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Isoforms Recommended:	CYP2

Results for "

CYP2A6

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (8) Adrenergic Receptor (5) Androgen Receptor (2) Autophagy (7) Bacterial (1) Calcium Channel (2) Cannabinoid Receptor (2) Cholinesterase (ChE) (3) Constitutive Androstane Receptor (1) COX (2) CXCR (2) Cytochrome P450 (51) Drug Metabolite (7) EGFR (3) Endogenous Metabolite (2) FGFR (1) Fungal (2) GABA Receptor (1) Glucocorticoid Receptor (4) HBV (1) HCV (2) HCV Protease (2) Histamine Receptor (1) HIV (2) iGluR (1) Influenza Virus (4) Isotope-Labeled Compounds (11) Monoamine Oxidase (1) nAChR (1) NF-κB (1) NO Synthase (1) Opioid Receptor (1) P2Y Receptor (3) Parasite (4) Potassium Channel (5) PPAR (6) Reverse Transcriptase (1) Ribosomal S6 Kinase (RSK) (1) ROCK (1) Small Interfering RNA (siRNA) (3) Sodium Channel (1)
By Research Areas:	Cancer (14) Cardiovascular Disease (18) Endocrinology (5) Infection (14) Inflammation/Immunology (16) Metabolic Disease (8) Neurological Disease (31)
Oligonucleotides:	Pre-designed siRNA Sets (3) siRNAs (3)

Inhibitors & Agonists

Fluorescent Dye

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N5132

(-)-Fenchone	Others	Others
(-)-Fenchone, a bicyclic monoterpene, is widely distributed in plants and found in essential oils from Foeniculum vulgare. (-)-Fenchone is oxidized to 6-endo-hydroxyfenchone, 6-exo-hydroxyfenchone and 10-hydroxyfenchone derivatives by CYP2A6 and CYP2B6 in human liver microsomes with CYP2A6 playing a more important role than CYP2B6 .

HY-135560

Nicotelline Nicotellin	Cytochrome P450	Neurological Disease
Nicotelline (Nicotellin) is a nicotine-related alkaloid, as well as a weak inhibitor of human cDNA-expressed cytochrome P-450 2A6 (CYP2A6). CYP2A6 mediates coumarin 7-hydroxylation, while Nicotelline fails to exhibit inhibition at 300 μM. Nicotelline can be used as a tracer and biomarker of particulate matter (PM) derived from tobacco smoke .

HY-N0494

Gentiopicroside 1 Publications Verification Gentiopicrin	Cytochrome P450 HCV	Inflammation/Immunology
Gentiopicroside, a naturally occurring iridoid glycoside, inhibits P450 activity, with an IC₅₀ and a K_i of 61 μM and 22.8 μM for CYP2A6; Gentiopicroside has anti-inflammatoryand antioxidative effects.

HY-RS03454

CYP2A6 Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
CYP2A6 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2A6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

CYP2A6 Human Pre-designed siRNA Set A CYP2A6 Human Pre-designed siRNA Set A

HY-W082430

CYP2A6-IN-2	Cytochrome P450	Neurological Disease
CYP2A6-IN-2 (compound 5) is a *CYP2A6* inhibitor. CYP2A6-IN-2 can be used in the study of nicotine dependence .

HY-155456

CYP2A6-IN-1	Cytochrome P450	Metabolic Disease
CD-6 is a flavonoid CYP2A6 inhibitor (IC₅₀: 1.566 μM). *CYP2A6* inhibits the metabolism of nicotine to cotinine, resulting in an increase in the amount of nicotine available in the blood, leading to increased smoking behavior. CD-6 mediates CYP2A6 inhibition and can be used in research on smoking cessation or smoking-related diseases .

HY-N5132R

(-)-Fenchone (Standard)	Others	Others
(-)-Fenchone (Standard) is the analytical standard of (-)-Fenchone. This product is intended for research and analytical applications. (-)-Fenchone, a bicyclic monoterpene, is widely distributed in plants and found in essential oils from Foeniculum vulgare. (-)-Fenchone is oxidized to 6-endo-hydroxyfenchone, 6-exo-hydroxyfenchone and 10-hydroxyfenchone derivatives by CYP2A6 and CYP2B6 in human liver microsomes with CYP2A6 playing a more important role than CYP2B6 .

HY-N8382

Chalepensin	Cytochrome P450	Neurological Disease
Chalepensin, a furanocoumarin, is a competitive *CYP2A6* inhibitor. Chalepensin also inhibits human CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to different extents .

HY-N6989

Isoglycycoumarin	Cytochrome P450	Metabolic Disease
Isoglycycoumarin is a flavonoid isolated from the roots of Glycyrrhiza uralensis. Isoglycycoumarin is a highly selective probe for human cytochrome P450 2A6 (CYP2A6) .

HY-134664

8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate	Cytochrome P450 Monoamine Oxidase	Inflammation/Immunology
8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate is an irreversible *CYP2A6* inhibitor with IC₅₀s of 8.64 μM and 22.3 μM with pre-incubation and co-incubaition, respectively. 8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate also inhibits MAO-A and MAO-B with IC₅₀s of 60.2 and 38.6 μM, respectively .

HY-24238

DLCI-1	Others	Others
DLCI-1 is a potent and selective oral inhibitor of cytochrome P450 2A6 (CYP2A6) that markedly reduces nicotine self-administration in both male and female mice.

HY-129105

Clomethiazole 2 Publications Verification	GABA Receptor Cytochrome P450	Neurological Disease
Chlormethiazole is an potent and orally active GABA_A agonist . Chlormethiazole inhibits cytochrome P450 isoforms: *CYP2A6* and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .

HY-N0494R

Gentiopicroside (Standard)	Cytochrome P450 HCV	Inflammation/Immunology
Gentiopicroside (Standard) is the analytical standard of Gentiopicroside. This product is intended for research and analytical applications. Gentiopicroside, a naturally occurring iridoid glycoside, inhibits P450 activity, with an IC50 and a Ki of 61 μM and 22.8 μM for CYP2A6; Gentiopicroside has anti-inflammatoryand antioxidative effects.

HY-N0904

Ginsenoside C-K 5 Publications Verification Ginsenoside compound K; Ginsenoside K	COX NO Synthase Cytochrome P450	Inflammation/Immunology
Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and *CYP2A6* in human liver microsomes with IC₅₀s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.

HY-RS03456

CYP2B6 Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
CYP2B6 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2B6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

CYP2B6 Human Pre-designed siRNA Set A CYP2B6 Human Pre-designed siRNA Set A

HY-RS03461

CYP2D6 Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
CYP2D6 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP2D6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

CYP2D6 Human Pre-designed siRNA Set A CYP2D6 Human Pre-designed siRNA Set A

HY-N2260

Cephaeline dihydrochloride 1 Publications Verification (-)-Cephaeline dihydrochloride; NSC 32944	Cytochrome P450	Infection
Cephaeline dihydrochloride is a selective *CYP2D6* inhibtor with an IC₅₀ of 121 μM.

HY-B0365AS

Memantine-d6 (hydrochloride)-6	Cytochrome P450 iGluR Autophagy	Neurological Disease
Memantine-d₆ (hydrochloride) is the deuterium labeled Memantine hydrochloride. Memantine (hydrochloride) (D-145 (hydrochloride)) is a moderate affinity, uncompetitive NMDA receptor antagonist, inhibit CYP2B6 and CYP2D6 with Ki of 0.51 nM and 94.9 μM, respectively[1].

HY-B1184

Mephenytoin 1 Publications Verification	Cytochrome P450	Neurological Disease
Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate .

HY-131630

O-Desmethylmetoprolol	Drug Metabolite	Others
O-Desmethylmetoprolol is the metabolite of Metoprolol (HY-17503) produced by CYP2D6 enzyme metabolism .

HY-10572A

(R)-Efavirenz (R)-DMP 266; (R)-EFV; (R)-L-743726	Reverse Transcriptase	Infection
(R)-Efavirenz ((R)-DMP 266) is a non-nucleoside reverse transcriptase inhibitor that acts by non-competitive inhibition of the viral enzyme. (R)-Efavirenz can be metabolized by CYP2B6 to 8-hydroxyefavirenz in a highly stereoselective manner. (R)-Efavirenz is promising to be a useful probe for the CYP2B6 active site and catalytic mechanisms .

HY-N2425

Rhodiosin	Cholinesterase (ChE)	Metabolic Disease
Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC₅₀ for CYP2D6 is 0.761 μM, and the K_i is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system

HY-N1483A

Guanfu base A hydrochloride	Potassium Channel	Cardiovascular Disease
Guanfu base A hydrochloride is an antiarrhythmic alkaloid with the ability to inhibit CYP2D6 enzyme activity. Guanfu base A hydrochloride can be used to inhibit arrhythmia-related diseases. Guanfu base A hydrochloride exhibits inhibitory effects on CYP2D6 in different species of organisms, including humans, monkeys, and dogs. The biological activity of Guanfu base A hydrochloride makes it have potential clinical application value .

HY-W040468

2-Phenyl-2-(1-piperidinyl)propane	Cytochrome P450	Metabolic Disease
2-Phenyl-2-(1-piperidinyl)propane is a selective and reversible human *CYP2B6* inhibitor with an IC₅₀ of 5.1 μM and a K_i of 5.6. 2-Phenyl-2-(1-piperidinyl)propane inhibits CYP2D6 (IC₅₀=74 μM), CYP3A (IC₅₀=200 μM) .

HY-N2129

N-Nornuciferine 1 Publications Verification	Cytochrome P450	Cardiovascular Disease Metabolic Disease
N-Nornuciferine is an aporphine alkaloid in lotus leaf that significantly inhibits *CYP2D6* with IC₅₀ and K_i of 3.76 and 2.34 μM, respectively.

HY-N11706

β-Cedrene (+)-β-Cedrene	Fungal	Infection Inflammation/Immunology
β-Cedrene ((+)-β-Cedrene) is a sesquiterpene compound that can be isolated from Centaurea kotschyi var. kotschyi and Centaurea kotschyi var. decumbens, exhibiting antibacterial, anti-inflammatory, antispasmodic, tonic, diuretic, sedative, insecticidal, and antifungal activities. β-Cedrene is also a potent competitive inhibitor of the CYP2B6-mediatedbupropion hydroxylase, with a K_i value of 1.6 μM .

HY-B1184S1

Mephenytoin-d5	Cytochrome P450	Neurological Disease
Mephenytoin-d₅ is the deuterium labeled Mephenytoin. Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate[1].

HY-N2260R

Cephaeline dihydrochloride (Standard)	Cytochrome P450	Infection
Cephaeline (dihydrochloride) (Standard) is the analytical standard of Cephaeline (dihydrochloride). This product is intended for research and analytical applications. Cephaeline dihydrochloride is a selective CYP2D6 inhibtor with an IC50 of 121 μM.

HY-N2425R

Rhodiosin (Standard)	Cholinesterase (ChE)	Metabolic Disease
Rhodiosin (Standard) is the analytical standard of Rhodiosin. This product is intended for research and analytical applications. Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC₅₀ for CYP2D6 is 0.761 μM, and the Ki is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system

HY-B1184S2

Mephenytoin-d8	Cytochrome P450	Neurological Disease
Mephenytoin-d₈ is the deuterium labeled Mephenytoin[1]. Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate[2].

HY-B1184R

Mephenytoin (Standard)	Cytochrome P450	Neurological Disease
Mephenytoin (Standard) is the analytical standard of Mephenytoin. This product is intended for research and analytical applications. Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate .

HY-N0598

Ginsenoside F1 20(S)-Ginsenoside F1	Cytochrome P450 Endogenous Metabolite	Cancer
Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.

HY-B1184S3

Mephenytoin-13C,d3	Isotope-Labeled Compounds Cytochrome P450	Neurological Disease
Mephenytoin-13C,d3 is a deuterated labeled Mephenytoin . Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate .

HY-105124A

Bufuralol hydrochloride 1 Publications Verification Ro 3-4787 hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Bufuralol (Ro 3-4787) hydrochloride is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate .

HY-105124

Bufuralol 1 Publications Verification Ro 3-4787	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Bufuralol (Ro 3-4787) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate .

HY-100064

O-Desmethyl gefitinib	EGFR	Cancer
O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC₅₀ of 36 nM in subcellular assays .

HY-N3090

Peucedanol	Cytochrome P450	Metabolic Disease
Peucedanol is a non-competitive inhibitor of CYP3A4 with a K_i value of 4.07 μM and a competitive inhibitor of CYP1A2 and *CYP2D6* with K_i values of 3.39 μM and 6.77 μM, respectively .

HY-100665

Dehydroaripiprazole 1 Publications Verification OPC-14857; DM-14857	5-HT Receptor	Neurological Disease
Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole .

HY-113575

Dehydroaripiprazole hydrochloride OPC-14857 hydrochloride; DM-14857 hydrochloride	5-HT Receptor	Neurological Disease
Dehydroaripiprazole (OPC-14857) hydrochloride is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole hydrochloride. Dehydroaripiprazole hydrochloride has with antipsychotic activity equivalent to Aripiprazole .

HY-109054

O-Demethyltramadol	Drug Metabolite	Neurological Disease
O-Demethyltramadol is a primary active metabolite of Tramadol. O-Demethyltramadol is mainly responsible for its µ-opioid receptor-related analgesic effect. Tramadol is metabolized to O-Demethyltramadol mainly by the cytochrome P450 (CYP) 2D6 enzyme .

HY-109054A

O-Desmethyltramadol hydrochloride	Drug Metabolite	Neurological Disease
O-Desmethyltramadol (hydrochloride) is a primary active metabolite of Tramadol. O-Demethyltramadol is mainly responsible for its µ-opioid receptor-related analgesic effect. Tramadol is metabolized to O-Demethyltramadol mainly by the cytochrome P450 (CYP) 2D6 enzyme .

HY-151239

ONT-993 AR 00440993	Cytochrome P450	Cancer
ONT-993 is an aliphatic hydroxylated metabolite. ONT-993 inhibits *CYP2D6* (IC₅₀=7.9 µM) and causes metabolism-dependent inactivation of CYP3A (KI=1.6 µM) .

HY-100637

Hydroxybupropion	Drug Metabolite Adrenergic Receptor nAChR	Neurological Disease
Hydroxybupropion is the major active metabolite of Bupropion. Hydroxybupropion is metabolized by CYP2B6. Bupropion is an atypical antidepressant and smoking-cessation agent. Hydroxybupropion inhibits norepinephrine uptake with an IC₅₀ value of 1.7 μM. Hydroxybupropion is also a nACh receptor antagonist .

HY-W803860

N-Depropylpropafenone	Drug Metabolite Sodium Channel	Cardiovascular Disease
N-Depropylpropafenone is an active metabolite of Propafenone (HY-B0432), generated through the CYP450 enzyme system (mainly *CYP2D6). It functions by blocking sodium ion channels*, slowing myocardial conduction and exhibiting certain antiarrhythmic effects .

HY-100238

Antihistamine-1	Histamine Receptor Cytochrome P450 Potassium Channel	Neurological Disease Endocrinology
Antihistamine-1 is a H1-antihistamine (K_i=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of *CYP2D6* and hERG channel with IC₅₀s of 5.4 and 0.8 μM, respectively.

HY-144285

CXCR4 antagonist 4	CXCR HIV	Inflammation/Immunology
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC₅₀=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC₅₀=7 nM) .

HY-W010195

2,6-Dimethylquinoline	Cytochrome P450	Others
2,6-Dimethylquinoline, a nature constituent from the roots of Peucedantu praeruptorum, is a CYP1A2 inhibitor with an IC₅₀ of 3.3 µM. 2,6-Dimethylquinoline also inhibits *CYP2B6* activity with an IC₅₀ of 480 µM .

HY-B0352A

(S)-Mirtazapine (S)-Org3770; (S)-6-Azamianserin	5-HT Receptor	Neurological Disease
(S)-Mirtazapine ((S)-Org3770) is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception. (S)-Mirtazapine is a stereoselective 5-HT₂ receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2 .

HY-100665S

Dehydroaripiprazole-d8 OPC-14857-d₈; DM-14857-d₈	Isotope-Labeled Compounds 5-HT Receptor	Neurological Disease
Dehydroaripiprazole-d₈ is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1][2][3].

HY-156330

HIV-IN-9	HIV Cytochrome P450	Infection
HIV-IN-9 (Compound 2b) is a HIV inhibitor (IC₅₀: 6.65 μg/mL), and has high binding affinity with HIV-RT. HIV-IN-9 also inhibits CYP3A4, CYP1A2, CYP2C1, and CYP2D6 .

Cat. No.	Product Name	Type

HY-17356G

Fenofibrate (GMP)

Fluorescent Dye

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.

Cat. No.	Product Name	Type

HY-17356G

Fenofibrate (GMP)

Biochemical Assay Reagents

Cat. No.	Product Name	Target	Research Area

HY-144285

CXCR4 antagonist 4	CXCR HIV	Inflammation/Immunology
CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC₅₀=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC₅₀=7 nM) .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N5132

(-)-Fenchone	Structural Classification Other Monoterpenes Classification of Application Fields Terpenoids Source classification Other Diseases Umbelliferae Plants Vernonia Schreb. Disease Research Fields	Others
(-)-Fenchone, a bicyclic monoterpene, is widely distributed in plants and found in essential oils from Foeniculum vulgare. (-)-Fenchone is oxidized to 6-endo-hydroxyfenchone, 6-exo-hydroxyfenchone and 10-hydroxyfenchone derivatives by CYP2A6 and CYP2B6 in human liver microsomes with CYP2A6 playing a more important role than CYP2B6 .

HY-N0494

Gentiopicroside 1 Publications Verification Gentiopicrin	Structural Classification Gentiana scabra Bunge Iridoids Classification of Application Fields Terpenoids Source classification Gentianaceae Plants Inflammation/Immunology Disease Research Fields	Cytochrome P450 HCV
Gentiopicroside, a naturally occurring iridoid glycoside, inhibits P450 activity, with an IC₅₀ and a K_i of 61 μM and 22.8 μM for CYP2A6; Gentiopicroside has anti-inflammatoryand antioxidative effects.

HY-N0904

Ginsenoside C-K 5 Publications Verification Ginsenoside compound K; Ginsenoside K	Panax ginseng C. A. Meyer Triterpenes Structural Classification Classification of Application Fields Terpenoids Source classification Plants Inflammation/Immunology Disease Research Fields Araliaceae	COX NO Synthase Cytochrome P450
Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and *CYP2A6* in human liver microsomes with IC₅₀s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.

HY-N2260

Cephaeline dihydrochloride 1 Publications Verification (-)-Cephaeline dihydrochloride; NSC 32944	Infection Alkaloids Structural Classification Monophenols other families Classification of Application Fields Source classification Phenols Plants Isoquinoline Alkaloids Disease Research Fields	Cytochrome P450
Cephaeline dihydrochloride is a selective *CYP2D6* inhibtor with an IC₅₀ of 121 μM.

HY-N2425

Rhodiosin	Flavonols Structural Classification Classification of Application Fields Crassulaceae Source classification Metabolic Disease Plants Rhodiola crenulata (HK. f. et.Thoms) H. Ohba Flavonoids Rhodiola rosea Linn. Phenols Polyphenols Disease Research Fields	Cholinesterase (ChE)
Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC₅₀ for CYP2D6 is 0.761 μM, and the K_i is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system

HY-N5132R

(-)-Fenchone (Standard)	Structural Classification Other Monoterpenes Terpenoids Source classification Umbelliferae Plants Vernonia Schreb.	Others
(-)-Fenchone (Standard) is the analytical standard of (-)-Fenchone. This product is intended for research and analytical applications. (-)-Fenchone, a bicyclic monoterpene, is widely distributed in plants and found in essential oils from Foeniculum vulgare. (-)-Fenchone is oxidized to 6-endo-hydroxyfenchone, 6-exo-hydroxyfenchone and 10-hydroxyfenchone derivatives by CYP2A6 and CYP2B6 in human liver microsomes with CYP2A6 playing a more important role than CYP2B6 .

HY-N8382

Chalepensin	Structural Classification Natural Products Haloxylon ammodendron (C. A. Mey.) Bunge Source classification Amaranthaceae Plants	Cytochrome P450
Chalepensin, a furanocoumarin, is a competitive *CYP2A6* inhibitor. Chalepensin also inhibits human CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to different extents .

HY-N6989

Isoglycycoumarin	Classification of Application Fields Leguminosae Source classification Coumarins Phenols Polyphenols Metabolic Disease Phenylpropanoids Plants Disease Research Fields Glycyrrhiza uralensis Fisch.	Cytochrome P450
Isoglycycoumarin is a flavonoid isolated from the roots of Glycyrrhiza uralensis. Isoglycycoumarin is a highly selective probe for human cytochrome P450 2A6 (CYP2A6) .

HY-134664

8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate	Structural Classification Terpenoids Sesquiterpenes Source classification Plants Compositae Vachellia nilotica (L.) P. J. H. Hurter & Mabb.	Cytochrome P450 Monoamine Oxidase
8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate is an irreversible *CYP2A6* inhibitor with IC₅₀s of 8.64 μM and 22.3 μM with pre-incubation and co-incubaition, respectively. 8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate also inhibits MAO-A and MAO-B with IC₅₀s of 60.2 and 38.6 μM, respectively .

HY-N0494R

Gentiopicroside (Standard)	Structural Classification Gentiana scabra Bunge Iridoids Terpenoids Source classification Gentianaceae Plants	Cytochrome P450 HCV
Gentiopicroside (Standard) is the analytical standard of Gentiopicroside. This product is intended for research and analytical applications. Gentiopicroside, a naturally occurring iridoid glycoside, inhibits P450 activity, with an IC50 and a Ki of 61 μM and 22.8 μM for CYP2A6; Gentiopicroside has anti-inflammatoryand antioxidative effects.

HY-N1483A

Guanfu base A hydrochloride	Structural Classification Alkaloids Aconitum coreanum (Lévl.) Rapaics Other Alkaloids Ranunculaceae Source classification Plants	Potassium Channel
Guanfu base A hydrochloride is an antiarrhythmic alkaloid with the ability to inhibit CYP2D6 enzyme activity. Guanfu base A hydrochloride can be used to inhibit arrhythmia-related diseases. Guanfu base A hydrochloride exhibits inhibitory effects on CYP2D6 in different species of organisms, including humans, monkeys, and dogs. The biological activity of Guanfu base A hydrochloride makes it have potential clinical application value .

HY-N2129

N-Nornuciferine 1 Publications Verification	Cardiovascular Disease Alkaloids Structural Classification other families Classification of Application Fields Source classification Metabolic Disease Nelumbo nucifera Gaertn. Plants Isoquinoline Alkaloids Nymphaeaceae Disease Research Fields	Cytochrome P450
N-Nornuciferine is an aporphine alkaloid in lotus leaf that significantly inhibits *CYP2D6* with IC₅₀ and K_i of 3.76 and 2.34 μM, respectively.

HY-N11706

β-Cedrene (+)-β-Cedrene	Centaurea kotschyi (Boiss.) Hayek Structural Classification Natural Products Source classification Plants Compositae	Fungal
β-Cedrene ((+)-β-Cedrene) is a sesquiterpene compound that can be isolated from Centaurea kotschyi var. kotschyi and Centaurea kotschyi var. decumbens, exhibiting antibacterial, anti-inflammatory, antispasmodic, tonic, diuretic, sedative, insecticidal, and antifungal activities. β-Cedrene is also a potent competitive inhibitor of the CYP2B6-mediatedbupropion hydroxylase, with a K_i value of 1.6 μM .

HY-N2260R

Cephaeline dihydrochloride (Standard)	Alkaloids Structural Classification Monophenols other families Source classification Phenols Plants Isoquinoline Alkaloids	Cytochrome P450
Cephaeline (dihydrochloride) (Standard) is the analytical standard of Cephaeline (dihydrochloride). This product is intended for research and analytical applications. Cephaeline dihydrochloride is a selective CYP2D6 inhibtor with an IC50 of 121 μM.

HY-N2425R

Rhodiosin (Standard)	Flavonols Structural Classification Flavonoids Rhodiola rosea Linn. Crassulaceae Source classification Phenols Polyphenols Plants Rhodiola crenulata (HK. f. et.Thoms) H. Ohba	Cholinesterase (ChE)
Rhodiosin (Standard) is the analytical standard of Rhodiosin. This product is intended for research and analytical applications. Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC₅₀ for CYP2D6 is 0.761 μM, and the Ki is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system

HY-N0598

Ginsenoside F1 20(S)-Ginsenoside F1	Panax ginseng C. A. Meyer Triterpenes Structural Classification Classification of Application Fields Terpenoids Source classification Plants Endogenous metabolite Disease Research Fields Araliaceae Cancer	Cytochrome P450 Endogenous Metabolite
Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.

HY-N3090

Peucedanol	Structural Classification Carpesium cernuum L. Source classification Coumarins Phenylpropanoids Plants Umbelliferae	Cytochrome P450
Peucedanol is a non-competitive inhibitor of CYP3A4 with a K_i value of 4.07 μM and a competitive inhibitor of CYP1A2 and *CYP2D6* with K_i values of 3.39 μM and 6.77 μM, respectively .

HY-W010195

2,6-Dimethylquinoline	Alkaloids Structural Classification Chrysanthemum × morifolium (Ramat.) Hemsl. Classification of Application Fields Source classification Other Diseases Quinoline Alkaloids Umbelliferae Plants Disease Research Fields	Cytochrome P450
2,6-Dimethylquinoline, a nature constituent from the roots of Peucedantu praeruptorum, is a CYP1A2 inhibitor with an IC₅₀ of 3.3 µM. 2,6-Dimethylquinoline also inhibits *CYP2B6* activity with an IC₅₀ of 480 µM .

HY-N6023

Thermopsoside	Flavonoids Classification of Application Fields Flavones Astragalus microcephalus Willd. Source classification Other Diseases Phenols Polyphenols Plants Compositae Disease Research Fields	Cytochrome P450
Thermopsoside is a flavone derivative isolated from Aspalathus linearis. Thermopsoside exhibits inhibitory effects on CYP450 isozymes with IC₅₀ values of 6.0 μM, 9.5 μM, 12.0 μM, 32.0 μM, for CYP3A4, CYP2C19, CYP2D6 and CYP2C9, respectively .

HY-W008364

Olivetol	Structural Classification Microorganisms other families Source classification Phenols Polyphenols Plants	Cytochrome P450 Cannabinoid Receptor
Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2 . Olivetol also inhibits CYP2C19 and *CYP2D6* activity, with IC₅₀s of 15.3 μM, 7.21 μM and K_is of 2.71 μM, 2.87 μM, respectively .

HY-N1483

Guanfu base A	Cardiovascular Disease Alkaloids Classification of Application Fields Source classification Ranunculaceae Aconitum carmichaeli Debx. Plants Disease Research Fields	Potassium Channel
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive *CYP2D6* inhibitor, with a K_i of 1.20 μM in human liver microsomes (HLMs) and a K_i of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (K_i of 0.38 μM) and dog (K_i of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .

HY-W008364R

Olivetol (Standard)	Structural Classification Microorganisms other families Source classification Phenols Polyphenols Plants	Cytochrome P450 Cannabinoid Receptor
Olivetol (Standard) is the analytical standard of Olivetol. This product is intended for research and analytical applications. Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2 . Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively .

HY-N0043

Ginsenoside Rd 1 Publications Verification Gypenoside VIII	Panax ginseng C. A. Meyer Cardiovascular Disease Triterpenes Structural Classification Classification of Application Fields Terpenoids Source classification Plants Endogenous metabolite Disease Research Fields Araliaceae Cancer	NF-κB COX Calcium Channel Cytochrome P450 Endogenous Metabolite
Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC₅₀ of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca ²⁺ influx. Ginsenoside Rd inhibits *CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC₅₀*s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.

Cat. No.	Product Name	Chemical Structure

HY-B0365AS

Memantine-d6 (hydrochloride)-6
Memantine-d₆ (hydrochloride) is the deuterium labeled Memantine hydrochloride. Memantine (hydrochloride) (D-145 (hydrochloride)) is a moderate affinity, uncompetitive NMDA receptor antagonist, inhibit CYP2B6 and CYP2D6 with Ki of 0.51 nM and 94.9 μM, respectively[1].

HY-B1184S1

Mephenytoin-d5
Mephenytoin-d₅ is the deuterium labeled Mephenytoin. Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate[1].

HY-100064S

O-Desmethyl gefitinib-d8
O-Desmethyl gefitinib-d₈ is a deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].

HY-133116S

4-Hydroxyatomoxetine-d3
4-Hydroxyatomoxetine-d₃ is a deuterium labeled 4-Hydroxyatomoxetine. 4-Hydroxyatomoxetine is an active metabolite of Atomoxetine (Tomoxetine). 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine is a potent and selective noradrenal in re-uptake inhibitor[1].

HY-B0352AS

(S)-Mirtazapine-d3
(S)-Mirtazapine-d₃ is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception.(S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2[1].

HY-B1184S2

Mephenytoin-d8
Mephenytoin-d₈ is the deuterium labeled Mephenytoin[1]. Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate[2].

HY-B1184S3

Mephenytoin-13C,d3
Mephenytoin-13C,d3 is a deuterated labeled Mephenytoin . Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate .

HY-100665S

Dehydroaripiprazole-d8
Dehydroaripiprazole-d₈ is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1][2][3].

HY-100064S1

O-Desmethyl gefitinib-d6
O-Desmethyl gefitinib-d₆ is the deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].

HY-109054AS

O-Desmethyltramadol-d6 hydrochloride
O-Desmethyltramadol-d6 (hydrochloride) is a deuterated labeled O-Desmethyltramadol (hydrochloride) . O-Desmethyltramadol (hydrochloride) is a primary active metabolite of Tramadol. O-Demethyltramadol is mainly responsible for its μ-opioid receptor-related analgesic effect. Tramadol is metabolized to O-Demethyltramadol mainly by the cytochrome P450 (CYP) 2D6 enzyme .

HY-132428S

O-Desmethyl Tramadol-d6
O-Desmethyl Tramadol-d₆ is the deuterium labeled O-Desmethyl Tramadol. O-Desmethyl Tramadol is a primary active metabolite of Tramadol. O-Desmethyl Tramadol is mainly responsible for its µ-opioid receptor-related analgesic effect. Tramadol is metabolized to O-Demethyltramadol mainly by the cytochrome P450 (CYP) 2D6 enzyme[1].

HY-135810S

Cletoquine-d4

Cletoquine-d₄ is deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].

HY-135810S1

Cletoquine-d4-1

Cletoquine-d₄-1 is the deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].

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-17356S1

Fenofibrate-d4
Fenofibrate-d₄ is the deuterium labeled Fenofibrate[1]. 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[2][3].

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-17459S

Clopidogrel-d3 hydrogen sulfate

Clopidogrel-d₃ (hydrogen sulfate) is the deuterium labeled Clopidogrel hydrogen sulfate[1]. Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively. Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation．Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor[2][3][4][5][6].

HY-W754151

N-Desmethyl apalutamide-d4

N-Desmethyl apalutamide-d₄ is the deuterium-labeled N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .

HY-135331S

N-Desmethyl-Apalutamide-15N,d4

N-Desmethyl-Apalutamide-15N,d4 is the ¹⁵N and deuterium labeled isotope of N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .

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