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Results for "

human CYP3A4

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (5) ADC Payload (1) Apoptosis (6) Aryl Hydrocarbon Receptor (1) Autophagy (8) Bacterial (1) Calcium Channel (2) Constitutive Androstane Receptor (2) Cytochrome P450 (42) Dopamine Receptor (3) Drug Isomer (1) Drug Metabolite (4) Endogenous Metabolite (1) Environmental Pollutants (2) Ephrin Receptor (1) Fungal (1) G protein-coupled Bile Acid Receptor 1 (1) GABA Receptor (2) HBV (1) iGluR (1) Indoleamine 2,3-Dioxygenase (IDO) (1) Interleukin Related (1) Isotope-Labeled Compounds (7) MDM-2/p53 (1) Microtubule/Tubulin (1) mTOR (1) NAMPT (2) Neurokinin Receptor (1) NF-κB (1) NTPDase (6) Opioid Receptor (1) P-glycoprotein (3) P2X Receptor (1) Parasite (2) PDGFR (1) PI3K (1) PPAR (6) Pregnane X Receptor (PXR) (3) PROTACs (1) Reference Standards (6) Renin (1) SARS-CoV (2) Sirtuin (1) Small Interfering RNA (siRNA) (1) Sodium Channel (2) Urotensin Receptor (1) VEGFR (1)
By Research Areas:	Cancer (19) Cardiovascular Disease (20) Endocrinology (1) Infection (5) Inflammation/Immunology (8) Metabolic Disease (13) Neurological Disease (11)
Oligonucleotides:	Human Pre-designed siRNA Sets (1) siRNAs (1)

Inhibitors & Agonists

Fluorescent Dyes

Biochemical Assay Reagents

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

Oligonucleotides

GMP Molecules

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-17356

Fenofibrate Maximum Cited Publications 33 Publications Verification	PPAR Cytochrome P450 Autophagy	Cardiovascular Disease Cancer
Fenofibrate is a selective PPARα agonist with an EC₅₀ of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC₅₀s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and *CYP3A4*, respectively.

HY-N6972

Cepharanthine Maximum Cited Publications 13 Publications Verification	Autophagy SARS-CoV Cytochrome P450 Apoptosis Parasite	Infection Inflammation/Immunology Cancer
Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC₅₀) and 90% inhibitory concentration (IC₉₀) values of 1.90 and 4.46 μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .

HY-100386

Ticlopidine 3 Publications Verification PCR 5332	NTPDase Cytochrome P450	Cardiovascular Disease
Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively.

HY-109171

Elinzanetant NT-814; BAY3427080	Neurokinin Receptor	Cardiovascular Disease Neurological Disease
Elinzanetant is an orally active and selective NK-1 and NK-3 receptor antagonist. Elinzanetant alleviates menopause-associated vasomotor symptoms, including hot flashes and night sweats. Elinzanetant reduces estradiol and progesterone levels. Elinzanetant can be used for the research of moderate to severe vasomotor and sleep disorders associated with menopause .

HY-B0153A

Ticlopidine hydrochloride 3 Publications Verification	NTPDase Cytochrome P450	Cardiovascular Disease Neurological Disease Cancer
Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively .

HY-B0822

Fipronil	Environmental Pollutants Cytochrome P450 GABA Receptor Apoptosis	Neurological Disease
Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC₅₀s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes .

HY-157421

Nampt activator-4	NAMPT	Metabolic Disease
Nampt activator-4 is an orally active NAMPT activator, with an EC₅₀ of 58 nM and a K_a of 85.38 nM against human NAMPT. Nampt activator-4 effectively relieves the feedback inhibition of nicotinamide and NAD ⁺, thereby enhancing enzymatic activity and significantly increasing intracellular NAD ⁺ levels. Nampt activator-4 exhibits moderate stability in human and mouse liver microsomes. Nampt activator-4 shows low to moderate inhibitory effects on cytochrome P450 (especially CYP3A4). Nampt activator-4 can be used for the research of type 2 diabetes and related metabolic disorders .

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-19958

XEN907	Sodium Channel	Neurological Disease
XEN907 is a potent and spirooxindole blocker of Na_V1.7, with an IC₅₀ of 3 nM. XEN907 also inhibits *CYP3A4* in a recombinant human enzyme assay. XEN907 can be used for the research of pain .

HY-113482

1β-Hydroxydeoxycholic acid 1β-OH-DCA	Endogenous Metabolite Cytochrome P450	Metabolic Disease
1β-Hydroxydeoxycholic acid (1β-OH-DCA), a secondary bile acid, is a CYP3A biomarker. Deoxycholic acid is specifically metabolized into 1β-Hydroxydeoxycholic acid by CYP3A4 and CYP3A7 using recombinant human CYP450 enzymes .

HY-G0006

Omeprazole sulfide 2 Publications Verification Ufiprazole	Drug Metabolite Aryl Hydrocarbon Receptor Bacterial	Infection Metabolic Disease
Omeprazole sulfide (Ufiprazole) is a metabolic degradation product of Omeprazole (HY-B0113). Omeprazole sulfide acts as a modulator of AhR. Omeprazole sulfide in cells with low CYP3A4 expression, functions as an AhR antagonist; however, in cells with high CYP3A4 expression, it is rapidly metabolized to Omeprazole, thereby acting as an AhR agonist. Omeprazole sulfide exhibits antibacterial activity when conjugated with silver nanoparticles (AgNPs). Omeprazole sulfide can be used in research on acid suppression and bacterial infections .

HY-128914

Tubulysin	ADC Payload Microtubule/Tubulin Apoptosis	Cancer
Tubulysin is a microtubule destabilizer that binds to the β-tubulin peptide site adjacent to the vinca alkaloid binding site and inhibits tubulin polymerization. Tubulysin induces apoptosis and exhibits antiproliferative activity against a variety of human cancer cells, including multidrug-resistant strains. Tubulysin can be conjugated to antibodies via a disulfide-containing quaternary ammonium linker for ADC synthesis . Tubulysin is applicable to tumor-related research .

HY-10505

Orteronel 2 Publications Verification TAK-700	Cytochrome P450	Cancer
Orteronel (TAK-700) is a highly selective inhibitor of human 17,20-lyase (CYP17) with IC₅₀ of 38 nM, and exhibits >1000-fold selectivity over other CYPs such as 11-hydroxylase and CYP3A4 .

HY-N6066

Praeruptorin E	Calcium Channel NF-κB Pregnane X Receptor (PXR) Cytochrome P450 Interleukin Related	Cardiovascular Disease Inflammation/Immunology
Praeruptorin E is an orally active pyranocoumarin compound. Praeruptorin E can be isolated from the dried roots of Peucedanum praeruptorum Dunn. Praeruptorin E reduces the expression of NF-κB. Praeruptorin E upregulates the expression of PXR and CYP3A4. Praeruptorin E inhibits Th2 cytokines, TNF-α, IL6, MPO, and blocks the Ca ²⁺ slow channel. Praeruptorin E promotes pulmonary tissue repair and relaxes porcine coronary artery strips. Praeruptorin E protects mice from lipopolysaccharide- and hydrochloric acid-induced acute lung injury. Praeruptorin E can be used in studies related to asthma and acute lung injury .

HY-N2411

Geissoschizine methyl ether 1 Publications Verification	5-HT Receptor	Neurological Disease
Geissoschizine methyl ether is an orally active, blood-brain barrier permeable alkaloid, and a partial agonist of the 5-HT₁A receptor. It can be isolated from Uncaria hook. Geissoschizine methyl ether potently inhibits the binding of [ ³H]8-OH-DPAT to the 5-HT₁A receptor in a concentration-dependent manner, with an IC₅₀ of 0.904 μM. It ameliorates isolation-induced increased aggression and reduced sociability in mice. Geissoschizine methyl ether promotes oligodendrocyte differentiation and remyelination in the medial prefrontal cortex of adult mice .

HY-17356S

Fenofibrate-d6	Isotope-Labeled Compounds PPAR Cytochrome P450 Autophagy	Cardiovascular Disease Cancer
Fenofibrate-d₆ is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.

HY-B0822R

Fipronil (Standard)	Reference Standards GABA Receptor Cytochrome P450 Apoptosis	Neurological Disease
Fipronil (Standard) is the analytical standard of Fipronil. This product is intended for research and analytical applications. Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC₅₀s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes .

HY-100386R

Ticlopidine (Standard) PCR 5332 (Standard)	Reference Standards NTPDase Cytochrome P450	Cardiovascular Disease
Ticlopidine (Standard) is the analytical standard of Ticlopidine. This product is intended for research and analytical applications. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively .

HY-111202

Pyributicarb TSH-888	Environmental Pollutants Cytochrome P450	Inflammation/Immunology
Pyributicarb, a carbamate-type herbicide, is a potent activator of both *CYP3A4* gene and human pregnane X receptor (hPXR).

HY-113031

16a-Hydroxydehydroisoandrosterone 16α-Hydroxy-DHEA; 16α-OH-DHEA; 16α-hydroxy DHEA	Cytochrome P450	Endocrinology
16a-Hydroxydehydroisoandrosterone (16α-Hydroxy-DHEA) is a metabolite of the endogenous steroid hormone dehydroepiandrosterone. 16α-hydroxy Dehydroepiandrosterone is formed from dehydroepiandrosterone via 16-hydroxylation by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP3A5 in adult human liver microsomes, as well as by fetal recombinant CYP3A7. It is a precursor to fetal estrogens, including estriol.

HY-17356R

Fenofibrate (Standard) Maximum Cited Publications 33 Publications Verification	Reference Standards PPAR Cytochrome P450 Autophagy	Cardiovascular Disease Cancer
Fenofibrate (Standard) is the analytical standard of Fenofibrate. This product is intended for research and analytical applications. Fenofibrate is a selective PPARα agonist with an EC₅₀ of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC₅₀s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and *CYP3A4*, respectively.

HY-109173

Filapixant BAY 1902607	P2X Receptor Cytochrome P450	Inflammation/Immunology
Filapixant (BAY 1902607) is an orally active and selective P2X3 receptor antagonist. Filapixant is applicable to the research of refractory chronic cough .

HY-N6065

Praeruptorin A 3 Publications Verification (+)-Praeruptorin A	Calcium Channel Drug Isomer Cytochrome P450 iGluR Apoptosis	Cardiovascular Disease Neurological Disease
Praeruptorin A ((+)-Praeruptorin A) is an orally active isomer of (±)-Praeruptorin A (HY-N0081). Praeruptorin A also acts as a Calcium channel blocker. Praeruptorin A can be isolated from Peucedanum. Praeruptorin A serves as a substrate for CYP3A4. Praeruptorin A downregulates NMDA receptors containing GluN2B and inhibits neuronal Apoptosis. Praeruptorin A mediates vasodilation, inhibits vascular hypertrophy and reduces blood pressure. Praeruptorin A can be used in research related to neurological diseases, myocardial ischemia, heart failure, exertional angina, renovascular hypertension and spontaneous hypertension .

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-133152

Brexpiprazole S-oxide DM-3411	5-HT Receptor Dopamine Receptor	Neurological Disease
Brexpiprazole S-oxide (DM-3411) is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT_1A and dopamine receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT_2A receptor antagonist with a K_i of 0.47 nM .

HY-RS03471

CYP3A4 Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
CYP3A4 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP3A4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

CYP3A4 Human Pre-designed siRNA Set A CYP3A4 Human Pre-designed siRNA Set A

HY-175266

MI1013	PROTACs Cytochrome P450 Pregnane X Receptor (PXR)	Metabolic Disease
MI1013 is a PROTAC PXR degrader (DC₅₀ = 89 nM, D_max = 82%). MI1013 degrades PXR in human hepatocellular carcinoma RG cells (HepaRG). MI1013 specifically and safely regulates CYP3A4 promoter activity through PXR degradation. MI1013 affects several key genes involved in sulfate conjugation (e.g., SULT1E1), bile acid synthesis (CYP7A1), gluconeogenesis (PCK1), ketone synthesis (HMGCS20), and hepatocyte proliferation (MKI67). (Pink: PXR ligand 3: HY-175267, Blue: Pomalidomide-propargyl ligand: HY-W410002, Pink + Black: PXR ligand-Linker Conjugate 1: HY-175268) .

HY-133152S

Brexpiprazole S-oxide-d8 DM-3411 d₈	Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor	Neurological Disease
Brexpiprazole S-oxide-d₈ (DM-3411 D₈) is a deuterium labeled Brexpiprazole S-oxide (HY-133152). Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM .

HY-112690A

Pradefovir mesylate 1 Publications Verification Remofovir mesylate	Cytochrome P450	Metabolic Disease
Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a K_m of 60 μM.

HY-W702907

DM-4103	P-glycoprotein	Metabolic Disease
DM-4103 is a major metabolite of Tolvaptan (HY-17000) that is metabolized primarily by the CYP3A4 enzyme in the liver. DM-4103 inhibits the ability of human liver transporters NTCP, BSEP, MRP2, MRP3, MRP4 (IC₅₀ values are 16.3, 4.15, 51.0, 44.6, 4.26 μM, respectively) and bile acid transport in SCHH cells. DM-4103 can be used in the study of autosomal dominant polycystic kidney disease (ADPKD) .

HY-17356G

Fenofibrate	Cytochrome P450 PPAR Autophagy	Cardiovascular Disease
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC₅₀ of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC₅₀s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and *CYP3A4*, respectively.

HY-173033

MI-883	Pregnane X Receptor (PXR) Constitutive Androstane Receptor Cytochrome P450	Metabolic Disease
MI-883 is the orally active agonist for Constitutive Androstane Receptor (CAR, EC₅₀=73 nM) and the antagonist for Pregnane X Receptor (PXR, IC₅₀=0.1 μM). MI-883 stimulates CAR LBD assembly (EC₅₀=0.38 µM) and CAR3 variant activation (EC₅₀=0.074 µM), induces CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. MI-883 inhibits basal PXR activity IC₅₀=2.03 µM) in transiently transfected HepG2 cells, blocks CYP3A4 mRNA expression in HepG2. MI-883 regulates cholesterol metabolism and bile acid excretion, improves hypercholesterolemia in mouse models .

HY-N6972R

Cepharanthine (Standard)	Autophagy Reference Standards SARS-CoV Cytochrome P450 Apoptosis Parasite	Infection Inflammation/Immunology Cancer
Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC₅₀) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .

HY-169217

CYP3A4-IN-4	Cytochrome P450	Cancer
CYP3A4-IN-4 (compound Δ,Λ-3), a Ru(II) Ir(III) Conjugate, is a photoactive inhibitor of the major human drug metabolizing enzyme CYP3A4. CYP3A4-IN-4 containing the [Ru(tpy)(Me2bpy)] photocaging group showed an IC₅₀ of 2.2 μM for inhibition of microsomal CYP3A4 under light conditions (λirr=530 nm, tirr=15 min) .

HY-124364

RO6889678	HBV Cytochrome P450	Infection Metabolic Disease
RO6889678 is a highly potent HBV capsid formation inhibitor with a complex absorption, distribution, metabolism, and excretion (ADME) profile. RO6889678 is a potent inducer of CYP3A4 and coregulated proteins in human hepatocytes. RO6889678 is metabolized by a combination of CYP3A4-mediated oxidation and UDP-glucuronosyltransferase UGT1A3- and UGT1A1-mediated direct glucuronidation .

HY-163324A

2-Me PeER	Cytochrome P450	Others
2-Me PeER is a rhodamine dye-based fluorescent probe that detects CYP3A4 activity. In fluorescence-activated cell sorting (FACS) based on CYP3A4 activity, homogeneous and functional human induced pluripotent stem cell (hiPSC)-derived hepatocytes and intestinal epithelial cells can be obtained with the aid of 2-Me PeER .

HY-112690

Pradefovir	Cytochrome P450	Metabolic Disease
Pradefovir is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a K_m of 60 μM.

HY-137580

N-Desmethyl Eletriptan	Cytochrome P450	Metabolic Disease
N-desmethyl Eletriptan is a metabolite of Eletriptan (HY-A0039). It is formed from eletriptan primarily by the cytochrome P450 (CYP) isoform CYP3A4 in human liver microsomes.

HY-N8094

Kushenol M	Cytochrome P450	Others
Kushenol M is a flavonoid from Sophora flavescens. Kushenol M is a cytochrome P450 (CYP) inhibitor, with IC₅₀ values of 1.29 μM for CYP3A4 in human liver microsomes .

HY-134522

DL5050	Constitutive Androstane Receptor	Metabolic Disease Cancer
DL5050 is a selective and potent human constitutive androstane receptor (hCAR) agonist that does not activate pregnane X receptor (PXR). DL5050 preferentially induces the expression of CYP2B6 (target of hCAR) over CYP3A4 (target of hPXR) on both the mRNA and protein levels. DL5050 can be used for the researches of cancer and metabolic disease, such as diabetes .

HY-135390

Hydroxy desmethyl Bosentan Ro 64-1056	Drug Metabolite	Cardiovascular Disease
Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver . Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ET_A and ET_B receptors with K_i of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial hypertension .

HY-W702908

DM-4107	P-glycoprotein	Metabolic Disease
DM-4107 is a major metabolite of Tolvaptan (HY-17000) that is metabolized primarily by the CYP3A4 enzyme in the liver. DM-4107 inhibits the ability of human liver transporters NTCP, BSEP, MRP3, MRP4 (IC₅₀ values are 95.6, 119, 61.2, 37.9 μM, respectively) and bile acid transport in SCHH cells. DM-4107 can be used in the study of autosomal dominant polycystic kidney disease (ADPKD) .

HY-155141

hCYP3A4-IN-1	Cytochrome P450	Cancer
hCYP3A4-IN-1 (compound C6) is a potent, orally active hCYP3A4 inhibitor. hCYP3A4-IN-1 shows the IC₅₀ values of 43.93 nM and 153.00 nM against hCYP3A4 in human liver microsomes (HLMs) and CHO-3A4 stably transfected cell line, respectively. hCYP3A4-IN-1 potently inhibits CYP3A4-catalyzed N-ethyl-1,8-naphthalimide (NEN) hydroxylation in a competitive manner (Ki = 30.00 nM) .

HY-17356S2

Fenofibrate-13C6	Isotope-Labeled Compounds Cytochrome P450 PPAR Autophagy	Cardiovascular Disease
Fenofibrate-13C6 is a deuterated labeled Fenofibrate . Fenofibrate is a selective PPARα agonist with an EC₅₀ of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC₅₀s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and *CYP3A4*, respectively.

HY-17356S1

Fenofibrate-d4	PPAR Autophagy Cytochrome P450	Cardiovascular Disease
Fenofibrate-d₄ is the deuterium labeled Fenofibrate . Fenofibrate is a selective PPARα agonist with an EC₅₀ of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC₅₀s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively .

HY-169119

Antifungal agent 114	Cytochrome P450 Fungal	Infection
Antifungal agent 114 (Compound 19g) is an inhibitor for Cytochrome P450, that inhibits CYP1A2, CYP2C9, CYP2C19 CYP2D6 and CYP3A4 at 10 μM. Antifungal agent 114 exhibits antifungal activity against Cryptococcus neoformans, Candida and Aspergillus, with MIC <0.0625 μg/mL. Antifungal agent 114 exhibits good metabolic stability in human liver microsomes with a half-time of 107 minutes .

HY-100386S

Ticlopidine-d4 PCR 5332-d₄	Isotope-Labeled Compounds NTPDase Cytochrome P450	Cardiovascular Disease
Ticlopidine-d₄ is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively .

HY-B0153AS

Ticlopidine-d4 hydrochloride	Isotope-Labeled Compounds NTPDase Cytochrome P450	Cardiovascular Disease
Ticlopidine-d₄ hydrochloride is the deuterium labeled Ticlopidine hydrochloride (HY-B0153A). Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively .

HY-W707554

Ticlopidine hydrochloride-d6	Isotope-Labeled Compounds Cytochrome P450	Cardiovascular Disease
Ticlopidine hydrochloride-d₆ is the deuterium labeled Ticlopidine hydrochloride (HY-B0153A). Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively .

HY-10672

Urotensin-II receptor antagonist-1	Urotensin Receptor Cytochrome P450 Sodium Channel Opioid Receptor	Cardiovascular Disease
Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, K_i=16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC₅₀=0.75 μM, CYP2D6; 1.4 μM, *CYP3A4), inhibits κ-opioid receptor (EC₅₀*=3.2 μM), targets cardiac sodium channels (K_i=2.5 μM) .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N6972

Cepharanthine Maximum Cited Publications 13 Publications Verification	Infection Alkaloids Stephania cepharantha Hayata Classification of Application Fields Plants Isoquinoline Alkaloids Menispermaceae Inflammation/Immunology Disease Research Fields Stephania japonica (Thunb.) Miers	Autophagy SARS-CoV Cytochrome P450 Apoptosis Parasite
Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC₅₀) and 90% inhibitory concentration (IC₉₀) values of 1.90 and 4.46 μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .

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-113482

1β-Hydroxydeoxycholic acid 1β-OH-DCA	Classification of Application Fields Metabolic Disease Endogenous metabolite Disease Research Fields Steroids Source Classification	Endogenous Metabolite Cytochrome P450
1β-Hydroxydeoxycholic acid (1β-OH-DCA), a secondary bile acid, is a CYP3A biomarker. Deoxycholic acid is specifically metabolized into 1β-Hydroxydeoxycholic acid by CYP3A4 and CYP3A7 using recombinant human CYP450 enzymes .

HY-N6066

Praeruptorin E	Cardiovascular Disease Structural Classification Classification of Application Fields Coumarins Salvia hypargeia Fisch. & C.A.Mey. Phenylpropanoids Umbelliferae Plants Disease Research Fields Source Classification	Calcium Channel NF-κB Pregnane X Receptor (PXR) Cytochrome P450 Interleukin Related
Praeruptorin E is an orally active pyranocoumarin compound. Praeruptorin E can be isolated from the dried roots of Peucedanum praeruptorum Dunn. Praeruptorin E reduces the expression of NF-κB. Praeruptorin E upregulates the expression of PXR and CYP3A4. Praeruptorin E inhibits Th2 cytokines, TNF-α, IL6, MPO, and blocks the Ca ²⁺ slow channel. Praeruptorin E promotes pulmonary tissue repair and relaxes porcine coronary artery strips. Praeruptorin E protects mice from lipopolysaccharide- and hydrochloric acid-induced acute lung injury. Praeruptorin E can be used in studies related to asthma and acute lung injury .

HY-N2411

Geissoschizine methyl ether 1 Publications Verification	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Alkaloids Structural Classification Rubiaceae Plants Indole Alkaloids Source Classification	5-HT Receptor
Geissoschizine methyl ether is an orally active, blood-brain barrier permeable alkaloid, and a partial agonist of the 5-HT₁A receptor. It can be isolated from Uncaria hook. Geissoschizine methyl ether potently inhibits the binding of [ ³H]8-OH-DPAT to the 5-HT₁A receptor in a concentration-dependent manner, with an IC₅₀ of 0.904 μM. It ameliorates isolation-induced increased aggression and reduced sociability in mice. Geissoschizine methyl ether promotes oligodendrocyte differentiation and remyelination in the medial prefrontal cortex of adult mice .

HY-N6065

Praeruptorin A 3 Publications Verification (+)-Praeruptorin A	Structural Classification Classification of Application Fields Coumarins Salvia hypargeia Fisch. & C.A.Mey. Phenylpropanoids Umbelliferae Plants Inflammation/Immunology Disease Research Fields Source Classification	Calcium Channel Drug Isomer Cytochrome P450 iGluR Apoptosis
Praeruptorin A ((+)-Praeruptorin A) is an orally active isomer of (±)-Praeruptorin A (HY-N0081). Praeruptorin A also acts as a Calcium channel blocker. Praeruptorin A can be isolated from Peucedanum. Praeruptorin A serves as a substrate for CYP3A4. Praeruptorin A downregulates NMDA receptors containing GluN2B and inhibits neuronal Apoptosis. Praeruptorin A mediates vasodilation, inhibits vascular hypertrophy and reduces blood pressure. Praeruptorin A can be used in research related to neurological diseases, myocardial ischemia, heart failure, exertional angina, renovascular hypertension and spontaneous hypertension .

HY-N6972R

Cepharanthine (Standard)	Structural Classification Alkaloids Stephania cepharantha Hayata Plants Isoquinoline Alkaloids Menispermaceae Stephania japonica (Thunb.) Miers	Autophagy Reference Standards SARS-CoV Cytochrome P450 Apoptosis Parasite
Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC₅₀) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .

HY-N8094

Kushenol M	Flavanonols Flavonoids Classification of Application Fields Leguminosae Other Diseases Phenols Polyphenols Plants Sophora flavescens Aiton Disease Research Fields Source Classification	Cytochrome P450
Kushenol M is a flavonoid from Sophora flavescens. Kushenol M is a cytochrome P450 (CYP) inhibitor, with IC₅₀ values of 1.29 μM for CYP3A4 in human liver microsomes .

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HY-P74210

	CYP3A4 Protein, Human (His) 1 Publications Verification Cytochrome P450 3A4; CYPIIIA3; CYP3A4; CYP3A3	Human	E. coli
	The CYP3A4 protein, encoded by the CYP3A4 gene, is a key enzyme in drug metabolism and the synthesis of cholesterol, steroids, and lipids. It localizes to the endoplasmic reticulum and is induced by glucocorticoids and certain drugs. CYP3A4 Protein, Human (His) is the recombinant human-derived CYP3A4 protein, expressed by E. coli , with N-10*His labeled tag.

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Cat. No.	Product Name	Chemical Structure

HY-17356S

Fenofibrate-d6
Fenofibrate-d₆ is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.

HY-133152S

Brexpiprazole S-oxide-d8

Brexpiprazole S-oxide-d₈ (DM-3411 D₈) is a deuterium labeled Brexpiprazole S-oxide (HY-133152). Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM .

HY-17356S2

Fenofibrate-13C6
Fenofibrate-13C6 is a deuterated labeled Fenofibrate . Fenofibrate is a selective PPARα agonist with an EC₅₀ of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC₅₀s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and *CYP3A4*, respectively.

HY-17356S1

Fenofibrate-d4
Fenofibrate-d₄ is the deuterium labeled Fenofibrate . Fenofibrate is a selective PPARα agonist with an EC₅₀ of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC₅₀s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively .

HY-100386S

Ticlopidine-d4

Ticlopidine-d₄ is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively .

HY-B0153AS

Ticlopidine-d4 hydrochloride

Ticlopidine-d₄ hydrochloride is the deuterium labeled Ticlopidine hydrochloride (HY-B0153A). Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively .

HY-W707554

Ticlopidine hydrochloride-d6

Ticlopidine hydrochloride-d₆ is the deuterium labeled Ticlopidine hydrochloride (HY-B0153A). Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively .

HY-166530S

Ticlopidine-d6 hydrochloride

Ticlopidine-d₆ hydrochloride is the deuterium labeled Ticlopidine hydrochloride. Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively .

Cat. No.	Product Name	Target	Research Areas	Chemical Structure