Thyroid Hormone Receptor Antagonist

NH-3 is an orally active, reversible thyroid hormone receptor (THR) antagonist with an IC₅₀ of 55 nM. NH-3, a derivative of the selective thyromi-metic GC-1, inhibits binding of thyroid hormones to their receptor and that inhibits cofactor recruitment. NH-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

(D-Trp12,Tyr34)-pTH (7-34) amide (bovine) is a potent and competitive antagonist of parathyroid hormone (PTH), with a K_i of 69 nM in bovine renal cortical membrane. (D-Trp12,Tyr34)-pTH (7-34) amide (bovine) can be used for growth and development regulation.

TR antagonist 1 is a high-affinity thyroid hormone receptor (TR) antagonist with IC₅₀s of 36 and 22 nM for TRα and TRβ, respectively.

Thyroid hormone receptor antagonist (1-850) is a competitive, selective and high-affinity thyroid hormone receptor (TR) antagonist with an IC₅₀ of 1.5 μM for antagonizing the effect of T3 on TR. Thyroid hormone receptor antagonist (1-850) blocks T3-mediated interaction of TRα and TRβ with nuclear receptor coactivator. Thyroid hormone receptor antagonist (1-850) has no effect on the activity of RARα.

VK-0214 is an agonist of the thyroid β receptor (TRβ). By activating the expression of ABCD2, it can reduce the accumulation of very long-chain fatty acids (VLCFAs) and further alleviate glioblastoma multiforme. VK-0214 has the effect of regulating fatty acid metabolism and can be used in the research of X-linked adrenoleukodystrophy (X-ALD).

TR antagonist 2 (Compound 10a) is a competitive thyroid hormone receptors (TRα/β) antagonist (IC₅₀=47 nM). TR antagonist 2 competes with triiodothyronine (T₃) for binding to the ligand-binding domain of TR to block receptor-coactivator complex formation and inhibit target gene transcription, reducing thyroid hormone-mediated hypermetabolic effects. TR antagonist 2 is promising for research of hyperthyroidism (e.g., Graves' disease) and thyrotoxicosis.

Parathyroid hormone (1-34) (rat) (acetate) is a parathyroid hormone. Parathyroid hormone (1-34) (rat) improves both cortical and cancellous bone structure. Parathyroid hormone (1-34) (rat) can be used for the research of osteoporosis.

GC 14 is a selective thyroid hormone receptor antagonist, with IC₅₀ values of 35 nM and 200 nM for hTRβ and hTRα, respectively.

MLS000389544 is a selective and potent methylsulfonylnitrobenzoate thyroid hormone receptor β (TRβ) antagonist that blocks the association of TRβ with steroid receptor coactivator 2 (SRC2).

THR-β agonist 12 is an orally active, potent, and highly selective thyroid hormone receptor β (THR-β) agonist (EC₅₀ = 36 nM). THR-β agonist 12 shows no significant activity against THRα and exhibits no cardiotoxicity in vivo. THR-β agonist 12 inhibits lipid synthesis by activating the AMPK-ACC-SREBP1 signaling axis. THR-β agonist 12 can be used on research into metabolic dysfunction-associated steatohepatitis (MASH) and related metabolic diseases.

TR antagonist 1 (Standard) is the analytical standard of TR antagonist 1 (HY-111443). This product is intended for research and analytical applications. TR antagonist 1 is a high-affinity thyroid hormone receptor (TR) antagonist with IC₅₀s of 36 and 22 nM for TRα and TRβ, respectively.