TRPM6 inhibitors are a class of compounds that target the transient receptor potential melastatin 6 (TRPM6) ion channel, which plays a critical role in regulating magnesium homeostasis. TRPM6 is a member of the larger TRP channel family, specifically involved in transporting magnesium and calcium ions across cellular membranes. The channel is expressed predominantly in the kidney and intestine, where it facilitates magnesium absorption and reabsorption. By inhibiting the function of TRPM6, these compounds can modulate ion flux across cell membranes, impacting various intracellular processes dependent on magnesium levels. Magnesium is essential for numerous biochemical reactions, acting as a cofactor for enzymes, influencing cellular metabolism, and maintaining ion gradients across membranes, making the control of its cellular concentrations crucial for physiological processes.
Inhibitors of TRPM6 are studied to gain insights into the biophysical and biochemical mechanisms governing magnesium transport at the molecular level. Understanding the interactions between TRPM6 and its inhibitors helps elucidate the structural features of the ion channel, such as its pore architecture and gating mechanisms. These inhibitors may also provide valuable information about the complex regulatory pathways involved in magnesium homeostasis, including the feedback mechanisms that adjust TRPM6 activity based on cellular magnesium needs. The study of these inhibitors contributes to a broader understanding of ion channel modulation and offers a window into the intricacies of magnesium-related cellular physiology. Additionally, TRPM6 inhibitors are used in basic research to explore how perturbations in magnesium flux influence broader cellular functions, including enzymatic activity, ion balance, and overall cell signaling pathways.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Diazoxide | 364-98-7 | sc-200980 | 1 g | $300.00 | 5 | |
Diazoxide hyperpolarizes the cell membrane by opening potassium channels, which could theoretically suppress the necessity for TRPM6's magnesium transport function, leading to a downregulation of TRPM6 gene expression as a compensatory cellular response. | ||||||
Magnesium sulfate anhydrous | 7487-88-9 | sc-211764 sc-211764A sc-211764B sc-211764C sc-211764D | 500 g 1 kg 2.5 kg 5 kg 10 kg | $45.00 $68.00 $160.00 $240.00 $410.00 | 3 | |
Elevated intracellular magnesium levels provided by magnesium sulfate could trigger a negative feedback loop, reducing TRPM6 expression to balance magnesium uptake and prevent cellular toxicity associated with magnesium excess. | ||||||
β-Estradiol | 50-28-2 | sc-204431 sc-204431A | 500 mg 5 g | $62.00 $178.00 | 8 | |
β-Estradiol may exert a repressive effect on TRPM6 expression by activating estrogen receptors that engage with specific DNA sequences in the TRPM6 gene promoter, thereby recruiting corepressor complexes that suppress gene transcription. | ||||||
Progesterone | 57-83-0 | sc-296138A sc-296138 sc-296138B | 1 g 5 g 50 g | $20.00 $51.00 $292.00 | 3 | |
Progesterone could downregulate TRPM6 expression by binding to its nuclear hormone receptors, which may then interact with co-repressors to silence TRPM6 gene transcription in a tissue-specific manner. | ||||||
Amiloride | 2609-46-3 | sc-337527 | 1 g | $290.00 | 7 | |
Amiloride, by diminishing cellular sodium uptake, could create an ionic imbalance, prompting a decrease in TRPM6 expression as part of a broader adjustment to ion transport homeostasis. | ||||||
Verapamil | 52-53-9 | sc-507373 | 1 g | $367.00 | ||
Verapamil's blockade of calcium channels might provoke a compensatory cellular response that includes the suppression of TRPM6 gene expression to recalibrate the overall cation transport within the cell. | ||||||
FK-506 | 104987-11-3 | sc-24649 sc-24649A | 5 mg 10 mg | $76.00 $148.00 | 9 | |
FK-506's inhibition of calcineurin could lead to a reduced transcription of TRPM6 by preventing the dephosphorylation and subsequent activation of transcription factors that are critical for TRPM6 gene expression. | ||||||
Cyclosporin A | 59865-13-3 | sc-3503 sc-3503-CW sc-3503A sc-3503B sc-3503C sc-3503D | 100 mg 100 mg 500 mg 10 g 25 g 100 g | $62.00 $90.00 $299.00 $475.00 $1015.00 $2099.00 | 69 | |
Cyclosporin A, through calcineurin inhibition, could repress TRPM6 gene expression by maintaining the phosphorylation state of transcription factors, thereby preventing their translocation to the nucleus and binding to the TRPM6 promoter. | ||||||
Lithium | 7439-93-2 | sc-252954 | 50 g | $214.00 | ||
Lithium's inhibition of glycogen synthase kinase 3 beta (GSK-3β) could reduce TRPM6 expression by altering the transcription factor dynamics that normally enhance TRPM6 gene transcription. | ||||||
Forskolin | 66575-29-9 | sc-3562 sc-3562A sc-3562B sc-3562C sc-3562D | 5 mg 50 mg 1 g 2 g 5 g | $76.00 $150.00 $725.00 $1385.00 $2050.00 | 73 | |
Forskolin may indirectly lead to a reduction in TRPM6 expression by elevating cAMP, which can activate protein kinase A (PKA) and subsequently alter the phosphorylation status of transcriptional regulators governing TRPM6 gene activity. | ||||||