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CYP3A4 inhibition

" in MedChemExpress (MCE) Product Catalog:

By Targets:	CGRP Receptor (1) Cytochrome P450 (14) DNA/RNA Synthesis (1) Endogenous Metabolite (3) Ephrin Receptor (1) Factor Xa (1) Flavivirus (1) Influenza Virus (1) IPK Superfamily (1) JAK (1) MAP3K (1) MAP4K (1) NAMPT (1) P-glycoprotein (1) Parasite (1) PDGFR (1) Potassium Channel (1) Reference Standards (2) SARS-CoV (1) Sodium Channel (1) STAT (1) TNF Receptor (1) VEGFR (1) γ-secretase (1)
By Research Areas:	Cancer (8) Cardiovascular Disease (1) Infection (3) Inflammation/Immunology (3) Metabolic Disease (3) Neurological Disease (6)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N0598

Ginsenoside F1 1 Publications Verification 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-134772

AS1810722	STAT Cytochrome P450	Inflammation/Immunology
AS1810722 is an orally active and potent STAT6 inhibitor with an IC₅₀ of 1.9 nM. AS1810722 shows a good profile of *CYP3A4* inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research .

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-110079

TNP	IPK Superfamily	Cancer
TNP is a competitive, reversible inhibitor of IP6K1 and IP3K, with IC₅₀s of 0.55 μM and 10.2 μM for IP6K1 and IP3K, respectively. TNP competitively binds to the ATP binding site of IP6K, inhibits the generation of 5-IP7, and thus relieves the inhibition of 5-IP7 on the AKT signaling pathway. TNP can enhance insulin sensitivity and promote thermogenesis in adipose tissue. TNP cannot effectively pass through the blood-brain barrier and is mainly used in the study of obesity, type 2 diabetes, and metabolic syndrome. However, TNP also inhibits CYP3A4 and may need further optimization[1][2][3].

HY-W267897

7-Benzyloxy-4-(trifluoromethyl)coumarin 7-BFC	Cytochrome P450	Others
7-Benzyloxy-4-(trifluoromethyl)coumarin (7-BFC) is a coumarin fluorescent substrate. 7-Benzyloxy-4-(trifluoromethyl)coumarin is a substrate for cDNA-expressed CYP1A2 and CYP3A4 and is metabolized to 7-hydroxy-4-trifluoromethylcoumarin (HFC). 7-Benzyloxy-4-(trifluoromethyl)coumarin is used for rapid CYP isoform metabolism and inhibition screening studies .

HY-132866

YS-370	P-glycoprotein	Cancer
YS-370 (compound 44) is a potent, high selective, and orally active inhibitor of P-glycoprotein (P-gp). YS-370 stimulates the P-gp ATPase activity and has moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity .

HY-18569AR

3-Indoleacetic acid sodium (Standard) Indole-3-acetic acid sodium (Standard); 3-IAA sodium (Standard)	Reference Standards Endogenous Metabolite	Metabolic Disease
Ginsenoside F1 (Standard) is the analytical standard of Ginsenoside F1. This product is intended for research and analytical applications. Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.

HY-W140208

3-Phenylthiophene	Cytochrome P450	Neurological Disease
3-Phenylthiophene (Compound 25) is a CYP2A6 inhibitor with a K_i value of 3.3 μM. The K_i values for CYP2E1, CYP2B6, CYP2C9, and CYP2C19 are 9.7, 14, 112, and 107 μM respectively. It shows no significant inhibition on CYP3A4 and CYP2D6. 3-Phenylthiophene can be used in smoking cessation research .

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-N0598R

Ginsenoside F1 (Standard) 20(S)-Ginsenoside F1 (Standard)	Reference Standards Cytochrome P450 Endogenous Metabolite	Cancer
Ginsenoside F1 (Standard) is the analytical standard of Ginsenoside F1. This product is intended for research and analytical applications. Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.

HY-10779

BMS-344577	Factor Xa Cytochrome P450	Cardiovascular Disease
BMS-344577 (Compound 22) is a potent and orally active factor Xa inhibitor (IC₅₀ = 4 nM, EC2xPT = 7 μM). BMS-344577 shows potent *CYP3A4* inhibition activity (IC₅₀ = 0.3 μM). BMS-344577 can be used for the research of cardiovascular disease .

HY-130609

Aβ42-IN-1	γ-secretase	Neurological Disease
Aβ42-IN-1, compound 1v, is a novel, potent and orally active?γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC₅₀?value of 0.091?μM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.

HY-180955

Desfluoro-BMS-694153	CGRP Receptor Cytochrome P450	Neurological Disease
Desfluoro-BMS-694153 (Compound 3) is a calcitonin gene-related peptide receptor (CGRP receptor) antagonist, with a K_i value of 0.01 nM. Desfluoro-BMS-694153 has a significantly reduced risk of *CYP3A4* inhibition, and its IC₅₀ values for CYP3A4-BFC and CYP3A4-BZR are 36 and 6 μM respectively. Desfluoro-BMS-694153 can be used for research on migraines .

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-16641

JAK1-IN-17	JAK	Cancer
JAK1-IN-17 (Compound 31) is a highly selective inhibitor of JAK1 with a K_i of 1.9 nM. JAK1-IN-17 exhibits a low whole blood shift, which allows maintaining good whole blood potency. JAK1-IN-17 is also a nitrile-containing analogue with consistent, yet weak reversible inhibition of CYP3A4 using a midazolam probe (IC₅₀ = 7.9 μM). JAK1-IN-17 can be studied in cancer research .

HY-19397

BMS-223131	Potassium Channel Cytochrome P450	Neurological Disease
BMS-223131 (Compound 1) is a potent maxi-K potassium channel opener. BMS-223131 has a strong inhibitory effect on the CYP2C9 enzyme (IC₅₀ = 1.7 μM) and also shows varying degrees of inhibition on other common CYP enzymes such as CYP1A2, CYP2C19, CYP2D6, and CYP3A4. BMS-223131 can enhance the outward current mediated by maxi-K, by promoting K ⁺ efflux to hyperpolarize the cell membrane and reducing Ca ²⁺ influx. BMS-223131 can be used for the research of neurological disease, such as stroke .

HY-175064

3,4-Methylenedioxyphenmetrazine hydrochloride 3,4-MDPM hydrochloride	Cytochrome P450	Neurological Disease
3,4-Methylenedioxyphenmetrazine (3,4-MDPM) hydrochloride is a psychoactive substance. 3,4-Methylenedioxyphenmetrazine exhibits strong CYP2D6 inhibition and moderate inhibition of *CYP3A4* and CYP1A2 .

HY-121698

GW694481	Cytochrome P450	Inflammation/Immunology
GW694481 is an ApoA1 upregulator with IC₅₀ values of 2.1 μM for CYP2C9 inhibition and 17.0 μM for *CYP3A4* inhibition. GW694481 upregulates ApoA1 expression in human hepatic cells.GW694481 can be used for the research of atherosclerosis .

HY-123965

PF-06745013	MAP4K TNF Receptor	Metabolic Disease Cancer
PF-06745013 (Compound 37) is a MAP4K4 inhibitor without time-dependent inhibition (TDI) risk of CYP3A4 (IC₅₀ of 0.4  nM for MAP4K4). PF-06745013 has no accumulation CNS-impaired and non-ATP competitive activities in mouse models. PF-06745013 can be used for inflammatory diseases like diabetes and cancers research .

HY-182761

Antiviral agent 81	DNA/RNA Synthesis Cytochrome P450 Flavivirus Influenza Virus	Infection
Antiviral agent 81 is an orally bioavailable N-acylated remdesivir derivative and RdRp inhibitor with 45.3% oral bioavailability (based on active metabolite GS-441524 exposure), plasma half-life >8 h, and reduced *CYP3A4* inhibition. Antiviral agent 81 exhibits activity against Coronaviridae, Flaviviridae, and Pneumoviridae, and shows no activity against Orthomyxoviridae, Herpesviridae, and Alphaviridae. Antiviral agent 81 can be used for the research of viral infections .

HY-175804

M2 ion channel blocker-2	SARS-CoV	Infection
M2 ion channel blocker-2 (Compound 10) is a M2 channel blocker. M2 ion channel blocker-2 significantly blocks wild-type and mutant M2 (L27F and V27A) ion channels. M2 ion channel blocker-2 has potent antiviral activity against HCoV-229E (EC₅₀: 4.7  μM in cytopathic effect) but not against influenza A virus. M2 ion channel blocker-2 has no significant inhibition of hERG and cytochrome P450 (CYP1A2, CYP2C19, and CYP3A4) activity .

HY-W663179

DNDI-VL-2098	Parasite Cytochrome P450	Infection
DNDI-VL-2098 is an orally active antileishmanial agent. DNDI-VL-2098 exhibits high permeability, in vitro metabolic stability, and selective inhibition of CYP2C19 (IC₅₀=0.47 μM). DNDI-VL-2098 does not affect the activities of other major CYP enzymes (CYP1A2, CYP2C9, CYP2D6 and CYP3A4) at concentrations up to 12.5 μM. It shows favorable pharmacokinetic properties in multiple animal models including mice, hamsters, rats and dogs. DNDI-VL-2098 is characterized by moderate to high plasma protein binding and can be used for the research of visceral leishmaniasis .

HY-16265A

JI-101 hydrochloride	Ephrin Receptor PDGFR VEGFR	Cancer
JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity .JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis .JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of *CYP3A4*, and shows stability in pre-clinical and human liver microsomes .JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route .JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors .

HY-181662

DLK-IN-2	MAP3K	Neurological Disease
DLK-IN-2 is a selective inhibitor of DLK and neuroprotective agent. DLK-IN-2 shows no significant inhibition against CYPs 3A4, 2D6 and 2C9. DLK-IN-2 inhibits acute axonal palmitoylation of DLK, blocks DLK-dependent pro-degenerative axon-to-soma retrograde signaling and suppresses c-Jun phosphorylation. DLK-IN-2 can be used for the mechanistic study of neurodegenerative diseases .

Cat. No.	Product Name

HY-L922

Good ADMET Diversity Library	25000 compounds
A diverse compound library with favorable ADMET properties (Absorption, Distribution, Metabolism, Excretion, and Toxicity) is crucial in drug discovery. Early evaluation of ADMET properties allows for the exclusion of molecules with unfavorable profiles at the initial stages, thereby reducing the risk of late-stage development failures, lowering R&D costs, and accelerating optimization of lead compounds. Based on predictions from ADMET-related AI algorithms, the compounds in this library are predicted to exhibit favorable oral bioavailability (F > 30%), reasonable plasma protein binding (PPB < 98%), minimized CYP3A4 inhibition potential (inhibition probability < 50%, CYP3A4 is the most critical drug-metabolizing enzyme in the cytochrome P450 family) , low toxicity profiles, with 140 potentially toxic substructures pre-identified and excluded via substructure searching to eliminate compounds containing hazardous fragments. The diversity library enables broad applicability in high-throughput screening (HTS) and high-content screening (HCS).

Good ADMET Diversity Library

25000 compounds

A diverse compound library with favorable ADMET properties (Absorption, Distribution, Metabolism, Excretion, and Toxicity) is crucial in drug discovery. Early evaluation of ADMET properties allows for the exclusion of molecules with unfavorable profiles at the initial stages, thereby reducing the risk of late-stage development failures, lowering R&D costs, and accelerating optimization of lead compounds. Based on predictions from ADMET-related AI algorithms, the compounds in this library are predicted to exhibit favorable oral bioavailability (F > 30%), reasonable plasma protein binding (PPB < 98%), minimized CYP3A4 inhibition potential (inhibition probability < 50%, CYP3A4 is the most critical drug-metabolizing enzyme in the cytochrome P450 family) , low toxicity profiles, with 140 potentially toxic substructures pre-identified and excluded via substructure searching to eliminate compounds containing hazardous fragments. The diversity library enables broad applicability in high-throughput screening (HTS) and high-content screening (HCS).

Ginsenoside F1 1 Publications Verification 20(S)-Ginsenoside F1	Panax ginseng C. A. Meyer Triterpenes Classification of Application Fields Terpenoids Plants Endogenous metabolite Disease Research Fields Araliaceae Source Classification 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.

3-Indoleacetic acid sodium (Standard) Indole-3-acetic acid sodium (Standard); 3-IAA sodium (Standard)	Structural Classification Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Reference Standards Endogenous Metabolite
Ginsenoside F1 (Standard) is the analytical standard of Ginsenoside F1. This product is intended for research and analytical applications. Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.

Ginsenoside F1 (Standard) 20(S)-Ginsenoside F1 (Standard)	Panax ginseng C. A. Meyer Triterpenes Structural Classification Terpenoids Plants Endogenous metabolite Araliaceae Source Classification	Reference Standards Cytochrome P450 Endogenous Metabolite
Ginsenoside F1 (Standard) is the analytical standard of Ginsenoside F1. This product is intended for research and analytical applications. Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.

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