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human liver microsomal

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) CD38 (1) COX (1) Cytochrome P450 (2) Dengue Virus (1) DNA/RNA Synthesis (1) Dopamine Receptor (1) Drug Derivative (1) Drug Metabolite (1) Ferroptosis (1) HBV (1) HCV (1) HCV Protease (1) Insecticide (1) Lipoxygenase (1) Methylenetetrahydrofolate Dehydrogenase (MTHFD) (1) Parasite (1) Ras (1)
By Research Areas:	Cancer (2) Cardiovascular Disease (2) Infection (5) Inflammation/Immunology (3) Metabolic Disease (1) Neurological Disease (1)

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Targets Recommended: LXR Microsomal Triglyceride Transfer Protein (MTP)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-150508

MK-0159 1 Publications Verification	CD38	Cardiovascular Disease Metabolic Disease Inflammation/Immunology
MK-0159 is an orally active, potent and selective CD38 inhibitor, with IC₅₀ values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD ⁺ (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart .

HY-N5132

(-)-Fenchone	Cytochrome P450	Others
(-)-Fenchone is a bicyclic monoterpene and serves as a substrate for human liver microsomal cytochrome P450 enzymes CYP2A6 and CYP2B6. (-)-Fenchone is not metabolized by human CYP1A1, CYP1A2, CYP1B1, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4 enzymes. (-)-Fenchone undergoes hydroxylation to produce 6-exo-hydroxyfenchone, 6-endo-hydroxyfenchone, and 10-hydroxyfenchone. During the metabolism of (-)-Fenchone, CYP2A6 may play a more important role than CYP2B6 .

HY-W089800

trans-2-Nonenal trans-2-Nonen-1-al	COX Lipoxygenase Apoptosis	Cardiovascular Disease Inflammation/Immunology
trans-2-Nonenal (trans-2-Nonen-1-al) is an endogenous peroxidation product of polyunsaturated fatty acids, acting as an inhibitor of COX and 12-LOX, as well as an inducer of apoptosis. trans-2-Nonenal is also a malodorous compound secreted by the human body, and its content gradually increases with aging. trans-2-Nonenal inhibits the activities of multiple enzymes such as platelet membrane-bound PTPase, preferentially covalently modifies proteins at lysine residues to form immunogenic adducts, and regulates platelet Arachidonic acid (HY-109590) metabolism. trans-2-Nonenal also exhibits significant cytotoxicity, reduces the viability of keratinocytes, promotes their apoptosis, and effectively decreases the thickness of epidermal models and the number of proliferating cells. trans-2-Nonenal is commonly used in studies of thrombotic, atherosclerotic diseases, renal adenocarcinoma, etc. .

HY-117580

16α-Hydroxyprednisolone OH-PRED	Drug Metabolite	Inflammation/Immunology
16α-Hydroxyprednisolone (OH-PRED) is a stereoselective metabolite of the 22(R) epimer of the glucocorticoid Budesonide (HY-13580). 16α-Hydroxyprednisolone formation is catalyzed by isoenzymes within the cytochrome P450 3A (CYP3A) subfamily. 16α-Hydroxyprednisolone formation can be inhibited by antibodies targeting the CYP3A subfamily .

HY-W424918

Opromazine hydrochloride	Dopamine Receptor	Neurological Disease
Opromazine hydrochloride is an antipsychotic medication that exhibits sedative and antiemetic pharmacological effects, making it effective for treating psychiatric disorders such as schizophrenia and psychosis. Opromazine hydrochloride functions by reducing dopaminergic activity through the blockade of dopamine receptors in the brain. Opromazine hydrochloride has been analyzed for its metabolites in various microsomal enzymes, revealing differences in formation rates that underscore the variability of drug-metabolizing enzymes in human liver and placenta microsomes.

HY-W331198

Tralopyril	Insecticide Ferroptosis	Infection
Tralopyril is an orally active, blood-brain barrier-penetrating antifouling insecticide and endocrine disruptor. By interfering with the thyroid hormone system and mitochondrial oxidative phosphorylation, Tralopyril downregulates the transcription of genes such as TRHR, Nkx2.1, TRα and induces ferroptosis. Tralopyril disrupts amino acid, energy and lipid metabolism, exhibits significant skeletal and reproductive toxicity, and causes developmental damage. Tralopyril has a long half-life in vivo and wide tissue distribution, posing potential risks to aquatic organisms and human health. Tralopyril shows species specificity in in vitro liver microsomal metabolism, exerts lethal effects on target insects and laboratory animals, and is commonly used in studies of chlorfenapyr poisoning and related toxic mechanisms .

HY-W413619

Cipargamin enantiomer NITD609 enantiomer; KAE609 enantiomer	Parasite	Infection
Cipargamin enantiomer (NITD609 enantiomer) is a Plasmodium falciparum inhibitor that can be characterized as a spirotetrahydro β-carboline (1S,3R stereoisomer). Cipargamin enantiomer exerts antiplasmodial activity against Plasmodium falciparum strains NF54 (IC₅₀ of 77 nM) and K1. Cipargamin enantiomer displays low liver microsomal intrinsic clearance in mouse and human systems. Cipargamin enantiomer does not inhibit CYP2C9. Cipargamin enantiomer can be used for the research of malaria .

HY-182042

DENV-IN-15	Dengue Virus	Infection
DENV-IN-15 is a sulfonyl anthranilic acid derivative and a pan-serotype anti-dengue virus (DENV) inhibitor with broad-spectrum anti-RNA virus activity. The EC₅₀ value of DENV-IN-15 against DENV-2 in Huh-7 cells is 0.7 μM. DENV-IN-15 selectively regulates the translation of mRNAs encoding translation-related proteins and containing a 5'-oligopyrimidine tract. DENV-IN-15 reduces the expression of specific ribosomal proteins, thereby inhibiting viral replication. DENV-IN-15 exhibits enhanced membrane permeability, human plasma stability and human liver microsomal metabolic stability. DENV-IN-15 is applicable to research related to dengue virus infection .

HY-115516

BI-1388	HCV HCV Protease Ras	Infection
BI-1388 is a macrocyclic acylsulfonamide-based HCV NS3-4A protease inhibitor. BI-1388 inhibits clinically relevant drug-resistant mutant strains (KRAS ^D168V gt 1b and KRAS ^R155K gt 1a) and exhibits high liver distribution. BI-1388 is applicable for the research of HCV infection .

HY-182355

MTHFD2-IN-7	Methylenetetrahydrofolate Dehydrogenase (MTHFD)	Cancer
MTHFD2-IN-7 is an orally active, selective MTHFD2 inhibitor with IC₅₀ values of 0.038 μM and 7.44 μM against human hMTHFD1 and hMTHFD2, respectively. MTHFD2-IN-7 exerts its function by binding to the substrate-binding site of MTHFD2 and maintaining interactions with NAD+. Verified by TSA and DARTS assays, MTHFD2-IN-7 not only binds effectively to the target protein, but also possesses Caco-2 permeability and liver microsomal metabolic stability. MTHFD2-IN-7 exhibits favorable pharmacokinetic properties in mice. MTHFD2-IN-7 also significantly inhibits cancer cell proliferation and reduces tumor volume, and serves as a promising small-molecule tool for acute myeloid leukemia research .

HY-N17448

Fraxinuacidoside	Drug Derivative	Others
Fraxinuacidoside functions as a norditerpene glucopyranoside with a unique carbon skeleton. Fraxinuacidoside can be found in the stem bark of Fraxinus sieboldiana .

HY-183260

HBV-IN-57	HBV Cytochrome P450	Infection
HBV-IN-57 is an orally active HBV inhibitor with pan-genotypic efficacy against HBV genotypes B/C. HBV-IN-57 inhibits HBV DNA replication and HBV capsid assembly. HBV-IN-57 can be used for the research of chronic hepatitis B .

HY-123599

IACS-4619	DNA/RNA Synthesis	Cancer
IACS-4619 (compound 4) is a highly selective 2-aminopyrimidine-based MTH1 (MutT homolog 1) inhibitor (IC₅₀=0.2 nM). IACS-4619 inhibits MTH1 by blocking its hydrolysis of oxidized purine nucleotides such as 8-oxo-dGTP, thereby preventing MTH1 from inhibiting the incorporation of oxidized nucleotides into DNA. IACS-4619 significantly inhibits endogenous MTH1 activity in MTH1-overexpressing U2OS cells, but without antiproliferative or cytotoxic effects on various human cancer and normal cell lines. IACS-4619 can be used in oncology research related to the MTH1 target .

Cat. No.	Product Name	Type

HY-W089800

trans-2-Nonenal trans-2-Nonen-1-al	Biochemical Assay Reagents
trans-2-Nonenal (trans-2-Nonen-1-al) is an endogenous peroxidation product of polyunsaturated fatty acids, acting as an inhibitor of COX and 12-LOX, as well as an inducer of apoptosis. trans-2-Nonenal is also a malodorous compound secreted by the human body, and its content gradually increases with aging. trans-2-Nonenal inhibits the activities of multiple enzymes such as platelet membrane-bound PTPase, preferentially covalently modifies proteins at lysine residues to form immunogenic adducts, and regulates platelet Arachidonic acid (HY-109590) metabolism. trans-2-Nonenal also exhibits significant cytotoxicity, reduces the viability of keratinocytes, promotes their apoptosis, and effectively decreases the thickness of epidermal models and the number of proliferating cells. trans-2-Nonenal is commonly used in studies of thrombotic, atherosclerotic diseases, renal adenocarcinoma, etc. .

trans-2-Nonenal

trans-2-Nonen-1-al

Biochemical Assay Reagents

trans-2-Nonenal (trans-2-Nonen-1-al) is an endogenous peroxidation product of polyunsaturated fatty acids, acting as an inhibitor of COX and 12-LOX, as well as an inducer of apoptosis. trans-2-Nonenal is also a malodorous compound secreted by the human body, and its content gradually increases with aging. trans-2-Nonenal inhibits the activities of multiple enzymes such as platelet membrane-bound PTPase, preferentially covalently modifies proteins at lysine residues to form immunogenic adducts, and regulates platelet Arachidonic acid (HY-109590) metabolism. trans-2-Nonenal also exhibits significant cytotoxicity, reduces the viability of keratinocytes, promotes their apoptosis, and effectively decreases the thickness of epidermal models and the number of proliferating cells. trans-2-Nonenal is commonly used in studies of thrombotic, atherosclerotic diseases, renal adenocarcinoma, etc. .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N5132

(-)-Fenchone	Structural Classification Other Monoterpenes Classification of Application Fields Terpenoids Other Diseases Umbelliferae Plants Vernonia Schreb. Disease Research Fields Source Classification	Cytochrome P450
(-)-Fenchone is a bicyclic monoterpene and serves as a substrate for human liver microsomal cytochrome P450 enzymes CYP2A6 and CYP2B6. (-)-Fenchone is not metabolized by human CYP1A1, CYP1A2, CYP1B1, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4 enzymes. (-)-Fenchone undergoes hydroxylation to produce 6-exo-hydroxyfenchone, 6-endo-hydroxyfenchone, and 10-hydroxyfenchone. During the metabolism of (-)-Fenchone, CYP2A6 may play a more important role than CYP2B6 .

HY-W089800

trans-2-Nonenal trans-2-Nonen-1-al	Source Classification	COX Lipoxygenase Apoptosis
trans-2-Nonenal (trans-2-Nonen-1-al) is an endogenous peroxidation product of polyunsaturated fatty acids, acting as an inhibitor of COX and 12-LOX, as well as an inducer of apoptosis. trans-2-Nonenal is also a malodorous compound secreted by the human body, and its content gradually increases with aging. trans-2-Nonenal inhibits the activities of multiple enzymes such as platelet membrane-bound PTPase, preferentially covalently modifies proteins at lysine residues to form immunogenic adducts, and regulates platelet Arachidonic acid (HY-109590) metabolism. trans-2-Nonenal also exhibits significant cytotoxicity, reduces the viability of keratinocytes, promotes their apoptosis, and effectively decreases the thickness of epidermal models and the number of proliferating cells. trans-2-Nonenal is commonly used in studies of thrombotic, atherosclerotic diseases, renal adenocarcinoma, etc. .

HY-N17448

Fraxinuacidoside	Structural Classification Fraxinus sieboldiana Blume Oleaceae Plants Saccharides Monosaccharides Source Classification	Drug Derivative
Fraxinuacidoside functions as a norditerpene glucopyranoside with a unique carbon skeleton. Fraxinuacidoside can be found in the stem bark of Fraxinus sieboldiana .

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human liver microsomal

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