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Results for "

Rapid metabolism

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adrenergic Receptor (2) Antibiotic (2) Antifolate (1) Bacterial (2) Biochemical Assay Reagents (1) Cholinesterase (ChE) (1) Cytochrome P450 (1) Dihydrofolate reductase (DHFR) (1) Drug Metabolite (1) Endogenous Metabolite (1) FAAH (1) G protein-coupled Bile Acid Receptor 1 (1) Glucocorticoid Receptor (1) KMO (1) Parasite (1) Raf (2) Reactive Oxygen Species (2)
By Research Areas:	Cancer (4) Cardiovascular Disease (1) Infection (3) Inflammation/Immunology (4) Metabolic Disease (2) Neurological Disease (2)

Inhibitors & Agonists

Screening Libraries

Targets Recommended: Mitochondrial Metabolism

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12853

Mesotrione	Reactive Oxygen Species	Others
Mesotrione is a herbicide belongs to the benzoylcyclohexanedione family. Mesotrione is a potent and competitive and reversible inhibitor of HPPD enzyme. Mesotrione is selective to maize due to rapid metabolism and relative high tolerance by the susceptible crop plant .

HY-112179

GSK180 1 Publications Verification	KMO	Inflammation/Immunology
GSK180 is a selective, competitive, and potent inhibitor of kynurenine-3-monooxygenase (KMO), a key enzyme of tryptophan metabolism (IC₅₀, ~6 nM), but shows negligible activity against other enzymes on the tryptophan pathway. GSK180 rapidly changes levels of kynurenine pathway metabolites, and acts as a useful tool to probe the therapeutic potential of KMO inhibition .

HY-14795

Mimopezil ZT-1	Cholinesterase (ChE)	Neurological Disease
Mimopezil (ZT-1) is an cholinesterase (ChE) inhibitor that rapidly degrades into the active metabolite Huperzine A (HY-17388) in water or aqueous organic solvents. After oral administration, Mimopezil is rapidly absorbed but has low bioavailability (0.37%) in rats. However, after metabolism, it is converted into Huperzine A, which accumulates in the blood and exhibits strong activity. Following intravenous administration, Mimopezil reaches higher blood concentrations and is also rapidly metabolized into Huperzine A .

HY-107010A

Esprolol hydrochloride	Adrenergic Receptor	Cardiovascular Disease
Esprolol hydrochloride is an orally active and potent β-adrenergic receptor antagonist. Esprolol hydrochloride undergoes rapid metabolism by blood and tissue esterases to form an active metabolite, amoxolol. Esprolol hydrochloride is promising for research of exertional angina .

HY-142820

B-Raf IN 5	Raf	Cancer
B-Raf IN 5 (compound 3b) is a potent inhibitor of protein kinase B-Raf with an IC₅₀ of 2.0 nM. B-Raf IN 5 is devoid of binding to the secondary target PXR and resists rapid metabolism. B-Raf IN 6 has the potential for the research of cancer disease .

HY-12853R

Mesotrione (Standard)	Reactive Oxygen Species	Others
Mesotrione (Standard) is the analytical standard of Mesotrione. This product is intended for research and analytical applications. Mesotrione is a herbicide belongs to the benzoylcyclohexanedione family. Mesotrione is a potent and competitive and reversible inhibitor of HPPD enzyme. Mesotrione is selective to maize due to rapid metabolism and relative high tolerance by the susceptible crop plant .

HY-142830

B-Raf IN 6	Raf	Cancer
B-Raf IN 6 (compound 2c) is a potent inhibitor of protein kinase B-Raf with an IC₅₀ of 1.7 nM. B-Raf IN 6 is devoid of binding to the secondary target PXR and resists rapid metabolism. B-Raf IN 6 has the potential for the research of cancer disease .

HY-146453

TGR5 Receptor Agonist 3	G protein-coupled Bile Acid Receptor 1	Metabolic Disease
TGR5 Receptor Agonist 3 (Compound 19) is a soft-agent G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist with reduced gallbladder-filling effects (favorable gallbladder safety), with EC50s of 16.4 and 209 nM for hTGR5 and mTGR5, respectively.

HY-124950

Picumeterol GR114297A	Adrenergic Receptor	Others
Picumeterol (GR114297A) is a potent and selective β₂-adrenoceptor agonist with bronchodilator and anti-bronchoconstrictor effects. Picumeterol produces long-lasting relaxation of airways smooth muscle both in vitro and in vivo. Picumeterol is cleared from plasma through a rapid and extensive hepatic metabolism. Picumeterol is proming for rasearch of asthma and related diseases .

HY-163672

Glucocorticoid receptor modulator 3	Glucocorticoid Receptor	Metabolic Disease Inflammation/Immunology
Glucocorticoid receptor modulator 3 (Payload 6) is a thioester-containing glucocorticoid receptor modulator (IC₅₀=0.6 nM). Glucocorticoid receptor modulator 3 is designed to inactivate unconjugated payloads rapidly through liver metabolism, thereby minimizing systemic exposure. Glucocorticoid receptor modulator 3 can be utilized in the development of antibody-drug conjugates (ADCs) targeting autoimmune diseases .

HY-W040235

Fluazuron	Endogenous Metabolite	Others
Fluazuron is an insect growth regulator with activity against larvae of Amblyomma sculptum. Fluazuron exhibits 100% efficacy by interfering with the molting process. Fluazuron has shown rapid absorption and slow metabolism in experiments. The use of Fluazuron offers a potential preventive measure for the control of Brazilian spotted fever. The results of Fluazuron offer good prospects for the development of feed products containing FLU to control ticks in free-living capybaras .

HY-112621

Leukotriene A4 methyl ester LTA4 methyl ester	Biochemical Assay Reagents	Inflammation/Immunology
Leukotriene A4 methyl ester (LTA4 methyl ester) is synthesized in mast cells, eosinophils, and neutrophils from arachidonic acid by 5-lipoxygenase (5-LO), which exhibits both lipoxygenase and LTA4 synthase activities. LTA4 is rapidly metabolized by LTA4 hydrolase or LTC4 synthase to LTB4 or LTC4, respectively. LTA4, from leukocytes, is known to undergo transcellular metabolism in platelets, erythrocytes, and endothelial cells. Further metabolism of LTA4 by 15-LO leads to lipoxin biosynthesis. LTA4 as a free acid is highly unstable. The methyl ester is stable and can be readily hydrolyzed to the free acid as needed.

HY-W013699

Chlorhexidine diacetate Maximum Cited Publications 11 Publications Verification	Bacterial Antibiotic	Infection Cancer
Chlorhexidine diacetate is a cationic antimicrobial agent that targets microbial cell membranes. It binds to cell membrane phospholipids non-specifically, destroys membrane structure and induces leakage of cell contents. It has broad-spectrum bactericidal activity against both Gram-positive and Gram-negative bacteria. Chlorhexidine diacetate can interfere with membrane permeability, cause protein precipitation and energy metabolism disorders, such as rapid inhibition of microbial growth and induction of cell death (necrosis or apoptosis) .

HY-W267897

7-Benzyloxy-4-(trifluoromethyl)coumarin 7-BFC	Cytochrome P450	Others
7-Benzyloxy-4-(trifluoromethyl)coumarin (7-BFC) is a coumarin fluorescent substrate. 7-Benzyloxy-4-(trifluoromethyl)coumarin is a substrate for cDNA-expressed CYP1A2 and CYP3A4 and is metabolized to 7-hydroxy-4-trifluoromethylcoumarin (HFC). 7-Benzyloxy-4-(trifluoromethyl)coumarin is used for rapid CYP isoform metabolism and inhibition screening studies .

HY-B1248

Chlorhexidine Maximum Cited Publications 11 Publications Verification	Bacterial Antibiotic	Infection Cancer
Chlorhexidine is a cationic antimicrobial agent that targets microbial cell membranes. It binds to cell membrane phospholipids non-specifically, destroys membrane structure and induces leakage of cell contents. It has broad-spectrum bactericidal activity against both Gram-positive and Gram-negative bacteria. Chlorhexidine can interfere with membrane permeability, cause protein precipitation and energy metabolism disorders, such as rapid inhibition of microbial growth and induction of cell death (necrosis or apoptosis) .

HY-108251

Methotrexate metabolite 1 Publications Verification DAMPA	Antifolate Drug Metabolite Dihydrofolate reductase (DHFR) Parasite	Infection Inflammation/Immunology
Methotrexate metabolite (DAMPA) is an active metabolite of Methotrexate. Methotrexate is a Folic acid (HY-16637) antagonist, widely used as an immunosuppressant. Methotrexate metabolite is an antimalarial agent that inhibits parasite growth under physiological folic acid conditions, with IC₅₀ values of 446 nM and 812 nM against folic acid-sensitive strains and highly resistant strains, respectively. Methotrexate metabolite exhibits pharmacokinetic characteristics of rapid clearance and extensive metabolism, with a mean clearance rate of 1.9 l/kg/h and a mean terminal half-life of 51 minutes. Methotrexate metabolite is promising for research in the field of inflammation .

HY-115004

MM-433593	FAAH	Neurological Disease
MM-433593 is a potent and selective inhibitor of fatty acid amide hydrolase-1 (FAAH-1) that is orally administered to inhibit pain, inflammation, and related disorders. Pharmacokinetic studies of MM-433593 in macaques revealed a biphasic elimination profile with a rapid distribution phase and a slower elimination phase, with a systemic clearance of 8-11 mL/min/kg. MM-433593 exhibits moderate oral bioavailability (14-21%) and its metabolism primarily involves oxidation of the methyl group on the indole ring, resulting in a variety of sulfate, glucuronide, or glutathione-conjugated metabolites .

Cat. No.	Product Name

HY-L146

Metabolic Enzyme Compound Library	3,611 compounds
Metabolism is the set of life-sustaining chemical reactions in organisms that maintain cell homeostasis. Metabolic pathways are enzyme-mediated biochemical reactions that lead to biosynthesis (anabolism) or breakdown (catabolism) of molecules including glucose metabolism, lipid metabolism and amino acid or protein metabolism within a cell or tissue. As catalysts, enzymes are crucial to metabolism as they allow a reaction to proceed more rapidly and tregulate the rate of a metabolic reaction. Due to the importance of metabolic balance in the organism, the abnormal function of metabolic enzymes often leads to the occurrence of a variety of metabolic diseases, such as diabetes, obesity, cardiovascular disease, etc. MCE designs a unique collection of 3,611 metabolic enzymes related small molecules, which is an important tool for studying the metabolic activities of organisms and developing drugs for metabolic diseases.

Metabolic Enzyme Compound Library

3,611 compounds

Metabolism is the set of life-sustaining chemical reactions in organisms that maintain cell homeostasis. Metabolic pathways are enzyme-mediated biochemical reactions that lead to biosynthesis (anabolism) or breakdown (catabolism) of molecules including glucose metabolism, lipid metabolism and amino acid or protein metabolism within a cell or tissue. As catalysts, enzymes are crucial to metabolism as they allow a reaction to proceed more rapidly and tregulate the rate of a metabolic reaction. Due to the importance of metabolic balance in the organism, the abnormal function of metabolic enzymes often leads to the occurrence of a variety of metabolic diseases, such as diabetes, obesity, cardiovascular disease, etc.

MCE designs a unique collection of 3,611 metabolic enzymes related small molecules, which is an important tool for studying the metabolic activities of organisms and developing drugs for metabolic diseases.

HY-L012

Metabolism/Protease Compound Library	5,712 compounds
Metabolism is the set of life-sustaining chemical reactions in organisms. Metabolic pathways are enzyme-mediated biochemical reactions that lead to biosynthesis (anabolism) or breakdown (catabolism) of natural product small molecules within a cell or tissue. Acting as catalysts, enzymes are crucial to metabolism - they allow a reaction to proceed more rapidly - and they also allow the regulation of the rate of a metabolic reaction. Proteases are used throughout an organism for various metabolic processes. Proteases control a great variety of physiological processes that are critical for life, including the immune response, cell cycle, cell death, wound healing, food digestion, and protein and organelle recycling. Imbalances in metabolic activities have been found to be critical in a number of pathologies, such as cardiovascular diseases, inflammation, cancer, and neurodegenerative diseases. MCE designs a unique collection of 5,712 Metabolism/Protease-related small molecules that act as a useful tool for drug discovery of metabolism-related diseases.

Metabolism/Protease Compound Library

5,712 compounds

Metabolism is the set of life-sustaining chemical reactions in organisms. Metabolic pathways are enzyme-mediated biochemical reactions that lead to biosynthesis (anabolism) or breakdown (catabolism) of natural product small molecules within a cell or tissue. Acting as catalysts, enzymes are crucial to metabolism - they allow a reaction to proceed more rapidly - and they also allow the regulation of the rate of a metabolic reaction. Proteases are used throughout an organism for various metabolic processes. Proteases control a great variety of physiological processes that are critical for life, including the immune response, cell cycle, cell death, wound healing, food digestion, and protein and organelle recycling. Imbalances in metabolic activities have been found to be critical in a number of pathologies, such as cardiovascular diseases, inflammation, cancer, and neurodegenerative diseases.

MCE designs a unique collection of 5,712 Metabolism/Protease-related small molecules that act as a useful tool for drug discovery of metabolism-related diseases.

HY-L064

Glutamine Metabolism Compound Library	1,197 compounds
Glutamine is an important metabolic fuel that helps rapidly proliferating cells meet the increased demand for ATP, biosynthetic precursors, and reducing agents. Glutamine Metabolism pathway involves the initial deamination of glutamine by glutaminase(GLS), yielding glutamate and ammonia. Glutamate is converted to the TCA cycle intermediate α-ketoglutarate (α-KG) by either glutamate dehydrogenase (GDH) or by the alanine or aspartate transaminases (TAs), to produce both ATP and anabolic carbons for the synthesis of amino acids, nucleotides and lipids. During periods of hypoxia or mitochondrial dysfunction, α-KG can be converted to citrate in a reductive carboxylation reaction catalyzed by IDH2. The newly formed citrate exits the mitochondria where it is used to synthesize fatty acids and amino acids and produce the reducing agent, NADPH. Cancer cells display an altered metabolic circuitry that is directly regulated by oncogenic mutations and loss of tumor suppressors. Mounting evidence indicates that altered glutamine metabolism in cancer cells has critical roles in supporting macromolecule biosynthesis, regulating signaling pathways, and maintaining redox homeostasis, all of which contribute to cancer cell proliferation and survival. Thus, intervention in glutamine metabolic processes could provide novel approaches to improve cancer treatment. MCE owns a unique collection of 1,197 compounds targeting the mainly proteins and enzymes involved in glutamine metabolism pathway. Glutamine Metabolism compound library is a useful tool for intervention in glutamine metabolic processes.

Glutamine Metabolism Compound Library

1,197 compounds

Glutamine is an important metabolic fuel that helps rapidly proliferating cells meet the increased demand for ATP, biosynthetic precursors, and reducing agents. Glutamine Metabolism pathway involves the initial deamination of glutamine by glutaminase(GLS), yielding glutamate and ammonia. Glutamate is converted to the TCA cycle intermediate α-ketoglutarate (α-KG) by either glutamate dehydrogenase (GDH) or by the alanine or aspartate transaminases (TAs), to produce both ATP and anabolic carbons for the synthesis of amino acids, nucleotides and lipids. During periods of hypoxia or mitochondrial dysfunction, α-KG can be converted to citrate in a reductive carboxylation reaction catalyzed by IDH2. The newly formed citrate exits the mitochondria where it is used to synthesize fatty acids and amino acids and produce the reducing agent, NADPH.

Cancer cells display an altered metabolic circuitry that is directly regulated by oncogenic mutations and loss of tumor suppressors. Mounting evidence indicates that altered glutamine metabolism in cancer cells has critical roles in supporting macromolecule biosynthesis, regulating signaling pathways, and maintaining redox homeostasis, all of which contribute to cancer cell proliferation and survival. Thus, intervention in glutamine metabolic processes could provide novel approaches to improve cancer treatment.

MCE owns a unique collection of 1,197 compounds targeting the mainly proteins and enzymes involved in glutamine metabolism pathway. Glutamine Metabolism compound library is a useful tool for intervention in glutamine metabolic processes.

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