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Cyp2c9 Inhibitors

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By Targets:	Autophagy (7) Bacterial (4) Calcium Channel (1) COX (1) Cytochrome P450 (30) Endogenous Metabolite (3) FGFR (1) Fungal (1) Glucocorticoid Receptor (2) HCV Protease (2) Histamine Receptor (3) HIV (2) Isotope-Labeled Compounds (2) NF-κB (1) Parasite (1) Potassium Channel (1) PPAR (8) Reverse Transcriptase (1) Ribosomal S6 Kinase (RSK) (1) ROCK (1) Sodium Channel (1) URAT1 (2) Virus Protease (2)
By Research Areas:	Cancer (12) Cardiovascular Disease (11) Endocrinology (3) Infection (12) Inflammation/Immunology (11) Metabolic Disease (8) Neurological Disease (2)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas

HY-B1218

Sulfaphenazole 5+ Cited Publications	Bacterial	Infection
Sulfaphenazole is a specific inhibitor of CYP2C9 which blocks atherogenic and pro-inflammatory effects of linoleic acid (increase in oxidative stress and activation of AP-1) mediated by CYP2C9.

HY-N1201

Apigenin Maximum Cited Publications 17 Publications Verification 4',5,7-Trihydroxyflavone; Apigenol; C.I. Natural Yellow 1	Autophagy Cytochrome P450 Endogenous Metabolite	Inflammation/Immunology Cancer
Apigenin (4',5,7-Trihydroxyflavone) is a competitive *CYP2C9* inhibitor with a K_i of 2 μM.

HY-N0893

Tetrahydrocurcumin 1 Publications Verification HZIV 81-2	Cytochrome P450 Autophagy Endogenous Metabolite	Cancer Inflammation/Immunology
Tetrahydrocurcumin is a Curcuminoid found in turmeric (Curcuma longa) that is produced by the reduction of Curcumin. Tetrahydrocurcumin inhibit *CYP2C9* and CYP3A4.

HY-151251

CYP2C9/CYP2C19-IN-1	Cytochrome P450 Virus Protease	Infection
CYP2C9/CYP2C19-IN-1 (compound 22d) is a potent *CYP2C9/CYP2C19* inhibitor, possessing no hepatotoxicity and ames toxicity. CYP2C9/CYP2C19-IN-1 can be used in study of anti-ZIKV.

HY-U00048

Bucolome

Paramidin; Paramidine
Cytochrome P450 Inflammation/Immunology

Bucolome is a CYP2C9 inhibitor, used as an uricosuric agent or anti-inflammatory agent.

Bucolome Paramidin; Paramidine	Cytochrome P450	Inflammation/Immunology
Bucolome is a *CYP2C9* inhibitor, used as an uricosuric agent or anti-inflammatory agent.

HY-N0688

Linderane	Cytochrome P450	Inflammation/Immunology
Linderane, isolated from the root of Lindera aggregata, is an irreversible inhibitor cytochrome P450 2C9 (CYP2C9). Linderane has the potential to relieve pain and cramp.

HY-114759

MS-PPOH	Cytochrome P450	Cancer Metabolic Disease Neurological Disease
MS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor. MS-PPOH inhibits CYP2C8 and *CYP2C9* with IC₅₀s of 15 and 11 µM, respectively.

HY-B0281A

Ranitidine hydrochloride	Histamine Receptor Cytochrome P450 Bacterial	Infection Endocrinology Metabolic Disease
Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist with an IC₅₀ of 3.3 μM that inhibits gastric secretion. Ranitidine hydrochloride is a weak inhibitor of CYP2C19 and *CYP2C9*.

HY-B0693

Ranitidine	Histamine Receptor Bacterial Cytochrome P450	Infection Endocrinology Metabolic Disease Cancer
Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist with an IC₅₀ of 3.3 μM that inhibits gastric secretion. Ranitidine is a weak inhibitor of CYP2C19 and *CYP2C9*.

HY-B0258

Gemfibrozil 1 Publications Verification CI-719	PPAR Cytochrome P450	Metabolic Disease Cardiovascular Disease Cancer
Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with K_i values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.

HY-B0281AS

Ranitidine-d6 hydrochloride	Histamine Receptor Cytochrome P450 Bacterial	Infection Endocrinology Metabolic Disease
Ranitidine-d₆ (hydrochloride) is the deuterium labeled Ranitidine hydrochloride. Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine hydrochloride is a weak inhibitor of CYP2C19 and CYP2C9[1][2].

HY-B0258S

Gemfibrozil-d6 CI-719-d₆	PPAR Cytochrome P450	Metabolic Disease Cardiovascular Disease
Gemfibrozil-d₆ is the deuterium labeled Gemfibrozil. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.

HY-128859

EMT inhibitor-2	Cytochrome P450	Metabolic Disease
EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC₅₀s of 49.72 and 5.54 μM, respectively.

HY-151253

CYP2C1/CYP2C19-IN-2	Cytochrome P450 Virus Protease	Infection
CYP2C1/CYP2C19-IN-2 (compound 21d) is a potent *CYP2C9/CYP2C19* inhibitor, possessing no hepatotoxicity and ames toxicity. CYP2C1/CYP2C19-IN-2 can be used in study of anti-ZIKV.

HY-153970

URAT1 inhibitor 7	URAT1	Inflammation/Immunology
URAT1 inhibitor 7 (compound 10f) is a potent URAT1 inhibitor, with an IC₅₀ of 12 nM. URAT1 inhibitor 7 exhibits microsomal stability (HLM <13 µL/min/mg). URAT1 inhibitor 7 also inhibits *CYP2C9, with an IC₅₀* of 4.2 μM. URAT1 inhibitor 7 can be used for gout research.

HY-B0258R

Gemfibrozil (Standard) CI-719 (Standard)	PPAR Cytochrome P450	Metabolic Disease Cardiovascular Disease Cancer
Gemfibrozil (Standard) is the analytical standard of Gemfibrozil. This product is intended for research and analytical applications. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with K_i values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.

HY-143906

URAT1 inhibitor 2	URAT1	Inflammation/Immunology
URAT1 inhibitor 2 is an orally active and potent URAT1 and CYP isozyme inhibitor, with IC₅₀ values of 1.36 μM, 16.97 μM, 5.22 μM for URAT1-mediated ¹⁴C-UA uptake, CYP1A2 and CYP2C9, respectively. URAT1 inhibitor 2 is a promising agent candidate in the study of hyperuricemia and gout.

HY-17356

Fenofibrate 5+ 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-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-114415

AWZ1066S	Parasite	Infection
AWZ1066S is a highly potent, specific and orally active anti-Wolbachia agent with EC₅₀ value of 121 nM. AWZ1066S also is a weak CYP2C9 inhibitor and a weak CYP3A4 inducer with IC₅₀ values of 9.7 μM and 37 uM, respectively. AWZ1066S can be used for the research of tropical diseases such as Onchocerciasis (river blindness) and lymphatic filariasis (elephantiasis) .

HY-100386

Ticlopidine PCR 5332	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-147807

HIV-1 inhibitor-40	HIV Cytochrome P450	Infection
HIV-1 inhibitor-40 (Compound 4ab) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 with an EC₅₀ of 1.9 nM. HIV-1 inhibitor-40 displays weak CYP sensitivity with IC₅₀ values of 5.16 μM and 4.51 μM against CYP2C9 and CYP2C19, respectively. HIV-1 inhibitor-40 has no apparent in vivo acute toxicity.

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-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) 5+ 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-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-100386S

Ticlopidine-d4 PCR 5332-d₄	Isotope-Labeled Compounds 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[1]. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively[2][3].

HY-17356G

Fenofibrate (GMP)	Autophagy PPAR Cytochrome P450	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-141547

Nav1.7-IN-8	Sodium Channel Cytochrome P450	Inflammation/Immunology
Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits *CYP2C9* and CYP3A4 with an IC₅₀ of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain.

HY-N0043

Ginsenoside Rd Gypenoside VIII	NF-κB COX Calcium Channel Cytochrome P450 Endogenous Metabolite	Inflammation/Immunology Cardiovascular Disease 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 Ca²⁺ 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-12946

BI 653048	Glucocorticoid Receptor Cytochrome P450 HCV Protease	Infection Inflammation/Immunology
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-12946A

BI 653048 phosphate	Glucocorticoid Receptor Cytochrome P450 HCV Protease	Infection Inflammation/Immunology
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-149866

HIV-1 inhibitor-58	Reverse Transcriptase HIV Cytochrome P450	Infection
HIV-1 inhibitor-58 (Compound 10c) is a broad-spectrum antiviral agent. HIV-1 inhibitor-58 is a non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-58 inhibits WT strain IIIB, NNRTI-resistant strains (such as K103N and E138K) in MT-4 cells, with EC₅₀ less than 50 nM. HIV-1 inhibitor-58 also inhibits CYP2C9 and CYP2C19 (IC₅₀: 2.06 μM, 1.91 μM). HIV-1 inhibitor-58 can be used for HIV infection reserch.

HY-N2071

Cedrol (+)-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-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).

Cat. No.	Product Name	Target	Category

HY-N1201

Apigenin 15+ Cited Publications 4',5,7-Trihydroxyflavone; Apigenol; C.I. Natural Yellow 1	Autophagy Cytochrome P450 Endogenous Metabolite	Phenols Polyphenols Flavones Structural Classification Flavonoids Umbelliferae Apium graveliens L. Human Gut Microbiota Metabolites Endogenous metabolite Plants Source classification Disease Research Fields Cancer Classification of Application Fields
Apigenin (4',5,7-Trihydroxyflavone) is a competitive *CYP2C9* inhibitor with a K_i of 2 μM.

HY-N0893

Tetrahydrocurcumin 1 Publications Verification HZIV 81-2	Cytochrome P450 Autophagy Endogenous Metabolite	Phenols Polyphenols Structural Classification Curcuma longa Endogenous metabolite Plants Source classification Zingiberaceae Inflammation/Immunology Disease Research Fields Cancer Anti-aging Classification of Application Fields
Tetrahydrocurcumin is a Curcuminoid found in turmeric (Curcuma longa) that is produced by the reduction of Curcumin. Tetrahydrocurcumin inhibit *CYP2C9* and CYP3A4.

HY-N0688

Linderane	Cytochrome P450	Sesquiterpenes Terpenoids Inflammation/Immunology Disease Research Fields Classification of Application Fields Source classification Plants Lauraceae Lindera aggregata (Sims) Kosterm.
Linderane, isolated from the root of Lindera aggregata, is an irreversible inhibitor cytochrome P450 2C9 (CYP2C9). Linderane has the potential to relieve pain and cramp.

HY-N0043

Ginsenoside Rd Gypenoside VIII	NF-κB COX Calcium Channel Cytochrome P450 Endogenous Metabolite	Triterpenes Terpenoids Disease Research Fields Cancer Classification of Application Fields Cardiovascular Disease Source classification Plants Araliaceae Panax ginseng C. A. Meyer 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 Ca²⁺ 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-N2071

Cedrol (+)-Cedrol; α-Cedrol	Cytochrome P450 Fungal	Sesquiterpenes Terpenoids Inflammation/Immunology Disease Research Fields Cancer Classification of Application Fields Source classification Plants Pinaceae Cedrus deodara (Roxburgh) G. Don
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.

Cat. No.	Product Name

HY-B0281AS

Ranitidine-d6 hydrochloride
Ranitidine-d₆ (hydrochloride) is the deuterium labeled Ranitidine hydrochloride. Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine hydrochloride is a weak inhibitor of CYP2C19 and CYP2C9[1][2].

HY-B0258S

Gemfibrozil-d6
Gemfibrozil-d₆ is the deuterium labeled Gemfibrozil. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.

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-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[1]. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively[2][3].

Cyp2c9 Inhibitors

Inhibitors & Agonists

NaturalProducts

Isotope-Labeled Compounds

Natural
Products