Search Result

Results for "

Pgp inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	P-glycoprotein (112) Akt (8) AMPK (1) Amylases (1) Amyloid-β (1) Anaplastic lymphoma kinase (ALK) (1) Angiotensin-converting Enzyme (ACE) (1) Antibiotic (3) Apoptosis (13) Autophagy (4) Bacterial (5) Bcl-2 Family (1) BCRP (9) Beta-secretase (2) c-Met/HGFR (2) Calcium Channel (13) Cannabinoid Receptor (1) Carbonic Anhydrase (1) Caspase (3) CCR (1) CDK (1) COX (1) Cytochrome P450 (18) Dopamine β-hydroxylase (1) Drug Derivative (1) Drug Metabolite (4) EGFR (1) Endogenous Metabolite (9) ERK (2) Ferroptosis (1) Glycosidase (1) HCV Protease (1) Hedgehog (3) HIV (8) HIV Protease (9) IAP (2) Isotope-Labeled Compounds (16) JNK (1) Microtubule/Tubulin (2) Mitochondrial Metabolism (1) mTOR (5) NF-κB (2) NO Synthase (1) p38 MAPK (2) Phosphatase (1) Phosphodiesterase (PDE) (1) PI3K (7) Potassium Channel (2) Reactive Oxygen Species (ROS) (3) Reference Standards (2) ROS Kinase (1) SARS-CoV (8) Serotonin Transporter (4) STAT (1) TAM Receptor (2) Toll-like Receptor (TLR) (4) Topoisomerase (1) Trk Receptor (4) Wee1 (2) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (108) Cardiovascular Disease (20) Infection (14) Inflammation/Immunology (10) Metabolic Disease (11) Neurological Disease (7)

By Targets:

P-glycoprotein (112)

Akt (8)

AMPK (1)

Amylases (1)

Amyloid-β (1)

Anaplastic lymphoma kinase (ALK) (1)

Angiotensin-converting Enzyme (ACE) (1)

Antibiotic (3)

Apoptosis (13)

Autophagy (4)

Bacterial (5)

Bcl-2 Family (1)

BCRP (9)

Beta-secretase (2)

c-Met/HGFR (2)

Calcium Channel (13)

Cannabinoid Receptor (1)

Carbonic Anhydrase (1)

Caspase (3)

CCR (1)

CDK (1)

COX (1)

Cytochrome P450 (18)

Dopamine β-hydroxylase (1)

Drug Derivative (1)

Drug Metabolite (4)

EGFR (1)

Endogenous Metabolite (9)

ERK (2)

Ferroptosis (1)

Glycosidase (1)

HCV Protease (1)

Hedgehog (3)

HIV (8)

HIV Protease (9)

IAP (2)

Isotope-Labeled Compounds (16)

JNK (1)

Microtubule/Tubulin (2)

Mitochondrial Metabolism (1)

mTOR (5)

NF-κB (2)

NO Synthase (1)

p38 MAPK (2)

Phosphatase (1)

Phosphodiesterase (PDE) (1)

PI3K (7)

Potassium Channel (2)

Reactive Oxygen Species (ROS) (3)

Reference Standards (2)

ROS Kinase (1)

SARS-CoV (8)

Serotonin Transporter (4)

STAT (1)

TAM Receptor (2)

Toll-like Receptor (TLR) (4)

Topoisomerase (1)

Trk Receptor (4)

Wee1 (2)

Wnt (1)

β-catenin (1)

By Research Areas:

Cancer (108)

Cardiovascular Disease (20)

Infection (14)

Inflammation/Immunology (10)

Metabolic Disease (11)

Neurological Disease (7)

135

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: P-glycoprotein

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-144366

P-gp inhibitor 3	P-glycoprotein	Cancer
P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel .

HY-155032

P-gp inhibitor 15	P-glycoprotein	Cancer
P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity，and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015)，inhibits tumor progress in nude mice KBV xenograft tumors model .

HY-157483

P-gp inhibitor 18	P-glycoprotein	Cancer
P-gp inhibitor 18 (compound 6G) is a potent inhibitor of *P-gp. P-gp* inhibitor 18 inhibits rhodamine 123 efflux in the P-gp overexpressed leukemia cells, K562/Dox .

HY-161260

P-gp inhibitor 20	P-glycoprotein	Cancer
P-gp inhibitor 20 (compound H27) is a low cytotoxicity P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 20 inhibits the efflux function of P-gp in a dose-dependent manner (without affecting the expression of P-gp), thereby reversing the multidrug resistance (MDR) of MCF-7/ADR cells, with an IC₅₀ value of 46.6 nM. P-gp inhibitor 20 can be used for cancer research .

HY-168008

P-gp inhibitor 25	P-glycoprotein	Cancer
P-gp inhibitor 25 (compound 16c) is a *P-gp* inhibitor. P-gp inhibitor 25 can enhance the oral absorption of paclitaxel (HY-B0015). P-gp inhibitor 25 can be used in anti-cancer research .

HY-162040

P-gp inhibitor 17	P-glycoprotein	Cancer
P-gp inhibitor 17 (compound 2g) is a *P-gp* inhibitor directly interacted with the transmembrane domain of *P-gp. P-gp* inhibitor 17 can be used for P-gp-mediated multidrug-resistant in tumor cells study .

HY-149981

P-gp inhibitor 13	P-glycoprotein	Cancer
P-gp inhibitor 13 is a *P-gp* inhibitor. P-gp inhibitor 13 can reverse P-glycoprotein-mediated paclitaxel resistance in A2780/T cell. P-gp inhibitor 13 can be used for the research of advanced acute myeloid leukemia .

HY-N144114

P-gp inhibitor 2	P-glycoprotein	Cancer
P-gp inhibitor 2 is a potent *P-gp* inhibitor. P-gp inhibitor 2 shows reverse Doxorubicin resistance (IC₅₀=0.22 µM) in P-gp overexpressing human colorectal carcinoma cells (SW600 Ad300) .

HY-149813

P-gp inhibitor 14	P-glycoprotein	Cancer
P-gp inhibitor 14 (Compound 8a) is a high affinity *P-gp* inhibitor. P-gp inhibitor 14 reverses P-gp-mediated multidrug resistance (EC₅₀=48.74 nM). P-gp inhibitor 14 has a weak inhibitory effect on CYP3A4 activity .

HY-159085

P-gp inhibitor 24	P-glycoprotein	Cancer
P-gp inhibitor 24 (Compound 10) is an inhibitor for P-glycoprotein (P-gp)), that inhibits the P-gp mediated fluorescent dye efflux. P-gp inhibitor 24 exhibits multidrug resistance (MDR) reversal effect, enhances the cytotoxicity of Vincristine (HY-N0488) and Etoposide (HY-13629) in cancer cells .

HY-168186

P-gp inhibitor 26	P-glycoprotein	Cancer
P-gp inhibitor 26 (Compound 7i) is a potent *P-gp* inhibitor. P-gp inhibitor 26 potently reverses P-gp-mediated multidrug resistance in K562/A02 cells .

HY-162447

P-gp inhibitor 22	P-glycoprotein Apoptosis	Cancer
P-gp inhibitor 22 is a P-glycoprotein (P-gp) inhibitor that effectively inhibits P-pg and efflux function. P-gp inhibitor 22 induces apoptosis and accumulation of MCF-7/ADR cells processed in the S phase .

HY-173401

P-gp inhibitor 29	P-glycoprotein	Cancer
P-gp inhibitor 29 (41) is a highly potent *P-gp* inhibitor and apoptosis inducer, with an IC₅₀ of 8.9 nM in Eca109/VCR cells. P-gp inhibitor 29 (41) can be used in the research for Esophageal Cancer .

HY-158435

P-gp inhibitor 23	P-glycoprotein Cytochrome P450	Cancer
P-gp inhibitor 23 (compound 14F) is a potent inhibitor of *P-gp* and CYP3A4, with the EC₅₀ and IC₅₀ of 28 nM and 223 nM, respectively .

HY-157330

P-gp inhibitor 16	P-glycoprotein Apoptosis	Cancer
P-gp inhibitor 16 (compound 14) is a p-glycoprotein inhibitor. P-gp inhibitor 16 significantly increases Doxorubicin-induced apoptosis and shows anticancer effects .

HY-150565

P-gp inhibitor 5	P-glycoprotein	Cancer
P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-In ^TM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015) .

HY-157484

P-gp inhibitor 19	P-glycoprotein	Cancer
P-gp inhibitor 19 (Compound 6i) is a P-gp inhibitor. P-gp inhibitor 19 can inhibit the efflux of rhodamine 123 (HY-D0816) in P-gp-overexpressing leukemia cells K562/Dox and also restore the sensitivity of DOX-resistant cells .

HY-168711

P-gp inhibitor 27	P-glycoprotein	Cancer
P-gp inhibitor 27 (Compound D2) is an inhibitor for P-glycoprotein (P-gp), that downregulates the expression of P-gp and MRP1, increases the Rh123 accumulation in A2780/T cell, and reverses multidrug resistance to Paclitaxel (HY-B0015) (EC₅₀ is 88 nM) and Cisplatin (HY-17394) .

HY-162396

P-gp inhibitor 21	P-glycoprotein	Cancer
P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity .

HY-173222

P-gp inhibitor 28	P-glycoprotein	Cancer
P-gp inhibitor 28 (Compound 4h) is an inhibitor targeting P-glycoprotein (P-gp). It can inhibit the proliferation of cancer cells, and its IC₅₀ value for MCF-7/ADR cells is between 15.88 and 21.96 μM. P-gp inhibitor 28 can increase the accumulation of Rho123 in MCF-7/ADR cells and can be used in research related to cancer and overcoming multidrug resistance in tumors .

HY-146391

P-gp inhibitor 4	P-glycoprotein	Cancer
P-gp inhibitor 4 (Compound 8b) is a selective P-glycoprotein modulator with an EC₅₀ of 94 nM. P-gp inhibitor 4 increases agent transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells .

HY-101791

P-gp inhibitor 1	P-glycoprotein	Cancer
P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.

HY-119823

PGP-4008	P-glycoprotein	Cancer
PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple agent resistance (MDR) solid tumor model when given in combination with Doxorubicin .

HY-176193

P-gp modulator-7	P-glycoprotein	Cancer
P-gp modulator-7 (Compound 9e) is a P-glycoprotein (P-gp) inhibitor. P-gp modulator-7 occupies the channel entrance of P-gp with a unique T-shaped configuration, hindering the peristaltic extrusion mechanism of transmembrane domains TM12 and TM9, thereby inhibiting P-gp from pumping drugs out of cells and reversing the multidrug resistance (MDR) of tumor cells. P-gp modulator-7 is promising for research of cancers .

HY-162822

P-gp modulator-5	P-glycoprotein	Cancer
P-gp modulator-5 (compound 25) is a modulator of *P-gp* and can inhibit the proliferation of multidrug resistant (MDR) tumors. P-gp modulator-5 inhibits the activity of drug efflux pumps in MDR cells, leading to a large accumulation of ROS and altered cell cycle profiles .

HY-168953

Lysosomal P-gp targeted agent 1	P-glycoprotein Apoptosis Bcl-2 Family Reactive Oxygen Species (ROS) Caspase	Cancer
Lysosomal P-gp targeted agent 1 (Compound 14) is an anti-tumor agent targeting lysosomal P-glycoprotein (Pgp). Lysosomal P-gp targeted agent 1 is selectively transported into lysosomes by overexpressed Pgp, release nitric oxide (NO) to generate reactive oxygen species (ROS), resulting in lysosomal membrane permeabilization (LMP) and inducing apoptosis. Lysosomal P-gp targeted agent 1 can overcome P-glycoprotein-mediated drug resistance and lead to cell cycle arrest, but relatively low toxicity to normal cells. Lysosomal P-gp targeted agent 1 has antitumor activity, significantly inhibits tumor volume .

HY-161645

P-gp modulator-4	P-glycoprotein	Cancer
P-gp modulator-4 (compound 4c) inhibits the efflux function of P-glycoprotein (P-gp). P-gp modulator-4 shows multidrug resistance (MDR) in cancer reversal activity (IC₅₀ of Paclitaxel (HY-B0015) = 8.80, reversal fold = 211.8) .

HY-19626

NSC23925	P-glycoprotein	Cancer
NSC23925 is a novel, selective and effective P-glycoprotein (Pgp) inhibitor.

HY-162369

PID-9	P-glycoprotein	Cancer
PID-9 is a P-glycoprotein inhibitor. PID-9 has multidrug resistance (MDR) reversal activity (IC₅₀ = 0.1338 μM) and low toxicity. PID-9 inhibits the transport function of P-gp without downregulating P-gp expression .

HY-10550A

Tariquidar methanesulfonate, hydrate 45+ Cited Publications XR9576 methanesulfonate, hydrate	P-glycoprotein	Cancer
Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) is a potent and specific inhibitor of P-glycoprotein (P-gp) with a K_d of 5.1 nM.

HY-149360

P-gb-IN-1	P-glycoprotein	Cancer
P-gb-IN-1 (compound Ⅲ-8), a 2,5-disubstituted furan derivative, is a highly effective, broadspectrum P-glycoprotein (P-gp) inhibitor. P-gb-IN-1 displayed the reversal activity by inhibiting P-gp efflux. P-gb-IN-1 has a potent affinity to P-gp by forming H-bond interactions with residues Asn 721 and Met 986. P-gb-IN-1 possesses broad-spectrum reversal activity and low toxicity in MCF-7/ADR cells .

HY-13646B

Encequidar hydrochloride HM30181 hydrochloride; HM30181A hydrochloride	P-glycoprotein	Others
Encequidar hydrochloride (HM30181 hydrochloride) is an oral P-glycoprotein (P-gp) inhibitor with the activity of enhancing the oral bioavailability of P-gp substrate drugs. Encequidar shows the highest potency among various MDR1 inhibitors, with IC₅₀=0.63nM. Encequidar effectively blocks the transepithelial transport of paclitaxel in MDCK monolayer cells, with IC₅₀=35.4nM .

HY-144393

P-gp/BCRP-IN-1	BCRP	Cancer
P-gp/BCRP-IN-1 (compound 19) is a potential, relatively safe, orally active and efficient efflux transporter (P-gp and BCRP) inhibitor. P-gp/BCRP-IN-1 exerts resistance reversal by inhibiting the efflux function of *P-gp* and BCRP. P-gp/BCRP-IN-1 can overcome the resistance and improve the oral bioavailability of PTX (Paclitaxel) .

HY-149277

FM04	P-glycoprotein	Cancer
FM04 is a potent P-glycoprotein (P-gp) inhibitor (EC₅₀=83 nM). FM04 inhibits P-gp in 2 mechanism: (1)FM04 binds to Q1193, followed by interacting with the functionally critical residues H1195 and T1226; or (2)FM04 binds to I1115 (a functionally critical residue itself), disrupting the R262-Q1081-Q1118 interaction pocket and uncoupling ICL2-NBD2 interaction and thereby inhibiting P-gp .

HY-110377

Tariquidar dihydrochloride XR9576 dihydrochloride	P-glycoprotein	Cancer
Tariquidar dihydrochloride (XR9576 dihydrochloride) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (K_d=5.1 nM) .

HY-10550

Tariquidar 45+ Cited Publications XR9576	P-glycoprotein	Cancer
Tariquidar (XR9576) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (K_d=5.1 nM) .

HY-173162

GPV0057	P-glycoprotein Potassium Channel	Cardiovascular Disease Cancer
GPV0057 (Compound 5d) is a selective and potent P-glycoprotein (P-gp) inhibitor. GPV0057 is also a selective potassium channel K_ir2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of K_ir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, K_ir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome .

HY-163204

RhQ-DMB	P-glycoprotein	Cancer
RhQ-DMB is a potent inhibitor of *P-gp*. RhQ-DMB exhibits high affinity and inhibitory activity in yeast strains expressing CmABCB1 .

HY-100750

Norverapamil hydrochloride 1 Publications Verification (±) -Norverapamil hydrochloride; D591 hydrochloride	Calcium Channel P-glycoprotein Drug Metabolite	Cardiovascular Disease
Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .

HY-135328

Norverapamil (±)-Norverapamil; D591	Calcium Channel P-glycoprotein Drug Metabolite	Cardiovascular Disease
Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .

HY-N1457

Chrysosplenetin	P-glycoprotein Cytochrome P450 Ferroptosis	Metabolic Disease
Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits *P-gp* activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A .

HY-169782

CJZ3	P-glycoprotein	Neurological Disease
CJZ3 is an reversible inhibitor for P-glycoprotein (P-gp), that accumulates the drug (Rh123) in cells, and improve the permeability of the blood-brain barrier (BBB) .

HY-107643

Reversan CBLC4H10	P-glycoprotein	Cancer
Reversan (CBLC4H10) is a potent and nontoxic multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp) inhibitor .

HY-N10563

Coleon-U-quinone	P-glycoprotein	Cancer
Coleon-U-quinone is a potent *P-gp* inhibitor. Coleon-U-quinone can inhibit cancer cells viability and sensitize multidrug resistance cancer cells to Doxorubicin (HY-15142A) .

HY-128685

FD 12-9 Ac12Az9	P-glycoprotein BCRP	Cancer
FD 12-9 is a flavonoid dimer, acts as a dual inhibitor of *P-gp* and BCRP, with EC₅₀s of 285 nM and 0.9 nM, respectively. Anti-glioblastoma activity .

HY-107197

8-Prenylchrysin	P-glycoprotein	Cancer
8-prenylchrysin is a C8-prenylated flavonoid. 8-prenylchrysin inhibits *P-gp*. 8-prenylchrysin can be used for tumor research .

HY-13925

PD0166285 5+ Cited Publications	Wee1 Apoptosis	Cancer
PD0166285, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC₅₀ values of 24 and 72 nM, respectively. PD0166285 exhibits an IC₅₀ of 3.433 μM for Chk1 .

HY-13925A

PD0166285 dihydrochloride	Wee1 Apoptosis	Cancer
PD0166285 dihydrochloride, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC₅₀ values of 24 and 72 nM, respectively. PD0166285 dihydrochloride exhibits an IC₅₀ of 3.433 μM for Chk1 .

HY-129698

MS-073 CP162398	P-glycoprotein	Cancer
MS-073 (CP162398) is a P-glycoprotein (P-gp) inhibitor. MS-073 reverses multidrug resistance in drug-resistant cells by competitively inhibiting drug binding to P-glycoprotein .

HY-N13157

11α-O-Benzoyl-12β-O-acetyltenacigenin B	P-glycoprotein	Cancer
11α-O-Benzoyl-12β-O-acetyltenacigenin B is a P-glycoprotein (Pgp) inhibitor derived from Marsdenia tenacissima and belongs to the Tenacigenin B (HY-N1168) derivatives. 11α-O-Benzoyl-12β-O-acetyltenacigenin B can inhibit multidrug resistance (MDR) caused by P-glycoprotein (Pgp) overexpression in HepG2/Dox cells and holds potential for research in the field of cancer .

Cat. No.	Product Name

HY-L011

Membrane Transporter/Ion Channel Compound Library

1,788 compounds

Most of molecules enter or leave cells mainly via membrane transport proteins, which play important roles in several cellular functions, including cell metabolism, ion homeostasis, signal transduction, the recognition process in the immune system, energy transduction, etc. There are three major types of transport proteins, ATP-powered pumps, channel proteins and transporters. Transport proteins such as channels and transporters play important roles in the maintenance of intracellular homeostasis, and mutations in these transport protein genes have been identified in the pathogenesis of a number of hereditary diseases. In the central nervous system, ion channels have been linked to, but not limited to, many diseases such asataxias, paralyses, epilepsies, and deafness. This indicates the roles of ion channels in the initiation and coordination of movement, sensory perception, and encoding and processing of information. Ion channels are a major class of drug targets in drug development.

MCE designs a unique collection of 1,788 smal-molecule modulators that can be used for the research of Ion Channel and Membrane Transporter or high throughput screening (HTS) related drug discovery.

Cat. No.	Product Name	Target	Research Area

HY-162396

P-gp inhibitor 21	P-glycoprotein	Cancer
P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity .

HY-P10856

CPI1	P-glycoprotein	Cancer
CPI1 is a potent and highly specific multidrug resistance protein 1 (MRP1) inhibitor. CPI1 inhibits MRP1 (K_i: 100 nM) with nanomolar potency but shows minimal inhibition of P-glycoprotein (Pgp). CPI1 and LTC4 compete to bind to the same site of MRP1, inhibiting ATP hydrolysis and substrate transport. CPI1 can be used to study drug delivery and chemotherapy resistance in cancer .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N1457

Chrysosplenetin	Flavonols Structural Classification Piscidia erythrina L. Flavonoids Classification of Application Fields Source classification Phenols Polyphenols Metabolic Disease Plants Compositae Disease Research Fields	P-glycoprotein Cytochrome P450 Ferroptosis
Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits *P-gp* activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A .

HY-N6684

Deoxynivalenol 5+ Cited Publications Vomitoxin	Structural Classification Microorganisms Classification of Application Fields Terpenoids Sesquiterpenes Source classification Metabolic Disease Disease Research Fields	P-glycoprotein
Deoxynivalenol, an orally active mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors .

HY-N4108

Hypophyllanthin	Phyllanthus urinaria Linn. Structural Classification Classification of Application Fields Source classification Lignans Euphorbiaceae Phenylpropanoids Plants Inflammation/Immunology Disease Research Fields	P-glycoprotein
Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity .

HY-N6748

Roquefortine C 1 Publications Verification	Infection Structural Classification Microorganisms Classification of Application Fields Cyclopeptides Source classification Disease Research Fields	P-glycoprotein Cytochrome P450 Bacterial Endogenous Metabolite
Roquefortine C, a fungal cyclopeptide isolated from Penicillium roquefortii, activates *P-gp* and also inhibits P450-3A and other haemoproteins. Roquefortine C has bacteriostatic activities against Gram-positive bacteria .

HY-W009141

1-Monopalmitin Glyceryl palmitate	Source classification Plants	P-glycoprotein IAP PI3K Akt Caspase Apoptosis
1-Monopalmitin (Glyceryl palmitate) is an activator of the PI3K/Akt pathway and an inhibitor of P-glycoprotein (P-gp). 1-Monopalmitin can induce G2/M arrest and caspase-dependent apoptosis in cancer cells, while inhibiting IAPs protein expression. 1-Monopalmitin can increase drug accumulation by inhibiting P-gp activity in intestinal Caco-2 cells. 1-Monopalmitin has the ability to induce protective autophagy and apoptosis of lung cancer cells (IC₅₀=50-58 μg/mL), with low toxicity to normal cells .

HY-N144114

P-gp inhibitor 2	Classification of Application Fields Disease Research Fields Cancer	P-glycoprotein
P-gp inhibitor 2 is a potent *P-gp* inhibitor. P-gp inhibitor 2 shows reverse Doxorubicin resistance (IC₅₀=0.22 µM) in P-gp overexpressing human colorectal carcinoma cells (SW600 Ad300) .

HY-N10563

Coleon-U-quinone	Structural Classification Ketones, Aldehydes, Acids Labiatae Smallanthus uvedalia (Linnaeus) Mackenzie Plants	P-glycoprotein
Coleon-U-quinone is a potent *P-gp* inhibitor. Coleon-U-quinone can inhibit cancer cells viability and sensitize multidrug resistance cancer cells to Doxorubicin (HY-15142A) .

HY-N13157

11α-O-Benzoyl-12β-O-acetyltenacigenin B	Structural Classification Natural Products Marsdenia tenacissima (Roxb.) Moon Source classification Asclepiadaceae Plants	P-glycoprotein
11α-O-Benzoyl-12β-O-acetyltenacigenin B is a P-glycoprotein (Pgp) inhibitor derived from Marsdenia tenacissima and belongs to the Tenacigenin B (HY-N1168) derivatives. 11α-O-Benzoyl-12β-O-acetyltenacigenin B can inhibit multidrug resistance (MDR) caused by P-glycoprotein (Pgp) overexpression in HepG2/Dox cells and holds potential for research in the field of cancer .

HY-N10564

8α,9α-Epoxycoleon-U-quinone	Structural Classification Ketones, Aldehydes, Acids Labiatae Smallanthus uvedalia (Linnaeus) Mackenzie Plants	P-glycoprotein
8α,9α-Epoxycoleon-U-quinone (compound 3) is a p-glycoprotein (P-gp) regulator that is selective for cancer cells (SI=2.0). 8α,9α-Epoxycoleon-U-quinone effectively inhibits *P-gp* activity in NCI-H460/R cells. 8α,9α-Epoxycoleon-U-quinone also reverses the resistance of cancer cells to Doxorubicin (DOX) (HY-15142A) and enhances the anticancer effect of DOX .

HY-N6684R

Deoxynivalenol (Standard)	Structural Classification Microorganisms Terpenoids Sesquiterpenes Source classification	P-glycoprotein
Deoxynivalenol (Standard) is the analytical standard of Deoxynivalenol. This product is intended for research and analytical applications. Deoxynivalenol, an orally active mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors .

HY-N11422R

Mycaminosyltylonolide (Standard)	Structural Classification Microorganisms Antibiotics Source classification Antibacterial Disease Research	Antibiotic Bacterial
Deoxynivalenol (Standard) is the analytical standard of Deoxynivalenol. This product is intended for research and analytical applications. Deoxynivalenol, an orally active mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors .

HY-N4108R

Hypophyllanthin (Standard)	Phyllanthus urinaria Linn. Structural Classification Source classification Lignans Euphorbiaceae Phenylpropanoids Plants	P-glycoprotein
Hypophyllanthin (Standard) is the analytical standard of Hypophyllanthin. This product is intended for research and analytical applications. Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity .

HY-W009141R

1-Monopalmitin (Standard) Glyceryl palmitate (Standard)	Source classification Plants	Reference Standards Apoptosis P-glycoprotein PI3K IAP Caspase Akt
1-Monopalmitin (Glyceryl palmitate) (Standard) is the analytical standard of 1-Monopalmitin (HY-W009141). This product is intended for research and analytical applications. 1-Monopalmitin (Glyceryl palmitate) is an activator of the PI3K/Akt pathway and an inhibitor of P-glycoprotein (P-gp). 1-Monopalmitin can induce G2/M arrest and caspase-dependent apoptosis in cancer cells, while inhibiting IAPs protein expression. 1-Monopalmitin can increase drug accumulation by inhibiting P-gp activity in intestinal Caco-2 cells. 1-Monopalmitin has the ability to induce protective autophagy and apoptosis of lung cancer cells (IC₅₀=50-58 μg/mL), with low toxicity to normal cells .

HY-17367

Atazanavir Maximum Cited Publications 11 Publications Verification BMS-232632	Infection Structural Classification Alkaloids Classification of Application Fields Source classification Pyridine Alkaloids Endogenous metabolite Disease Research Fields Cancer	HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Toll-like Receptor (TLR)
Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL ^pro inhibitor with an IC₅₀ of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .

HY-N3028

Taccalonolide B	Structural Classification Classification of Application Fields Source classification Schizocapsa plantaginea Hance Plants Disease Research Fields Taccaceae Steroids Cancer	Microtubule/Tubulin
Taccalonolide B is microtubule stabilizer isolated from Tacca plantaginea, with antitumor activity. Taccalonolide B is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug-resistance protein (MRP7). Taccalonolide B inhibits growth of SK-OV-3 cells with an IC₅₀ of 208 nM .

HY-17367A

Atazanavir sulfate Maximum Cited Publications 11 Publications Verification BMS-232632 sulfate	Infection Structural Classification Alkaloids Classification of Application Fields Source classification Pyridine Alkaloids Endogenous metabolite Disease Research Fields Cancer	HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Toll-like Receptor (TLR)
Atazanavir (BMS-232632) sulfate is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CL ^pro inhibitor with an IC₅₀ of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .

HY-17367AR

Atazanavir (sulfate) (Standard)	Structural Classification Alkaloids Source classification Pyridine Alkaloids Endogenous metabolite	HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite
Atazanavir (sulfate) (Standard) is the analytical standard of Atazanavir (sulfate). This product is intended for research and analytical applications. Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC₅₀ of 3.49 μM .

HY-17367R

Atazanavir (Standard)	Structural Classification Alkaloids Source classification Pyridine Alkaloids Endogenous metabolite	HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite
Atazanavir (Standard) is the analytical standard of Atazanavir. This product is intended for research and analytical applications. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL ^pro inhibitor with an IC₅₀ of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .

HY-N1941

Isosinensetin	Structural Classification Flavonoids other families Classification of Application Fields Flavones Source classification Plants Inflammation/Immunology Disease Research Fields	P-glycoprotein Bacterial HIV Protease Phosphatase Reactive Oxygen Species (ROS) NF-κB p38 MAPK ERK JNK Calcium Channel
Isosinensetin is a flavonoid compound and an inhibitor of HIV-1 protease and PTP1B (IC₅₀: 2.61 µM; K_i: 0.92 µM). Isosinensetin inhibits P-glycoprotein (P-gp) in MDR1-MDCKII cells. Isosinensetin has multiple activities such as anti-tumor, anti-viral, anti-inflammatory, and antioxidant effects. Isosinensetin can be used in the research of various diseases including cancer, inflammation, osteoporosis, diabetes, etc .

HY-N0217

Benzoylaconine 1 Publications Verification Benzoylaconitine; Isaconitine; Pikraconitin	Alkaloids Structural Classification Classification of Application Fields Other Alkaloids Ranunculaceae Source classification Other Diseases Aconitum carmichaeli Debx. Plants Disease Research Fields	Angiotensin-converting Enzyme (ACE) Reactive Oxygen Species (ROS) Toll-like Receptor (TLR) NF-κB COX NO Synthase p38 MAPK P-glycoprotein
Benzoylaconine (Benzoylaconitine) is an orally active monoester alkaloid found in the traditional Chinese medicine Aconitum carmichaelii. Benzoylaconine is an ACE2 agonist (EC₅₀: 1.5 μM) with antihypertensive and anti-heart failure effects. Benzoylaconine inhibits TLR-induced MAPK and NF-κB pathways to exert anti-inflammatory effects. Benzoylaconine upregulates the protein levels of *P-gp, MRP2*, and has anti-tumor effects .

HY-N6932

Voacamine	Alkaloids Structural Classification other families Classification of Application Fields Source classification Metabolic Disease Plants Disease Research Fields Indole Alkaloids	Cannabinoid Receptor P-glycoprotein PI3K Akt mTOR Apoptosis Autophagy EGFR
Voacamine is an indole alkaloid with cannabinoid 1 (CB1) antagonistic activity. Voacamine can inhibit nuclear translocation. Voacamine is effective in enhancing the effect of Doxorubicin (HY-15142A) as it interferes with the P-glycoprotein (P-gp) function. Voacamine promotes apoptosis-independent autophagic cell death in human osteosarcoma cells. Voacamine activates mitochondrial-associated apoptosis signaling pathway and inhibition of PI3K/Akt/mTOR signaling pathway to suppress breast cancer progression. Voacamine inhibits EGFR to exert oncogenic activity against colorectal cancer .

Cat. No.	Product Name	Chemical Structure

HY-135328AS

Norverapamil-d7 hydrochloride
Norverapamil-d₇ (hydrochloride) is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .

HY-A0064S

Verapamil-d3 hydrochloride

Verapamil-d₃ (hydrochloride) is the deuterium labeled Verapamil hydrochloride. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .

HY-17367S4

Atazanavir-d6

Atazanavir-d₆ is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC₅₀ of 3.49 μM .

HY-135328S

Norverapamil-d7
Norverapamil-d₇ is a deuterium labeled Norverapamil ((±)-Norverapamil). Norverapamil, an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .

HY-W699430

Norverapamil-d6 hydrochloride
Norverapamil-d₆ ((±)-Norverapamil-d₆) hydrochloride is deuterium labeled Norverapamil (hydrochloride). Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .

HY-W716916

Vismodegib-d7
Vismodegib-d₇ is deuterium labeled Vismodegib. Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC₅₀ of 3 nM. Vismodegib also inhibits *P-gp, ABCG2* with IC₅₀ values of 3.0 μM and 1.4 μM, respectively .

HY-W705354

Vismodegib-d4
Vismodegib-d₄ is deuterium labeled Vismodegib. Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC₅₀ of 3 nM. Vismodegib also inhibits *P-gp, ABCG2* with IC₅₀ values of 3.0 μM and 1.4 μM, respectively .

HY-14275S

Verapamil-d3
Verapamil-d₃ ((±)-Verapamil-d₃) is deuterium labeled Verapamil. Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .

HY-14275S2

Verapamil-d6
Verapamil-d₆ ((±)-Verapamil-d₆) is deuterium labeled Verapamil. Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .

HY-14275S1

Verapamil-d7
Verapamil-d₇ is the deuterium labeled Verapamil (HY-14275). Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .

HY-17367S3

Atazanavir-d5

Atazanavir-d₅ is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC₅₀ of 3.49 μM .

HY-17367S2

Atazanavir-d9

Atazanavir-d₉ is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC₅₀ of 3.49 μM .

HY-A0064S1

Verapamil-d6 hydrochloride

Verapamil-d₆ (CP-16533-1-d₆) hydrochloride is the deuterium labled Verapamil (hydrochloride) (HY-A0064). Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .

HY-17367S5

Atazanavir-d24

Atazanavir-d₂₄ (BMS-232632-d₂₄) is deuterium labeled Atazanavir. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL ^pro inhibitor with an IC₅₀ of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .

HY-14794AS

Levomilnacipran-d10 hydrochloride

Levomilnacipran-d₁₀ ((1S,2R)-Milnacipran-d₁₀) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC₅₀ values of 10.5 nM and 19.0 nM, and K_i values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression .

HY-B0168BS

Levomilnacipran-d5 hydrochloride

Levomilnacipran-d5 ((1S,2R)-Milnacipran-d5) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC₅₀ values of 10.5 nM and 19.0 nM, and K_i values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks