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CYP2A6 Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Adrenergic Receptor (2) Autophagy (5) Calcium Channel (3) Cannabinoid Receptor (1) Cholinesterase (ChE) (1) Constitutive Androstane Receptor (1) COX (2) Cytochrome P450 (28) Drug Metabolite (1) EGFR (2) Endogenous Metabolite (2) FGFR (1) Fungal (2) GABA Receptor (1) Glucocorticoid Receptor (2) HCV (1) HIV (1) Isotope-Labeled Compounds (2) Monoamine Oxidase (1) NF-κB (2) P2Y Receptor (3) Potassium Channel (2) PPAR (5) Ribosomal S6 Kinase (RSK) (1) ROCK (1)
By Research Areas:	Cancer (12) Cardiovascular Disease (11) Endocrinology (2) Infection (3) Inflammation/Immunology (8) Metabolic Disease (6) Neurological Disease (8)

By Targets:

5-HT Receptor (1)

Adrenergic Receptor (2)

Autophagy (5)

Calcium Channel (3)

Cannabinoid Receptor (1)

Cholinesterase (ChE) (1)

Constitutive Androstane Receptor (1)

COX (2)

Cytochrome P450 (28)

Drug Metabolite (1)

EGFR (2)

Endogenous Metabolite (2)

FGFR (1)

Fungal (2)

GABA Receptor (1)

Glucocorticoid Receptor (2)

HCV (1)

HIV (1)

Isotope-Labeled Compounds (2)

Monoamine Oxidase (1)

NF-κB (2)

P2Y Receptor (3)

Potassium Channel (2)

PPAR (5)

Ribosomal S6 Kinase (RSK) (1)

ROCK (1)

By Research Areas:

Cancer (12)

Cardiovascular Disease (11)

Endocrinology (2)

Infection (3)

Inflammation/Immunology (8)

Metabolic Disease (6)

Neurological Disease (8)

Inhibitors & Agonists

Fluorescent Dye

Biochemical Assay Reagents

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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-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-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-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-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-100064

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 .

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-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-N2071

Cedrol 1 Publications Verification (+)-Cedrol; α-Cedrol	Cytochrome P450 Fungal	Infection Inflammation/Immunology Cancer
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with K_i of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes . Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities .

HY-100238

Antihistamine-1
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-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 .

HY-133116S

4-Hydroxyatomoxetine-d3	Adrenergic Receptor	Neurological Disease
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-100064S

O-Desmethyl gefitinib-d8	EGFR	Cancer
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-100064S1

O-Desmethyl gefitinib-d6	Isotope-Labeled Compounds EGFR	Cancer
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-110134

S07662	Constitutive Androstane Receptor	Metabolic Disease
S07662 is a human constitutive androstane receptor (hCAR) inhibitor with an IC₅₀ of 0.7 μM. S07662 recruits the corepressor NCoR in cell-based assays and attenuate the expression of CYP2B6 mRNA in human primary hepatocytes induced by phenytoin (HY-B0448) and CITCO (HY-103244) .

HY-133116

4-Hydroxyatomoxetine	Adrenergic Receptor	Neurological Disease
4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (K_i values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .

HY-W008364

Olivetol	Cytochrome P450 Cannabinoid Receptor	Neurological Disease
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-W011235

Norfluoxetine hydrochloride	5-HT Receptor Calcium Channel Drug Metabolite	Neurological Disease
Norfluoxetine hydrochloride is an active N-demethylated metabolite of Fluoxetine. Fluoxetine is a selective serotonin (5-HT) reuptake inhibitor that is metabolized to Norfluoxetine hydrochloride by cytochrome P450 (CYP) 2D6, CYP2C19, and CYP3A4. Norfluoxetine hydrochloride inhibits 5-HT uptake and inhibits CaV3.3 T current (IC50 = 5 μM). Norfluoxetine hydrochloride has anticonvulsant activity .

HY-18063

ML252	Potassium Channel Cytochrome P450	Neurological Disease
ML252 is a selective inhibitor of potassium channel, targeting to KCNQ2 channel (Kv7.2) (IC₅₀=69 nM). ML252 also inhibits Cytochrome P450 with IC₅₀s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively .

HY-17459

Clopidogrel hydrogen sulfate Maximum Cited Publications 17 Publications Verification (S)-(+)-Clopidogrel bisulfate; (S)-(+)-Clopidogrel hydrogen sulfate	Cytochrome P450 P2Y Receptor	Cardiovascular Disease Cancer
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 .

HY-N1483

Guanfu base A	Potassium Channel	Cardiovascular Disease
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-16718

Dagrocorat PF-00251802	Glucocorticoid Receptor Cytochrome P450	Inflammation/Immunology Endocrinology
Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC₅₀=1.3 μM in human liver microsomes) and *CYP2D6* (K_i=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis .

HY-16718A

Dagrocorat hydrochloride PF-00251802 hydrochloride	Glucocorticoid Receptor Cytochrome P450	Inflammation/Immunology Endocrinology
Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC₅₀=1.3 μM in human liver microsomes) and *CYP2D6* (K_i=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis .

HY-17356

Fenofibrate 10+ Cited Publications	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-17459S

Clopidogrel-d3 hydrogen sulfate (S)-(+)-Clopidogrel bisulfate-d₃; (S)-(+)-Clopidogrel-d₃ hydrogen sulfate	P2Y Receptor Cytochrome P450
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-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-148597

FGFR-IN-10	FGFR Cytochrome P450	Cancer
FGFR-IN-10 is an orally active inhibitor of FGFR and Cytochrome P450 (CYPs). FGFR-IN-10 inhibits wide type and V564F mutant FGFR2 with IC₅₀s of 104.1 nM and 43.6 nM, respectively. FGFR-IN-10 also inhibits CYPs with IC₅₀s of 3.33 μM (CYP2C9), 18.75 μM (CYP2C19), 4.34 μM (CYP2CD6), and 0.69 μM (CYP3A4), respectively .

HY-17459R

Clopidogrel hydrogen sulfate (Standard) (S)-(+)-Clopidogrel bisulfate (Standard); (S)-(+)-Clopidogrel hydrogen sulfate (Standard)	Cytochrome P450 P2Y Receptor	Cardiovascular Disease Cancer
Clopidogrel (hydrogen sulfate) (Standard) is the analytical standard of Clopidogrel (hydrogen sulfate). This product is intended for research and analytical applications. 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 .

HY-17356S1

Fenofibrate-d4	PPAR Autophagy Cytochrome P450
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-17356R

Fenofibrate (Standard) 10+ Cited Publications	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-N0043

Ginsenoside Rd Gypenoside VIII	NF-κB COX Calcium Channel Cytochrome P450 Endogenous Metabolite	Cardiovascular Disease Inflammation/Immunology Cancer
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.

HY-12946A

BI 653048 phosphate
BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC₅₀ value of 55 nM . BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC₅₀>30 μM) . BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .

HY-12946

BI 653048
BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC₅₀ value of 55 nM . BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC₅₀>30 μM) . BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .

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-N0043R

Ginsenoside Rd (Standard) Gypenoside VIII (Standard)	NF-κB COX Calcium Channel Cytochrome P450 Endogenous Metabolite	Cardiovascular Disease Inflammation/Immunology Cancer
Ginsenoside Rd (Standard) is the analytical standard of Ginsenoside Rd. This product is intended for research and analytical applications. 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.

HY-14362

GSK-25	ROCK Ribosomal S6 Kinase (RSK)	Cardiovascular Disease
GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC₅₀=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC₅₀=398 nM, p70S6K: IC₅₀=1 μM). GSK-25 inhibits P450 profile (IC₅₀s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively) .

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.

Fenofibrate (GMP)	Biochemical Assay Reagents
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	Category	Target	Chemical Structure

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-N2425

Rhodiosin	Flavonols Structural Classification Classification of Application Fields Source classification Crassulaceae 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-N2129

N-Nornuciferine 1 Publications Verification	Cardiovascular Disease Alkaloids other families Classification of Application Fields Source classification Metabolic Disease Nelumbo nucifera Gaertn. Plants Isoquinoline Alkaloids Disease Research Fields Nymphaeaceae	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-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-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-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-N3090

Peucedanol	Structural Classification Source classification Isodon yuennanensis (Handel-Mazzetti) H. Hara 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 Chrysanthemum × morifolium (Ramat.) Hemsl. Classification of Application Fields Source classification Other Diseases Quinoline Alkaloids Plants Umbelliferae 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-N2071

Cedrol 1 Publications Verification (+)-Cedrol; α-Cedrol	Cedrus deodara (Roxburgh) G. Don Classification of Application Fields Pinaceae Terpenoids Sesquiterpenes Source classification Plants Inflammation/Immunology Disease Research Fields Cancer	Cytochrome P450 Fungal
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with K_i of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes . Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities .

HY-W008364

Olivetol	Structural Classification other families Microorganisms 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-N0043

Ginsenoside Rd Gypenoside VIII	Cardiovascular Disease Panax ginseng C. A. Meyer Triterpenes 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.

HY-N0043R

Ginsenoside Rd (Standard) Gypenoside VIII (Standard)	Cardiovascular Disease Panax ginseng C. A. Meyer 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 (Standard) is the analytical standard of Ginsenoside Rd. This product is intended for research and analytical applications. 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-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-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-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-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-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-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].

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