tr antagonist 1

TR antagonist 1 is a highly potent thyroid hormone receptor (TR) antagonist (IC50 of 36 and 22 nM for TRα and TRβ, respectively) that can be used to study diseases caused by endocrine abnormalities.

OT-R antagonist 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM). OT-R antagonist 1 is a new effective and selective nonpeptide low molecular weight OT-R antagonist.

(E/Z)-OT-R antagonist 1 is a mixture of the E/Z configurations of OT-R antagonist 1. This compound is a novel, potent, selective, non-peptide OT-R antagonist that inhibits oxytocin-induced intracellular Ca2+ activity with an IC50 of 8 nM.

CELT-133 is a selective fluorescent antagonist for the hα1A adrenergic receptor, demonstrating complete selectivity towards α1A over α2A receptors, with a Ki of 5 nM and 15% displacement at 1 μM in radioligand binding assays, respectively. It displays equivalent affinity across all α1 adrenergic receptor subtypes. Notably, CELT-133 features excitation and emission maxima (λ) at 560 and 571 nm, respectively, making it suitable for use as an acceptor dye in time-resolved Förster resonance energy transfer (TR-FRET) assays when paired with the CoraFluor 1 TR-FRET donor.