CROT Inhibitors
Chemical inhibitors of CROT function through diverse mechanisms that impede CROT's ability to participate in fatty acid metabolism. Orlistat, a lipase inhibitor, reduces the gastrointestinal absorption of fats, leading to a decrease in fatty acid availability for the CROT-mediated conversion of octanoyl-CoA and carnitine into octanoylcarnitine. Perhexiline and Oxfenicine, by inhibiting carnitine palmitoyltransferase (CPT), decrease mitochondrial uptake of long-chain fatty acids, thus reducing the substrate pool for CROT. Similarly, Etomoxir's inhibition of CPT1 curtails the transport of fatty acyl chains into mitochondria, constraining the acyl-carnitine substrates necessary for CROT's enzymatic function. Malonyl-CoA, a natural inhibitor of CPT1, also diminishes the pool of fatty acyl-CoAs, indirectly limiting CROT's activity by substrate deprivation.
Trimetazidine and Ranolazine function by inhibiting enzymes in fatty acid oxidation, thereby lowering the availability of acyl-carnitines for CROT. Mildronate inhibits γ-butyrobetaine hydroxylase, thereby decreasing carnitine synthesis and subsequently the substrate availability for CROT. Metformin indirectly influences CROT by activating AMPK, which can lead to reduced acyl-CoA levels and hence, decreased CROT activity. Fenofibrate activates PPARα, leading to increased fatty acid oxidation, which can deplete the fatty acid substrates required for CROT activity. Nicotinic Acid reduces the mobilization of free fatty acids from adipose tissue, which in turn can limit the substrates available for CROT, resulting in the functional inhibition of the protein's fatty acid transferase activity. Each of these chemicals interacts with different facets of fatty acid metabolism, and by doing so, they can suppress the functional activity of CROT through a reduction in substrate availability or competitive inhibition.
Items 1 to 10 of 11 total
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Lipase Inhibitor, THL | 96829-58-2 | sc-203108 | 50 mg | $51.00 | 7 | |
Orlistat is a lipase inhibitor that reduces the absorption of dietary fats. CROT, carnitine O-octanoyltransferase, is involved in the metabolism of fatty acids by converting octanoyl-CoA and carnitine to octanoylcarnitine. By inhibiting lipase, Orlistat decreases the availability of fatty acids, which can reduce the substrate availability for CROT, thus functionally inhibiting it. | ||||||
rac Perhexiline Maleate | 6724-53-4 | sc-460183 | 10 mg | $184.00 | ||
Perhexiline is a metabolic modulator that inhibits carnitine palmitoyltransferase (CPT), a key enzyme in fatty acid metabolism and closely related to CROT's function. By inhibiting CPT, perhexiline reduces the transport of long-chain fatty acids into the mitochondria, leading to decreased substrate for CROT's activity, thus potentially inhibiting it. | ||||||
(+)-Etomoxir sodium salt | 828934-41-4 | sc-215009 sc-215009A | 5 mg 25 mg | $148.00 $496.00 | 3 | |
Etomoxir inhibits carnitine palmitoyltransferase 1 (CPT1), the enzyme that controls the entry of long-chain acyl-CoA into mitochondria. By inhibiting CPT1, etomoxir reduces the availability of acyl-carnitines for CROT, which may lead to a functional inhibition of CROT by limiting its substrates. | ||||||
Lithium | 7439-93-2 | sc-252954 | 50 g | $214.00 | ||
Malonyl-CoA is a natural inhibitor of carnitine palmitoyltransferase 1 (CPT1). Elevated levels of Malonyl-CoA inhibit CPT1, thereby limiting the transport of fatty acyl-CoAs into the mitochondria for β-oxidation, which in turn can reduce the substrate pool for CROT, leading to its functional inhibition. | ||||||
Trimetazidine Dihydrochloride | 13171-25-0 | sc-220334 | 10 mg | $209.00 | ||
Trimetazidine is a fatty acid oxidation inhibitor that primarily inhibits long-chain 3-ketoacyl-CoA thiolase, which is involved in the β-oxidation of fatty acids. By inhibiting this enzyme, trimetazidine indirectly lowers the availability of acyl-carnitines for CROT, potentially inhibiting its function. | ||||||
4-Hydroxy-L-phenylglycine | 32462-30-9 | sc-254680A sc-254680 | 5 g 10 g | $82.00 $109.00 | ||
Oxfenicine inhibits carnitine palmitoyltransferase (CPT), and it is structurally related to etomoxir. By inhibiting CPT, oxfenicine reduces long-chain fatty acid uptake into mitochondria for β-oxidation, thereby decreasing the substrate availability for CROT and potentially inhibiting its activity. | ||||||
Meldonium | 76144-81-5 | sc-207887 | 100 mg | $252.00 | 1 | |
Mildronate inhibits γ-butyrobetaine hydroxylase, an enzyme involved in the synthesis of carnitine. A reduction in carnitine levels can lower the availability of substrates for CROT's transacylation reaction, potentially leading to functional inhibition of CROT. | ||||||
Ranolazine | 95635-55-5 | sc-212769 | 1 g | $107.00 | 3 | |
Ranolazine is known to inhibit fatty acid oxidation. By shifting the substrate utilization from fatty acids to glucose, ranolazine can decrease the availability of long-chain fatty acids that are substrates for CROT, which may lead to functional inhibition of the enzyme. | ||||||
Metformin-d6, Hydrochloride | 1185166-01-1 | sc-218701 sc-218701A sc-218701B | 1 mg 5 mg 10 mg | $286.00 $806.00 $1510.00 | 1 | |
Metformin activates AMP-activated protein kinase (AMPK), leading to an increase in fatty acid oxidation and a decrease in lipogenesis. This activation could reduce the levels of long-chain acyl-CoAs, thus decreasing the availability of CROT's substrates and functionally inhibiting its activity. | ||||||
Fenofibrate | 49562-28-9 | sc-204751 | 5 g | $40.00 | 9 | |
Fenofibrate is a fibric acid derivative that activates peroxisome proliferator-activated receptor alpha (PPARα), leading to increased fatty acid oxidation. This enhanced oxidation can deplete the long-chain fatty acids required by CROT for its enzymatic activity, thus potentially inhibiting CROT. | ||||||