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NCGC00161856

Chemical Structure : NCGC00161856

CAS No.: 361187-13-5

NCGC00161856 (NCGC 00161856)

Catalog No.: PC-20499Not For Human Use, Lab Use Only.

NCGC00161856 is the first small-molecule ligand and inverse agonist of TSHR, inhibits basal cAMP production by TSHR in HEK-EM 293 cells stably expressing TSHRs with IC50 of 3.0 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

NCGC00161856 is the first small-molecule ligand and inverse agonist of TSHR, inhibits basal cAMP production by TSHR in HEK-EM 293 cells stably expressing TSHRs with IC50 of 3.0 uM.
NCGC00161856 also inhibits TSH-stimulated cAMP production with IC50 of 0.78 uM.
NCGC00161856 is a competitive antagonist of TSH-stimulated signaling.
NCGC00161856 (30 uM) inhibits the basal expression of mRNAs for TPO, TSHR, TG, NIS, and DIO2 in primary cultures of human thyrocytes.

Physicochemical Properties

M.Wt 468.55
Formula C29H28N2O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

O=C1N(CC2=CC=CO2)C(C3=CC=C(OC)C(COC4=C(C)C=CC=C4C)=C3)NC5=C1C=CC=C5

References

1. Neumann S, et al. Endocrinology 151:3454–3459.

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