. [Content Brief]
- [2]. van Zeijl CJ, et al. Complete inhibition of rhTSH-, Graves' disease IgG-, and M22-induced cAMP production in differentiated orbital fibroblasts by a low-molecular-weight TSHR antagonist. The Journal of clinical endocrinology and metabolism. 2012 May;97(5):E781-5.
- [3]. Faust B, et al. Autoantibody mimicry of hormone action at the thyrotropin receptor. Nature. 2022 Sep;609(7928):846-853.
