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Results for "

p-glycoprotein efflux

" in MedChemExpress (MCE) Product Catalog:

42

Inhibitors & Agonists

1

Inhibitory Antibodies

4

Natural
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2

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15134
    ONT-093

    OC 144-093; OC 144093

    		 P-glycoprotein Infection Cancer
    ONT-093 (OC 144-093) is a potent and orally active inhibitor of P-glycoprotein pump. ONT-093 inhibits P-gp-mediated ATPase activity with an IC50 of 0.16 μM. ONT-093 can inhibit drug efflux and increase bioavailability. ONT-093 reverses cancer cells multidrug resistance to chemotherapeutic drugs. ONT-093 can be used for the researches of cancer and infection, such as colon cancer and malarial .
    ONT-093
  • HY-50879
    Elacridar
    Maximum Cited Publications
    30 Publications Verification

    GF120918; GW0918; GG918; GW120918

    		 P-glycoprotein BCRP Cancer
    Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on agent distribution to brain and the research of cancer .
    Elacridar
  • HY-50880
    Elacridar hydrochloride
    Maximum Cited Publications
    30 Publications Verification

    GF120918A

    		 P-glycoprotein BCRP Cancer
    Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on agent distribution to brain and it can be used for the research of cancer .
    Elacridar hydrochloride
  • HY-N2947
    Boeravinone B

    		P-glycoprotein Infection Inflammation/Immunology
    Boeravinone B, a dual inhibitor of NorA bacterial efflux pump of Staphylococcus aureus and human P-Glycoprotein, reduces the biofilm formation and intracellular invasion of bacteria. Boeravinone B act as anti-aging and anti-apoptosis phyto-molecules during oxidative stress .
    Boeravinone B
  • 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 .
    P-gp inhibitor 22
  • HY-143792
    HTT-D3

    		P-glycoprotein Neurological Disease
    HTT-D3 is a potent and orally active huntingtin (HTT) splicing modulator. HTT-D3 acts by promoting the inclusion of a pseudoexon containing a premature termination codon (stop-codon psiExon), leading to HTT mRNA degradation and reduction of HTT levels. HTT-D3 reduces p-glycoprotein (P-gp) efflux, and can be uesd for Huntington's disease research .
    HTT-D3
  • HY-158264
    SNRI-IN-1

    		Serotonin Transporter Endocrinology
    SNRI-IN-1 (Compound 7a) is a dual serotonin and noradrenaline monoamine reuptake inhibitor, P-glycoprotein Efflux Ratio is 20 .
    SNRI-IN-1
  • HY-19446
    UK-371800

    		Phosphodiesterase (PDE) Others
    UK-371800 is a highly selective PDE5 inhibitor (IC50 = 4.2 nM). UK-371800 has good permeability and is not affected by the efflux of P-glycoprotein .
    UK-371800
  • HY-N15297
    Isotenulin

    		P-glycoprotein Cancer
    Isotenulin inhibits the efflux function of P-glycoprotein by stimulation of P-glycoprotein ATPase, thereby overcoming the multidrug resistance (MDR) of cancer cells. Isotenulin exhibits cytotoxicity in multidrug-resistant cancer cell KB-vin and sensitive cancer cell HeLaS3. Isotenulin exhibits synergistic effect with Paclitaxel (HY-B0015), Vinblastine (HY-13780) and Doxorubicin (HY-15142) .
    Isotenulin
  • HY-128038
    N-Desmethyl-loperamide

    		Opioid Receptor Neurological Disease
    N-Desmethyl-loperamide is a major metabolite of loperamide, a drug that selectively activates peripheral μopioid receptors with a Ki value of 0.16 nM. N-Desmethyl-loperamide is a substrate of the ATP-dependent efflux transporter P-glycoprotein .
    N-Desmethyl-loperamide
  • HY-126940
    Furanodiene

    		Reactive Oxygen Species (ROS) P-glycoprotein Apoptosis Cancer
    Furanodiene is a natural terpenoid isolated from Rhizoma Curcumae. Furanodiene plays anti-cancer effects through anti-angiogenesis and inducing ROS production, DNA strand breaks and apoptosis. Furanodiene suppresseed efflux transporter Pgp (P-glycoprotein) function and reduced Pgp protein level .
    Furanodiene
  • HY-50879R
    Elacridar (Standard)

    		P-glycoprotein BCRP Cancer
    Elacridar (Standard) is the analytical standard of Elacridar. This product is intended for research and analytical applications. Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on agent distribution to brain and the research of cancer .
    Elacridar (Standard)
  • HY-W777317
    Elacridar-d4(Major)

    		Isotope-Labeled Compounds P-glycoprotein BCRP Cancer
    Elacridar-d4(Major) is the deuterium labeled Elacridar (HY-50879). Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on agent distribution to brain and the research of cancer .
    Elacridar-d4(Major)
  • HY-174454
    Antitrypanosomal agent 24

    		P-glycoprotein Infection
    Antitrypanosomal agent 24 is a benzothiazole amidoxime with strong and selective antitrypanosomal activity (IC50 = 0.92 μM). Antitrypanosomal agent 24 is a substrate of the P-glycoprotein efflux pump. Antitrypanosomal agent 24 has high membrane permeability and good metabolic stability. Antitrypanosomal agent 24 binds to DNA/RNA by intercalation .
    Antitrypanosomal agent 24
  • 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) .
    P-gp modulator-4
  • 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 .
    P-gp inhibitor 3
  • HY-B0777
    Moxidectin
    1 Publications Verification

    CL301423

    		 Antibiotic BCRP P-glycoprotein Parasite Infection
    Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
    Moxidectin
  • HY-50880R
    Elacridar hydrochloride (Standard)

    		P-glycoprotein BCRP Cancer
    Elacridar (hydrochloride) (Standard) is the analytical standard of Elacridar (hydrochloride). This product is intended for research and analytical applications. Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on agent distribution to brain and it can be used for the research of cancer .
    Elacridar hydrochloride (Standard)
  • 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 .
    P-gp inhibitor 24
  • HY-N2947R
    Boeravinone B (Standard)

    		Reference Standards P-glycoprotein Infection Inflammation/Immunology
    Boeravinone B (Standard) is the analytical standard of Boeravinone B. This product is intended for research and analytical applications. Boeravinone B, a dual inhibitor of NorA bacterial efflux pump of Staphylococcus aureus and human P-Glycoprotein, reduces the biofilm formation and intracellular invasion of bacteria. Boeravinone B act as anti-aging and anti-apoptosis phyto-molecules during oxidative stress .
    Boeravinone B (Standard)
  • HY-144880
    SC209

    3-Aminophenyl Hemiasterlin

    		 ADC Payload Microtubule/Tubulin P-glycoprotein Cancer
    SC209 (3-Aminophenyl Hemiasterlin) is a 3-aminophenyl hemiasterlin derivative that serves as a cytotoxin for ADCs, targeting tubulin. SC209 has reduced potential for drug efflux via P-glycoprotein 1 drug pump compared with other tubulin-targeting payloads. SC209 exhibits antitumor activity and can be used in the synthesis of ADC molecules .
    SC209
  • 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 .
    P-gp inhibitor 15
  • HY-157876
    Anticancer agent 191

    		P-glycoprotein BCRP Cancer
    Anticancer agent 191 (Compound 2) is a derivative of probenecid (HY-B0545). As a cancer cell efflux inhibitor, Anticancer agent 191 is designed to inhibit P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and/or multiple multidrug resistance proteins (MRPs). Anticancer agent 191 increases the accumulation of vinblastine in cancer cells, which is used for cancer research .
    Anticancer agent 191
  • HY-U00244A
    Benzquinamide hydrochloride

    P2647 hydrochloride; BZQ hydrochloride; Benzoquinamide hydrochloride

    		 Adrenergic Receptor Cancer
    Benzquinamide (P2647) is an antiemetic which can bind to the α2A, α2B, and α2C adrenergic receptors (α2-AR) with Ki values of 1,365, 691, and 545 nM, respectively. Benzquinamide also inhibits P-glycoprotein mediated drug efflux and potentiates anticancer agent cytotoxicity in multidrug resistant cells .
    Benzquinamide hydrochloride
  • HY-B0777R
    Moxidectin (Standard)

    CL301423 (Standard)

    		 Antibiotic BCRP P-glycoprotein Parasite Reference Standards Infection
    Moxidectin (Standard) is the analytical standard of Moxidectin. This product is intended for research and analytical applications. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
    Moxidectin (Standard)
  • 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 .
    P-gp inhibitor 20
  • HY-B0777S
    Moxidectin-d3

    CL-301423-d3

    		 Isotope-Labeled Compounds BCRP Parasite Antibiotic P-glycoprotein Infection
    Moxidectin-d3 (CL-301423-d3) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
    Moxidectin-d3
  • HY-17013A
    Dofequidar fumarate
    2 Publications Verification

    MS-209

    		 P-glycoprotein Cancer
    Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar fumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar fumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
    Dofequidar fumarate
  • HY-17013
    Dofequidar
    2 Publications Verification

    MS-209 free base

    		 P-glycoprotein Cancer
    Dofequidar (MS-209 free base) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
    Dofequidar
  • HY-17013D
    Dofequidar sesquifumarate

    MS-209 sesquifumarate

    		 P-glycoprotein Cancer
    Dofequidar (MS-209) sesquifumarate is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar sesquifumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar sesquifumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
    Dofequidar sesquifumarate
  • 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 .
    P-gb-IN-1
  • HY-175838
    P-gp-IN-32

    		P-glycoprotein Cancer
    P-gp-IN-32 is a P-glycoprotein (P-gp) inhibitor. P-gp-IN-32 exhibits low cytotoxicity and potent multidrug resistance (MDR) reversal activity against Doxorubicin (HY-15142A) in MCF7/ADR cells (IC50 = 0.11 μM, reversal fold (RF) = 215.9). P-gp-IN-32 can bind to P-gp directly, induce a conformation change of P-gp and inhibit the efflux function. P-gp-IN-32 can be used for the research of cancer, such as breast cancer .
    P-gp-IN-32
  • HY-17013AR
    Dofequidar fumarate (Standard)

    		P-glycoprotein Cancer
    Dofequidar (fumarate) (Standard) is the analytical standard of Dofequidar (fumarate). This product is intended for research and analytical applications. Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar fumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar fumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
    Dofequidar fumarate (Standard)
  • HY-175522
    P-gp-IN-31

    		P-glycoprotein Apoptosis Cancer
    P-gp-IN-31 is a P-glycoprotein (P-gp) inhibitor with IC50 values of 0.42 μM for KB cells and 0.43 μM for MDR KBvin cells. P-gp-IN-31 can pass P-gp-mediated drug efflux mechanisms and shows collateral sensitivity via P-gp downregulation. P-gp-IN-31 inhibits cell proliferation, induces apoptosis and arrests the cell cycle at G2/M phase. P-gp-IN-31 can be used for the research of cancer, such as multidrug-resistant (MDR) malignancies .
    P-gp-IN-31
  • 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 Kir2.1 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 Kir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, Kir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome .
    GPV0057
  • HY-175206
    P-gp-IN-30

    		P-glycoprotein Cancer
    P-gp-IN-30 (Compound 13) is a P-glycoprotein (P-gp) inhibitor by targeting YB-1. P-gp-IN-30 significantly enhances sensitivity to Paclitaxel by reducing total YB-1 and nucleus YB-1 protein expression, inhibiting the expression and function of downstream P-gp, further suppressing the efflux rate of Paclitaxel. P-gp-IN-30 potently inhibits tumor growth in A549/Taxol xenografts mice model with combination of Paclitaxel (HY-B0015). P-gp-IN-30 can be used for non-small cell lung cancer (NSCLC) research .
    P-gp-IN-30
  • HY-P990196
    Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2)

    		P-glycoprotein Cancer
    Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) is an anti-monkey/human MDR-1/CD243 IgG2a monoclonal antibody. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) can efficiently inhibit P-glycoprotein. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) enhances the inhibitory effect on multidrug resistance (MDR) by suppressing drug efflux. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) can be used for research on cancer .
    Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2)
  • HY-176287
    ARN25657

    		Dopamine Receptor GSK-3 PKA P-glycoprotein Neurological Disease
    ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders .
    ARN25657
  • HY-151517
    SOS1-IN-14

    		SOS1 Ras Cancer
    SOS1-IN-14 is a potent, selective and orally active SOS1 inhibitor with an IC50 value of 3.9 nM. SOS1-IN-14 can be absorbed in the intestine via a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 can be used to research KRAS-mutated cancers. SOS1-IN-14 has better potent tumor suppression than BI-3406 (HY-125817) .
    SOS1-IN-14
  • HY-138074
    Milbemycin A4 oxime

    5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime

    		 Parasite Infection
    Milbemycin A4 oxime (5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime) is a derivative of Milbemycin A4 (HY-126906) and a component of Milbemycin oxime (HY-B0778), both of which have insecticidal and nematicidal activities. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae in naturally infected dogs with D. immitis and inhibits the growth of clinical isolates of Candida glabrata (MIC80=16-32 μg/mL). Milbemycin A4 oxime (2.5 μg/mL) blocks the efflux of Fluconazole (HY-B0101) from clinical isolates of Candida glabrata. Milbemycin A4 oxime enhances doxorubicin-induced cell growth inhibition and increases the intracellular accumulation of doxorubicin and P-glycoprotein substrate Rhodamine 123 (HY-D0816) in doxorubicin-resistant but not sensitive MCF-7 breast cancer cells in a concentration-dependent manner.
    Milbemycin A4 oxime
  • HY-172771
    Multi-target kinase inhibitor 4

    		PI3K DNA-PK P-glycoprotein Cancer
    Multi-target kinase inhibitor 4 (Compound 2) is a PI3K/DNA-PK inhibitor and potent chemosensitizer that can increase the amount of DNA double strand breaks induced by Doxorubicin (HY-15142A). Multi-target kinase inhibitor 4, is an efficient inhibitor of multidrug resistance (MDR) that exhibits inhibitory activity toward P-glycoprotein-mediated drug efflux. Multi-target kinase inhibitor 4 can be loaded into PEG-coated LNPs .
    Multi-target kinase inhibitor 4
  • HY-101453
    Ceefourin 1

    		P-glycoprotein Cancer
    Ceefourin 1 is a potent and highly selective multidrug resistance protein 4 (MRP4) inhibitor. Ceefourin 1 inhibits transport of a broad range of MRP4 substrates, yet is highly selective for MRP4 over other ABC transporters. Ceefourin 1 is a benzothiazol and primarily as a chemosensitizer for high-risk neuroblastoma .
    Ceefourin 1

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