MEA-1 Inhibitors
MEA-1 inhibitors are a class of chemical compounds designed to specifically target and modulate the enzymatic activity of the enzyme monoacylglycerol lipase (MAGL), also known as MEA-1. MAGL plays a key role in lipid metabolism, particularly in the hydrolysis of monoacylglycerols (MAGs) into fatty acids and glycerol. These inhibitors act by binding to the active site of MAGL, blocking the enzyme's ability to catalyze the breakdown of monoacylglycerols. This inhibition leads to the accumulation of monoacylglycerols, such as 2-arachidonoylglycerol (2-AG), which is a key endocannabinoid involved in various physiological processes. The structural diversity of MEA-1 inhibitors allows them to interact with the enzyme in different ways, ranging from covalent inhibitors that irreversibly bind to the active site to non-covalent inhibitors that exert reversible binding. The design of these inhibitors often focuses on optimizing their selectivity for MAGL over other related enzymes in lipid metabolism, such as fatty acid amide hydrolase (FAAH), to avoid off-target effects.
Chemically, MEA-1 inhibitors encompass a wide range of molecular scaffolds. Many of these inhibitors are derived from small organic molecules that incorporate specific functional groups capable of interacting with the catalytic residues of the enzyme's active site. Structural studies using X-ray crystallography and computational modeling have greatly advanced the understanding of how these inhibitors bind to MAGL, providing insights into structure-activity relationships (SARs) that guide the development of more potent and selective compounds. Additionally, the chemical optimization of MEA-1 inhibitors involves improving their stability, solubility, and bioavailability, ensuring they can interact with MAGL effectively under physiological conditions. The structural diversity of MEA-1 inhibitors and their ability to modulate lipid metabolism pathways make them important tools in the study of lipid signaling and enzymatic regulation.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Flutamide | 13311-84-7 | sc-204757 sc-204757A sc-204757D sc-204757B sc-204757C | 1 g 5 g 25 g 500 g 1 kg | $46.00 $153.00 $168.00 $515.00 $923.00 | 4 | |
Flutamide may downregulate MEA-1 by competitively binding to androgen receptors, reducing the transcriptional activity that would normally be upregulated by androgens, potentially essential for MEA-1 expression in male gonad development. | ||||||
Ketoconazole | 65277-42-1 | sc-200496 sc-200496A | 50 mg 500 mg | $62.00 $260.00 | 21 | |
Ketoconazole has the potential to reduce MEA-1 expression by inhibiting steroidogenesis, leading to a deficit in androgen levels that could be critical for sustaining MEA-1 expression in testicular tissue. | ||||||
Spironolactone | 52-01-7 | sc-204294 | 50 mg | $107.00 | 3 | |
Spironolactone could decrease MEA-1 expression due to its antiandrogenic properties, which may lead to reduced androgen receptor activation, a pathway that could be integral for MEA-1 transcription in the context of male reproductive development. | ||||||
Bicalutamide | 90357-06-5 | sc-202976 sc-202976A | 100 mg 500 mg | $41.00 $143.00 | 27 | |
Bicalutamide might attenuate MEA-1 expression by obstructing the androgen receptor signaling pathway, potentially decreasing the expression of androgen-responsive genes like MEA-1. | ||||||
Finasteride | 98319-26-7 | sc-203954 | 50 mg | $103.00 | 3 | |
Finasteride could indirectly lead to a decrease in MEA-1 expression by inhibiting the conversion of testosterone to the more potent dihydrotestosterone (DHT), potentially diminishing the androgen-driven expression of MEA-1. | ||||||
Dutasteride | 164656-23-9 | sc-207600 | 10 mg | $167.00 | 2 | |
Dutasteride may diminish MEA-1 expression through its robust inhibition of both isoforms of 5-alpha reductase, resulting in a reduction of DHT levels that may be critical for MEA-1 gene transcription. | ||||||
MDV3100 | 915087-33-1 | sc-364354 sc-364354A | 5 mg 50 mg | $240.00 $1030.00 | 7 | |
MDV3100 could suppress MEA-1 expression by acting as a potent antagonist of the androgen receptor, potentially reducing the expression of genes that are regulated by androgen signaling, including MEA-1. | ||||||
Diethylstilbestrol | 56-53-1 | sc-204720 sc-204720A sc-204720B sc-204720C sc-204720D | 1 g 5 g 25 g 50 g 100 g | $70.00 $281.00 $536.00 $1076.00 $2142.00 | 3 | |
Diethylstilbestrol may suppress MEA-1 expression by acting as a potent synthetic estrogen, possibly disrupting the hormonal balance and downregulating genes that are typically promoted by androgens. | ||||||
Busulfan | 55-98-1 | sc-204658 | 10 g | $48.00 | 3 | |
Busulfan might reduce MEA-1 expression due to its alkylating properties, which can lead to testicular atrophy and suppression of spermatogenesis, processes that might be associated with MEA-1 activity. | ||||||
Letrozole | 112809-51-5 | sc-204791 sc-204791A | 25 mg 50 mg | $85.00 $144.00 | 5 | |
Letrozole has the potential to downregulate MEA-1 expression by inhibiting aromatase activity, thereby reducing estrogen synthesis and possibly leading to a hormonal environment that does not favor MEA-1 expression. | ||||||