TRα Inhibitors
TRα inhibitors belong to a class of chemical compounds designed to target and modulate the activity of the thyroid hormone receptor alpha (TRα). These receptors are part of the nuclear hormone receptor superfamily, playing a crucial role in the regulation of gene expression in response to thyroid hormones. TRα exists in two isoforms, TRα1 and TRα2, with TRα1 being the more widely studied and expressed isoform. The primary function of TRα is to bind to thyroid hormones, specifically triiodothyronine (T3), and mediate their effects on various physiological processes, including metabolism, growth, and development.
TRα inhibitors work by interfering with the binding of T3 to the receptor, thereby modulating its transcriptional activity. These inhibitors can act as antagonists, stopping the receptor from activating target genes, or as partial agonists, eliciting a less potent response compared to T3. They achieve this by binding to the ligand-binding domain of TRα and altering its conformation, thus inhibiting its ability to bind to thyroid hormones or co-activators required for gene transcription. This modulation of TRα activity can have profound effects on the regulation of gene expression and cellular processes, making TRα inhibitors a valuable tool in studying the role of thyroid hormones in various physiological and pathological contexts.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Amiodarone | 1951-25-3 | sc-480089 | 5 g | $312.00 | ||
Amiodarone is known to have an inhibitory effect on thyroid hormone synthesis and may indirectly affect TRα expression levels by altering thyroid hormone concentrations. | ||||||
6-Propyl-2-thiouracil | 51-52-5 | sc-214383 sc-214383A sc-214383B sc-214383C | 10 g 25 g 100 g 1 kg | $36.00 $55.00 $220.00 $1958.00 | ||
As a thyroid hormone synthesis inhibitor, 6-Propyl-2-thiouracil might reduce the levels of thyroid hormones, subsequently affecting the expression of hormone-dependent receptors like TRα. | ||||||
4-Hydroxy-2-mercapto-6-methylpyrimidine | 56-04-2 | sc-238861 | 100 g | $111.00 | ||
4-Hydroxy-2-mercapto-6-methylpyrimidine decreases the availability of thyroid hormones and thus influencing TRα expression. | ||||||
Methimazole | 60-56-0 | sc-205747 sc-205747A | 10 g 25 g | $69.00 $110.00 | 4 | |
Methimazole inhibits the synthesis of thyroid hormones, which could lead to a reduction in TRα expression due to lower hormone levels. | ||||||
Ketoconazole | 65277-42-1 | sc-200496 sc-200496A | 50 mg 500 mg | $62.00 $260.00 | 21 | |
Ketoconazole can inhibit steroidogenesis and might exert its effect on TRα by reducing thyroid hormone levels indirectly. | ||||||
Rifampicin | 13292-46-1 | sc-200910 sc-200910A sc-200910B sc-200910C | 1 g 5 g 100 g 250 g | $95.00 $322.00 $663.00 $1438.00 | 6 | |
As an antibiotic, Rifampicin can induce hepatic enzymes that metabolize thyroid hormones, potentially reducing their levels and affecting TRα expression. | ||||||
Lithium | 7439-93-2 | sc-252954 | 50 g | $214.00 | ||
Lithium is known to affect thyroid hormone synthesis and might therefore have an inhibitory effect on the expression of TRα. | ||||||
Bexarotene | 153559-49-0 | sc-217753 sc-217753A | 10 mg 100 mg | $54.00 $245.00 | 6 | |
Although primarily a retinoid X receptor (RXR) agonist, bexarotene can affect thyroid hormone levels and may thus alter TRα expression indirectly. | ||||||