Org 274178-0

Org 274178-0 is a selective thyroid-stimulating hormone receptor (TSHR) antagonist with a pIC50 value for TSHR is 5.03. Org 274178-0 inhibits the activation of cAMP signaling pathway and phospholipase C (PLC) signaling pathway mediated by thyroid-stimulating hormone (TSH) and TSH receptor-stimulating immunoglobulins (TSIs) . Org 274178-0 is promising for research of Graves’ disease and Graves’ ophthalmopathy[1].

Product Specifications

UNSPSC

12352005

Target

TSH Receptor

Related Pathways

GPCR/G Protein

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Endocrinology

Purity

99.40

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

Molecular Formula

C28H27F3N2O2

Molecular Weight

480.52

References & Citations

[1]van Koppen CJ, et al. Mechanism of action of a nanomolar potent, allosteric antagonist of the thyroid-stimulating hormone receptor. Br J Pharmacol. 2012 Apr;165 (7) :2314-24.