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Catalog No.
Product Name
Application
Product Information
Citations
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α-glucosidase/α-amylase Dual Inhibitor
2,7"-Phloroglucinol-6,6'-bieckol functions as a dual inhibitor of α-glucosidase and α-amylase, exhibiting IC50 values of 6.94 μM and 23.35 μM, respectively. This compound has demonstrated the ability to mitigate postprandial hyperglycemia in diabetic mouse models. 2,7"-Phloroglucinol-6,6'-bieckol is valuable for research focused on diabetes and glucose metabolism. -
α-glucosidase/α-amylase enzyme Dual Inhibitor
α-Amylase/α-Glucosidase-IN-7 is a competitive dual inhibitor targeting α-glucosidase and α-amylase, demonstrating IC50 values of 18.52 µM and 20.25 µM, respectively. Additionally, this compound effectively inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 values of 9.25 µM and 10.06 µM. α-Amylase/α-Glucosidase-IN-7 is valuable for research applications related to diabetes and Alzheimer’s disease. -
α-Amylase Inhibitor
Quercetin 3-(6″-caffeoylsophoroside) is a potent α-amylase inhibitor with an IC50 of 73.66 μg/mL, demonstrating significant potential for antidiabetic applications. Isolated from the hydro-methanolic extract of Cardamine hirsuta Linn., this compound exerts its biological activity by reducing oxidative stress and inhibiting α-amylase. It is a valuable tool for researchers investigating the mechanisms and treatment strategies for diabetes mellitus. -
α-Amylase/α-Glucosidase Inhibitor
3,4,6-Tri-O-galloyl-D-glucose is a mixed-type inhibitor of α-amylase and α-glucosidase, with an IC50 of 334.6 μM against porcine α-amylase and 46.5 μM against yeast α-glucosidase. This compound demonstrates free radical scavenging capabilities, ferric-reducing power, and significant antioxidant activity. Its properties make it a valuable tool for research focused on diabetes and related metabolic disorders. -
α-Amylase Inhibitor
α-Amylase-IN-13 is a selective inhibitor of α-amylase that operates via a mixed inhibition mechanism (IC50 = 0.71 μM). This brain-penetrant compound has demonstrated the ability to significantly lower blood glucose levels in diabetic rat models and promotes notable histopathological improvements in the kidney, liver, and pancreas. α-Amylase-IN-13 is a valuable tool for investigating diabetic complications and evaluating therapeutic strategies for diabetes management. -
α-Amylase Inhibitor
Gibbestatin B is an α-amylase inhibitor that targets the expression of α-amylase induced by gibberellin in de-embryonated rice and barley, with an IC50 ranging from 25 to 50 ppm. Its specific action on α-amylase makes it a valuable tool in studying carbohydrate metabolism and plant physiological responses to gibberellin. Notably, Gibbestatin B exhibits no antibacterial, anti-yeast, or antifungal activity at concentrations of 100 ppm, allowing for focused research on its enzymatic inhibition. -
α-Amylase Inhibitor
α-Amylase-IN-10 is a potent inhibitor of α-amylase, exhibiting an IC50 value of 5.00 µM. This compound is valuable for research focusing on type 2 diabetes mellitus, providing insights into carbohydrate metabolism and potential therapeutic strategies. Its ability to modulate α-amylase activity makes it a useful tool in studies aimed at understanding metabolic disorders and developing anti-diabetic agents. -
α-Amylase Inhibitor
α-Amylase-IN-7 is a specific inhibitor of α-Amylase, exhibiting an IC50 value of 40 μM. This compound demonstrates potential as an antidiabetic agent by regulating carbohydrate metabolism. Research applications may include the study of glycemic control and the development of therapeutic strategies for diabetes management. -
PCSK9 Inhibitor
DC371739 is a potent PCSK9 inhibitor that exhibits oral bioactivity. It effectively reduces the mRNA expression of both PCSK9 and ANGPTL3, while simultaneously increasing the protein expression of LDLR. This compound holds promise for research applications related to hyperlipidemia and the modulation of lipid metabolism. -
CA/MAO-B Inhibitor
CA/MAO-B-IN-1 is a potent dual inhibitor of human brain carbonic anhydrases (CA) and Monoamine Oxidase-B (MAO-B), exhibiting IC50 values of 8.8 nM and 7.0 nM, respectively. This compound demonstrates significant potential for research applications related to neurological conditions, as it may modulate both enzymatic activity and associated pathways. Additionally, in silico predictions suggest favorable oral absorption of 71.9%, making it a relevant candidate for further pharmacological studies. -
CES Inhibitor
Dibromsalicil is a selective inhibitor of carboxylesterases (CES), exhibiting inhibitory activity with IC50 values of 72.7 nM against human intestinal carboxylesterase (hiCE) and 53.5 nM against rabbit liver carboxylesterase (rCE). This compound demonstrates minimal activity against human liver carboxylesterase (hCE1) and cholinesterase, making it a valuable tool for research applications focused on drug metabolism and enzymatic activity modulation. Its specificity for hiCE and rCE positions Dibromsalicil as an important reagent for studying carboxylesterase-related pathways. -
hCES2A Inhibitor
Isolicoflavonol is a potent inhibitor of hCES2A (Human carboxylesterase 2), exhibiting reversible and mixed inhibition of fluorescein diacetate hydrolysis. With Ki values below 1.0 μM, it serves as a valuable tool for exploring enzymatic activity and regulation in biochemical research. Its specificity and efficacy make it suitable for investigations into drug metabolism and enzyme kinetics. -
hCES2 Inhibitor
CES2-IN-1 is a reversible and selective inhibitor of human carboxylesterase 2 (hCES2), exhibiting an IC50 value of 6.72 μM. This compound effectively reduces CES2 levels in living cells, making it useful for studies involving drug metabolism. CES2-IN-1 has demonstrated efficacy in preclinical models for conditions such as irinotecan-induced delayed diarrhea and dextran sulfate sodium (DSS)-induced ulcerative colitis, supporting its application in gastrointestinal research. -
Carboxylesterase Inhibitor
Tanshinone IIA anhydride is a potent irreversible inhibitor of human carboxylesterases, demonstrating Ki values of 1.9 nM for human carboxylesterase 1 and 1.4 nM for human intestinal carboxylesterase. This compound is valuable for studying the regulatory mechanisms of esterases in various biological processes. Its application extends to biochemical studies focused on enzyme inhibition and metabolic pathway analysis. -
CE Inhibitor
1-Methylisatin is a selective carboxylesterase (CE) inhibitor, exhibiting inhibitory constants of 38.2 μM for human isoform CE (hiCE) and 5.38 μM for human carboxylesterase 1 (hCE1). This compound interacts with human adult hemoglobin through hydrophobic binding and electrostatic interactions. 1-Methylisatin serves as a valuable tool for investigating the regulation of drug metabolism and biochemical pathways in vivo. -
PL/hCES1A Inhibitor
Pancreatic lipase/Carboxylesterase 1-IN-1 is a potent inhibitor of pancreatic lipase (PL) and human carboxylesterase 1A (hCES1A), displaying IC50 values of 2.13 µM and 0.055 µM, respectively. This dual inhibition makes it a valuable tool for studying lipid metabolism and the enzymatic pathways related to drug metabolism and detoxification processes. It has potential applications in research focused on obesity, metabolic disorders, and pharmacokinetics. -
hCES2A Inhibitor
Gancaonin I is an isoflavone that serves as a moderate inhibitor of human carboxylesterase 2 (hCES2A) with an IC50 of 1.72 μM. It effectively inhibits the hCES2A-mediated hydrolysis of fluorescein diacetate (FD), making it a valuable tool for research applications involving enzyme regulation and drug metabolism studies. -
Carboxylesterase (CES) Inhibitor
PMPMEase-IN-1 is a selective inhibitor of carboxylesterase (CES) that targets PMPMEase activity, thereby modulating protein methylation processes. This compound demonstrates potential anti-cancer activity by enhancing sensitivity to polyisoprenyl derivatives, with an effective concentration (EC50) observed in inducing degeneration of human neuroblastoma SH-SY5Y cells. By specifically inhibiting PMPMEase, PMPMEase-IN-1 may contribute to the regulation of polyisoprenyl protein metabolism, promoting normal cellular function. Its utility in research could pave the way for therapeutic advancements in treating cancer and degenerative diseases. -
hCES2A Inhibitor
CES2A-IN-3 is a potent inhibitor of human carboxylesterase 2A (hCES2A), acting through a serine-targeting covalent mechanism with an IC50 of 0.12 nM. This compound holds significant promise for research applications related to gastrointestinal disorders, including diarrhea and ulcerative colitis, by modulating enzyme activity linked to these conditions. Its high specificity and efficacy make it an essential tool for exploring hCES2A's role in related biological pathways. -
Carboxylesterase Inhibitor
Carboxylesterase-IN-4 is a highly potent inhibitor of carboxylesterase, exhibiting an IC50 of 1.58 nM. This compound facilitates research into cholesterolemia by effectively modulating carboxylesterase activity, making it a valuable tool in the study of lipid metabolism and associated disorders. -
Carboxylesterase Inhibitor
Carboxylesterase-IN-5 is an irreversible and competitive inhibitor of carboxylesterase with an IC50 of 21.7 nM for porcine liver carboxylesterase. This reagent is suitable for studies investigating the role of carboxylesterases in metabolic processes and is particularly relevant for research pertaining to hypocholesterolemia. Its specificity and potency make it a valuable tool in biochemical and pharmacological investigations. -
Carboxylesterase Inhibitor
Carboxylesterase-IN-1 is a potent carboxylesterase inhibitor, demonstrating significant inhibitory activity at a concentration of 50 μg/mL. By interfering with carboxylesterase function, it serves as a valuable tool in the study of enzyme regulation and pesticide effects on biological systems. This compound is suitable for research applications focusing on enzyme inhibition and the molecular mechanisms of pesticide action. -
Carboxylesterase (CES) Inhibitor
SQ-24798 is a potent inhibitor of carboxylesterase (CES), specifically designed to bind the zinc ion in the enzyme's active site via its sulfhydryl group, leading to effective enzyme inhibition. This compound exhibits high affinity and specificity, making it a valuable tool in biochemical research focused on understanding CES-related pathways. Its applications include studying drug metabolism and the physiological roles of CES in various biological processes. -
AChE/CES Inhibitor
Heptenophos is a potent inhibitor of acetylcholinesterase (AChE) and plasma carboxylesterase (CES). By obstructing AChE activity, Heptenophos leads to the accumulation of acetylcholine at cholinergic synapses, which can result in symptoms characteristic of organophosphate poisoning. Its rapid toxicity in animal models, such as male albino mice, allows for the investigation of detoxification strategies, particularly in conjunction with agents like obidoxime and Memantine. This compound is widely utilized in research exploring the mechanisms underlying organophosphate effects and potential antidotal treatments. -
CETP Inhibitor
Obicetrapib potassium is a selective cholesteryl ester transfer protein (CETP) inhibitor that plays a crucial role in regulating lipid metabolism by modulating levels of LDL cholesterol (LDL-C), apolipoprotein B (apoB), and high-density lipoprotein cholesterol (HDL-C). This compound is valuable for research applications focused on dyslipidemia and associated cardiovascular diseases, providing insights into lipid transport mechanisms and potential therapeutic interventions. -
CETP Inhibitor
CP-532623 is a selective inhibitor of cholesteryl ester transfer protein (CETP), designed to elevate high-density lipoprotein (HDL) cholesterol levels. This compound is a close structural analogue of Torcetrapib and exhibits significant lipophilicity. CP-532623 is utilized in research exploring lipid metabolism, cardiovascular disease, and the modulation of plasma lipoprotein profiles. -
CETP Inhibitor
MK-8262 is a potent inhibitor of cholesteryl ester transfer protein (CETP) with an IC50 of 53 nM and a log D of 5.3, indicating good oral bioavailability. This bistrifluoromethyl analogue is primarily used in research related to coronary heart disease (CHD), specifically studying the dynamics of high-density lipoprotein (HDL) and low-density lipoprotein (LDL). Its inhibition of CETP activity positions it as a valuable tool for investigating lipid metabolism and potential therapeutic approaches for cardiovascular conditions. -
CETP Inhibitor
TAP311 is a selective inhibitor of cholesteryl ester transfer protein (CETP), exhibiting an IC50 of 62 nM. By blocking CETP activity, TAP311 effectively regulates lipid metabolism and enhances high-density lipoprotein (HDL) levels. This compound is valuable for research focused on cardiovascular disease, specifically in studies investigating the role of CETP in lipid regulation and atherosclerosis. -
CETP Inhibitor
BMS-795311 is a potent cholesteryl ester transfer protein (CETP) inhibitor, demonstrating an IC50 of 4 nM in enzyme-based scintillation proximity assays and 0.22 μM in human whole plasma assays. This compound is utilized in research to explore lipid metabolism and its implications in cardiovascular diseases. Its oral bioavailability supports in vivo studies, making it a valuable tool in understanding CETP's role in lipid transport and potential therapeutic strategies for dyslipidemia. -
CETP Inhibitor
CETP-IN-4 is a selective inhibitor of cholesteryl ester transfer protein (CETP), which plays a crucial role in lipid metabolism. By inhibiting CETP activity, this compound has the potential to elevate high-density lipoprotein (HDL) cholesterol levels, thereby influencing cardiovascular health. CETP-IN-4 is suitable for research applications aimed at understanding lipid metabolism disorders and developing therapeutic strategies for cardiovascular diseases. -
CETP Inhibitor
CP-800569 is an orally active inhibitor of cholesteryl ester transfer protein (CETP). This compound has been shown to effectively reduce low-density lipoprotein levels and postprandial triglycerides while increasing high-density lipoprotein levels. CP-800569 is valuable for research focusing on metabolic diseases, providing insights into lipid metabolism and cardiovascular health. -
CETP/HMGCR Inhibitor
Colestolone is a 15-ketosterol compound that functions as an inhibitor of both HMG-CoA reductase and cholesteryl ester transfer protein (CETP), with an in vitro IC50 value of 660 μM. This compound exhibits cholesterol-lowering properties and is valuable in researching endocrine and metabolic diseases, particularly hyperlipidemia. Its dual action on lipid metabolism makes Colestolone a significant tool for studying cholesterol regulation and associated disorders. -
Cholesteryl Ester Transfer Protein Inhibitor
DRL-17822 is a selective inhibitor of cholesteryl ester transfer protein (CETP). This compound effectively elevates high-density lipoprotein (HDL) levels, which is key in the management of type II hyperlipidemia and atherosclerotic cardiovascular disease. Notably, the bioavailability of DRL-17822 is enhanced after a high-fat meal, with improved exposure observed in the fasted state compared to its nanocrystal formulation. This makes DRL-17822 a valuable tool for research focused on lipid metabolism and cardiovascular health. -
CETP Inhibitor
CP 524515 is a potent inhibitor of cholesteryl ester transfer protein (CETP), which contributes to the increase of high-density lipoprotein (HDL) cholesterol levels. This compound has significant implications in cardiovascular research, particularly in the study of lipid metabolism and atherosclerosis. Its ability to modulate lipid profiles makes it a valuable tool for exploring therapeutic strategies aimed at cardiovascular diseases. -
CETP Inhibitor
Erabulenol A is a potent inhibitor of cholesteryl ester transfer protein (CETP), which plays a critical role in lipid metabolism. This compound, isolated from Penicillium sp., exhibits significant biological activity in modulating lipid levels and improving plasma HDL cholesterol levels. Erabulenol A is valuable for research applications focused on cardiovascular diseases and metabolic disorders related to cholesterol transport and homeostasis. -
hMAO-B/MB-COMT Inhibitor
hMAO-B/MB-COMT-IN-1 is a dual inhibitor of human monoamine oxidase B (hMAO-B) and membrane-bound catechol-O-methyltransferase (MB-COMT), exhibiting IC50 values of 2.5 µM and 3.84 µM, respectively. This compound is effective in protecting cells from oxidative damage, making it a valuable tool for studying neurodegenerative diseases, including Parkinson's Disease. Its dual inhibition profile provides insights into the molecular mechanisms underlying these conditions and aids in the development of potential therapeutic strategies. -
hMAO-B/MB-COMT Inhibitor
hMAO-B/MB-COMT-IN-2 is a potent dual inhibitor of hMAO-B and MB-COMT, exhibiting IC50 values of 4.27 μM and 2.69 μM, respectively. This compound effectively protects cells from oxidative damage, making it valuable for studies related to neurodegenerative diseases. hMAO-B/MB-COMT-IN-2 is particularly relevant in the research of conditions such as Parkinson’s Disease, offering insights into potential therapeutic strategies. -
CYP11A1 Inhibitor
Opevesostat is a selective inhibitor of CYP11A1, designed for oral administration. This compound demonstrates significant potential in the study of metastatic castration-resistant prostate cancer (mCRPC), supporting research into therapeutic approaches targeting steroidogenesis. Its specificity for CYP11A1 makes it a valuable tool in understanding the biochemical pathways involved in androgen synthesis and cancer progression. -
CYP2C19 Inhibitor
(S)-(+)-N-3-Benzylnirvanol is a selective and competitive inhibitor of the cytochrome P450 isoform CYP2C19, exhibiting a Ki value of 250 nM. This compound displays low inhibition against other CYP isoforms, including CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2D6, CYP2E1, and CYP3A4. It is primarily utilized in pharmacological research to study drug metabolism and drug-drug interactions involving CYP2C19. -
CYP2J2 Inhibitor
LKY-047 is a selective reversible inhibitor of cytochrome P450 2J2 (CYP2J2), exhibiting an IC50 of 1.7 μM. This compound demonstrates high specificity, remaining inactive against other human cytochrome P450 isoforms, including CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A. LKY-047 is utilized in research applications focused on understanding the role of CYP2J2 in drug metabolism and cardiovascular diseases. -
CYP3A4 Inhibitor
6',7'-Dihydroxybergamottin (6′,7′-DHB) is a furanocoumarin that acts as a potent inhibitor of the cytochrome P450 enzyme CYP3A4. This compound is instrumental in studying drug metabolism and interactions, making it valuable for research in pharmacokinetics and toxicology. Its ability to modulate CYP3A4 activity has implications for understanding the effects of herbal supplements and dietary compounds on drug efficacy and safety. -
CYP Epoxygenase Inhibitor
MS-PPOH is a selective inhibitor of cytochrome P450 epoxygenases, primarily targeting CYP2C8 and CYP2C9 with IC50 values of 15 μM and 11 μM, respectively. This compound demonstrates key biological activity through the modulation of enzymatic metabolism pathways, making it valuable for research in pharmacology and toxicology. Additionally, MS-PPOH features an alkyne group, enabling its application in click chemistry via copper-catalyzed azide-alkyne cycloaddition (CuAAc) for tagging and labeling in various biochemical assays. -
CYP11B2 Inhibitor
Lorundrostat is a selective inhibitor of CYP11B2, targeting aldosterone synthase. This compound exhibits significant antihypertensive activity and is primarily utilized in research focused on the management of high blood pressure and related cardiovascular conditions. Its ability to modulate aldosterone levels makes it a valuable tool in studying endocrine and cardiovascular function. -
CYP3Aa Inhibitor
Azamulin is an irreversible, highly selective inhibitor of human CYP3A4, effectively targeting this crucial cytochrome P450 enzyme. With IC50 values ranging from 0.03 to 0.24 μM, Azamulin exhibits potent CYP3A inhibition, making it a valuable tool in the study of drug metabolism and pharmacokinetics. Additionally, it holds potential for research in anti-infection therapies, providing insights into therapeutic strategies against infectious agents. -
CYP2E1 Inhibitor
Fomepizole hydrochloride is a potent inhibitor of cytochrome P450 enzyme CYP2E1. It functions as a competitive inhibitor of alcohol dehydrogenase, effectively preventing the metabolic conversion of methanol and ethylene glycol into harmful metabolites. This compound is primarily used in clinical settings as an antidote for poisoning due to methanol or ethylene glycol exposure, showcasing its significant biological activity in toxicology research. -
CYP2C19 Inhibitor
(±)-N-3-Benzylnirvanol acts as an inhibitor of the cytochrome P450 enzyme CYP2C19. This racemic mixture, comprised of both (+)-N-3-Benzylnirvanol and (-)-N-3-Benzylnirvanol, exhibits potent inhibitory activity with Ki values of 0.25 μM and 5.3 μM, respectively, for the respective enantiomers. It is valuable in pharmacological research aimed at understanding drug metabolism and potential drug-drug interactions involving CYP2C19. -
CYP2B6 Inhibitor
2-Phenyl-2-(1-piperidinyl)propane is a selective and reversible inhibitor of the human cytochrome P450 enzyme CYP2B6, displaying an IC50 value of 5.1 μM and a Ki of 5.6. In addition to its primary activity, this compound also moderately inhibits CYP2D6 and CYP3A, with IC50 values of 74 μM and 200 μM, respectively. This reagent is pertinent for research into drug metabolism and interactions involving CYP2B6 and other related P450 enzymes. -
CYP1B1 Inhibitor
CYP1B1-IN-4 is a selective CYP1B1 inhibitor, demonstrating a potent inhibitory activity with an IC50 value of 0.2 nM. This compound exhibits low cytotoxicity and maintains high stability in both human and rat liver microsomes, making it suitable for pharmacological studies. Its selectivity and stability position CYP1B1-IN-4 as a valuable tool for research into CYP1B1-related biological pathways and diseases. -
CYP4A11/CYP4F2 Inhibitor
TP0472993 is a potent and orally active dual inhibitor of cytochrome P450 enzymes CYP4A11 and CYP4F2, exhibiting IC50 values of 140 nM and 40 nM, respectively. This compound is valuable for investigating the role of these enzymes in renal diseases, contributing to a deeper understanding of their biological functions and potential therapeutic implications. Its selective inhibition profile makes TP0472993 a useful tool for studying the pharmacological effects related to cytochrome P450-mediated pathways. -
CYP2D6 Inhibitor
ONT-993 is a hydroxylated metabolite that primarily inhibits the cytochrome P450 enzyme CYP2D6, with an IC50 value of 7.9 µM. Additionally, ONT-993 induces metabolism-dependent inactivation of CYP3A, characterized by a KI of 1.6 µM. This compound is useful in research applications focused on drug metabolism and pharmacokinetics, particularly regarding interactions involving CYP450 enzymes.
