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efflux activity

" in MedChemExpress (MCE) Product Catalog:

38

Inhibitors & Agonists

2

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1

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2

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8

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Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-Y1777

    Drug Derivative Infection
    2-Phenylacetophenone has broad-spectrum efflux pump inhibition activity. 2-Phenylacetophenone is a benzoin derivative used as a photoinitiator in vinyl polymerization .
    2-Phenylacetophenone
  • HY-P10551

    Transmembrane Glycoprotein NF-κB TNF Receptor Cardiovascular Disease
    Apo A-I mimetic 5A peptide is a synthetic peptide molecule designed based on the structure and function of naturally occurring apolipoprotein A-I (Apo A-I). Apo A-I mimetic 5A peptide can promote the efflux of cholesterol from cells and help reduce the accumulation of cholesterol in cells. Apo A-I mimetic 5A peptide also shows anti-inflammatory activity and can reduce inflammatory markers in blood and tissues. Apo A-I mimetic 5A peptide can be used in the study of cardiovascular diseases .
    Apo A-I mimetic 5A peptide
  • HY-P10874

    Bacterial Infection
    SMR efflux inhibitor targets the small multidrug resistance (SMR) efflux pump, blocks the interaction of TM4-TM4, and exhibits board-spectrum antibacterial activity .
    SMR efflux inhibitor
  • HY-13766A

    VX-853-2

    Bacterial Others
    Timcodar mesylate (VX-853-2) and its analog VX-710 are mammalian multidrug-resistant bacterial efflux pump inhibitors that directly inhibit ethidium bromide efflux in Staphylococcus aureus. Timcodar mesylate has the potential to enhance antibiotic activity by inhibiting bacterial efflux pumps, effectively reducing the minimum inhibitory concentration of some antibiotics against Gram-positive pathogens such as Staphylococcus aureus, Enterococcus and Streptococcus pneumoniae .
    Timcodar mesylate
  • HY-124819

    Bacterial Infection
    D13-9001 is a potent AcrB (AcrAB-TolC efflux pump subunit) and MexB (MexAB-OprM efflux pump subunit) inhibitor with the KD values of 1.15 μM and 3.57 μM in E. coli and P. aeruginosa, respectively . D13-9001 exhibits antibiotic activities .
    D13-9001
  • HY-163454

    Bacterial Infection
    NorA-IN-2 (compound DZ-3) is a potent NorA inhibitor. NorA-IN-2 shows NorA efflux pump inhibitors (EPI) activity .
    NorA-IN-2
  • HY-N9947

    Bacterial Antibiotic Infection
    Methyl-6-gingerol is an antimicrobial agent derived from Aframomum melegueta that exhibits anti-mycobacterial activity by inhibiting the efflux of toxins within Mycobacterium species .
    Methyl-6-gingerol
  • HY-N12171

    Bacterial Infection Neurological Disease
    Isoreserpiline is an orally active and BBB-penatrable indole alkaloids with antibacterial and antipsychotic activity. Isoreserpiline is even more effective when used in combination with antibiotics and inhibits the activity of bacterial efflux pumps. Isoreserpiline improves Amphetamine-induced hyperactivity in mice .
    Isoreserpiline
  • HY-163473

    Bacterial Infection
    IITR08367 is a potent effector pump Acinetobacter baumannii Fosfomycin Efflux pump (AbaF) inhibitor for enhancing the antimicrobial activity of Fosfomycin (HY-B1075A) against Acinetobacter baumannii. IITR08367 acts by interfering with Fosfomycin/H + reverse transporter activity. .
    IITR08367
  • HY-146067

    Fungal Reactive Oxygen Species Infection
    β-Nor-lapachone is a Candida glabrata antibiofilm agent. β-Nor-lapachone can stimulate ROS production, inhibits efflux activity, adhesion, biofilm formation and the metabolism of mature biofilms of Candida glabrata. β-Nor-lapachone has antifungal activity .
    β-Nor-lapachone
  • HY-B0501

    CP 76136-27

    P-glycoprotein Bacterial Antibiotic Infection
    Danofloxacin mesylate (CP 76136-27) is a fluoroquinolone used as a veterinary drug. Danofloxacin mesylate has a broad spectrum of bactericidal activity, mainly inhibiting the DNA cycloenzyme of the bacteria. In addition, Danofloxacin mesylate is a substrate for ATP-dependent efflux transporters (P-gp and MRP2) .
    Danofloxacin mesylate
  • HY-14942

    RTA 744 free base; WP 744 free base; WP 769

    P-glycoprotein Cancer
    Berubicin (RTA 744 free base; WP 744) is a 4'-O-benzyldoxorubicin that inhibits P-gp and MRP1-mediated efflux and has anticancer activity. Berubicin inhibits glioblastoma multiforme (GBM) and exhibits cytotoxicity. Berubicin has poor bioavailability in mice .
    Berubicin
  • HY-17390A

    5-HT Receptor Dopamine Receptor Infection Neurological Disease
    Loxapine succinate is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistant Salmonella enterica serovar Typhimurium in macrophages .
    Loxapine succinate
  • HY-102008

    NVP-PDF 713; VIC-104959

    Bacterial Antibiotic Infection
    LBM-415 (NVP-PDF 713) is a peptide deformylase (PDF) inhibitor that exhibits inhibitory activity against various antimicrobial-resistant gram-positive cocci, with a MIC90 range of 0.12-8 µg/ml. Additionally, inhibiting efflux pump activity can enhance bacterial sensitivity to LBM415, thereby improving its antibacterial efficacy .
    LBM-415
  • HY-162822

    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 .
    P-gp modulator-5
  • HY-117763

    Calcium Channel Others
    A-39355 is a compound that can overcome multidrug resistance and has the activity of reversing multidrug resistance. A-39355 can enhance the cytotoxicity of antitumor compounds in multidrug-resistant cells, increase the accumulation of compounds in cells, inhibit the efflux of compounds, and compared with calcium antagonists, it has no serious hypotensive effect. Its activity may be unrelated to the ability to block calcium transport.
    A-39355
  • HY-120768

    Drug Derivative Others
    A-30312 is a compound that can overcome multidrug resistance and has the activity of reversing multidrug resistance. A-30312 can enhance the cytotoxicity of antitumor compounds in multidrug-resistant cells, increase the accumulation of compounds in cells, inhibit the efflux of compounds, and compared with calcium antagonists, it has no serious hypotensive effect. Its activity may be unrelated to the ability to block calcium transport.
    A-30312
  • HY-161645

    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-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-B0501R

    Bacterial Antibiotic Infection
    Danofloxacin mesylate (Standard) is the analytical standard of Danofloxacin mesylate. This product is intended for research and analytical applications. Danofloxacin mesylate (CP 76136-27) is a fluoroquinolone used as a veterinary drug. Danofloxacin mesylate has a broad spectrum of bactericidal activity, mainly inhibiting the DNA cycloenzyme of the bacteria. In addition, Danofloxacin mesylate is a substrate for ATP-dependent efflux transporters (P-gp and MRP2) .
    Danofloxacin (mesylate) (Standard)
  • HY-N12320

    Antibiotic Infection
    Majoranaquinone exhibits a high antibacterial effect against 4 Staphylococcus, 1 Moraxella, and 1 Enterococcus strains. Majoranaquinone shows substantial efflux pump inhibitory activity in Escherichia coliATCC 25922 strain. Majoranaquinone is found to be an effective biofilm formation inhibitor on E.coli, ATCC 25922 and E. coli K-12 AG100 bacteria .
    Majoranaquinone
  • HY-N9947A

    Antibiotic Bacterial Infection
    (rac)-Methyl-6-gingerol (Compound 14) is the racemate of Methyl-6-gingerol (HY-N9947). Methyl-6-gingerol is an antibiotic that can be isolated from Aframomum melegueta. Methyl-6-gingerol exhibits anti-mycobacterial activity by inhibiting the efflux of toxins within Mycobacterium species .
    (rac)-Methyl-6-gingerol
  • HY-108694
    γ-Tocotrienol
    1 Publications Verification

    Endogenous Metabolite NF-κB Metabolic Disease Inflammation/Immunology
    γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment .
    γ-Tocotrienol
  • HY-108694R

    Endogenous Metabolite NF-κB Metabolic Disease Inflammation/Immunology
    γ-Tocotrienol (Standard) is the analytical standard of γ-Tocotrienol. This product is intended for research and analytical applications. γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment .
    γ-Tocotrienol (Standard)
  • HY-W107077

    Bacterial Infection
    INF55 is a NoA multidrug resistance pump inhibitor with the activity of inhibiting the NoA pump. The heterocomplex formed by INF55 combined with berberine shows the potential to combat the resistance of bacterial compounds. INF55 can enhance the antibacterial activity of berberine by reducing its efflux. The structural variants of INF55 can show different NoA inhibitory activities, thereby affecting the antibacterial effect of its corresponding heterocomplexes. Different derivatives of INF55 show similar activity in terms of antibacterial dose and effectiveness .
    INF55
  • HY-130282

    Bacterial Infection
    Ianthelliformisamine C ditrifluoroacetate is an antibiotic enhancer with activity against resistant Gram-negative bacteria. Ianthelliformisamine C ditrifluoroacetate has been shown to improve the efficacy of doxycycline against Pseudomonas aeruginosa. Ianthelliformisamine C ditrifluoroacetate was prepared using peptide coupling, resulting in high chemical yields of 27 to 91%. Ianthelliformisamine C ditrifluoroacetate exhibits its mechanism of action by inducing ATP efflux and causing membrane depolarization in bacterial cells.
    Ianthelliformisamine C ditrifluoroacetate
  • HY-17390AR

    5-HT Receptor Dopamine Receptor Infection Neurological Disease
    Loxapine (succinate) (Standard) is the analytical standard of Loxapine (succinate). This product is intended for research and analytical applications. Loxapine succinate is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistant Salmonella enterica serovar Typhimurium in macrophages .
    Loxapine (succinate) (Standard)
  • HY-155032

    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-156965

    Fluorescent Dye Metabolic Disease Cancer
    BAY-771, a structurally close pyrimidinedione, is a chemical probe with good lead-like properties and high permeability in Caco-2 cells (no hint of efflux). BAY-771 shows very weak inhibitory activity in the BCAT1 biochemical assay and no activity in BCAT2. BAY-771 can be used as a negative control of HY-148242 BAY-069. BAY-771 can be used for the research of tumor metabolism .
    BAY-771
  • HY-168077

    Fungal Infection
    Antibiofilm agent-12 (Compound C13) is an antifungal agent that belongs to the class of carbazate derivatives. Antibiofilm agent-12 exhibits significant antifungal activity against Candida auris, with a MIC90 of 237.9 μM. By inhibiting the drug efflux pump activity of Candida auris and promoting ergosterol depletion, Antibiofilm agent-12 hinders biofilm formation and reduces the metabolic flexibility of Candida auris. Additionally, Antibiofilm agent-12 demonstrates antifungal activity in a Candida auris-infected C. elegans model .
    Antibiofilm agent-12
  • HY-19895

    Bacterial Infection
    DS-8587 is a new fluoroquinolone with significant antibacterial activity. The MIC value of DS-8587 against clinically isolated amoxicillin-resistant Bacillus strains is superior to ciprofloxacin and levofloxacin. The antibacterial activity of DS-8587 is less affected by adeA/adeB/adeC or abeM efflux pumps, and has more advantages than ciprofloxacin. DS-8587 has a lower single-step mutation frequency than ciprofloxacin. DS-8587 may be an effective drug for inhibiting amoxicillin-resistant Bacillus infections .
    DS-8587
  • HY-117931

    Potassium Channel Neurological Disease
    NS004 is a potassium (BK) channel activator that increases Iberiotoxin (HY-P0190) or Tetraethylammonium (HY-B1793)-sensitive whole-cell efflux currents. NS004 also significantly increased the activity of individual GH3 cell BK channels and rat brain BK channels reorganized into planar lipid bilayers, causing an increase in channel mean open time, a decrease in intermittent time, and an increase in channel voltage/calcium sensitivity .
    NS004
  • HY-149360

    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-155198

    Fungal Infection
    Antifungal agent 72 (Compound B8) is a potent antifungal agent. Antifungal agent 72 suppresses the function of efflux pump and down-regulates the resistance-associated genes through blocking the Pdr1-KIX interaction (Ki: 11.7 μM). Antifungal agent 72 is active against Fluconazole (HY-B0101)-resistant with a MIC value of 63 ng/mL, and shows synergistic inhibitory activity with Fluconazole. Antifungal agent 72 can be used for C. glabrata infection research .
    Antifungal agent 72
  • HY-N4314
    Scutellarein tetramethyl ether
    1 Publications Verification

    4',5,6,7-Tetramethoxyflavone

    Bacterial COX NO Synthase NF-κB Infection Inflammation/Immunology Cancer
    Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive compound extracted from Eupatorium odoratum. Scutellarein tetramethyl ether exhibits anti-inflammatory, antibacterial, pro-coagulant, and anti-tumor activities. Scutellarein tetramethyl ether exerts its anti-inflammatory effects by modulating the NF-κB pathway and regulates bacterial resistance through the inhibition of efflux pumps. Additionally, Scutellarein tetramethyl ether accelerates coagulation time via the endogenous coagulation pathway. Studies have shown that Scutellarein tetramethyl ether can effectively inhibit the growth of the liver cancer cell line HepG2 (IC50= 20.08 μg/mL) .
    Scutellarein tetramethyl ether
  • HY-N4314R

    Bacterial COX NO Synthase NF-κB Infection Inflammation/Immunology Cancer
    Scutellarein tetramethyl ether (Standard) is the analytical standard of Scutellarein tetramethyl ether. This product is intended for research and analytical applications. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive compound extracted from Eupatorium odoratum. Scutellarein tetramethyl ether exhibits anti-inflammatory, antibacterial, pro-coagulant, and anti-tumor activities. Scutellarein tetramethyl ether exerts its anti-inflammatory effects by modulating the NF-κB pathway and regulates bacterial resistance through the inhibition of efflux pumps. Additionally, Scutellarein tetramethyl ether accelerates coagulation time via the endogenous coagulation pathway. Studies have shown that Scutellarein tetramethyl ether can effectively inhibit the growth of the liver cancer cell line HepG2 (IC50= 20.08 μg/mL) .
    Scutellarein tetramethyl ether (Standard)
  • HY-124187

    Ethyl pinolenate

    Biochemical Assay Reagents Others
    Pinolenic acid is a polyunsaturated fatty acid found in the seed oils of red pine (Pinus orientalis) and maritime pine (Pinus pinaster). Both oils were found to have lipid-lowering properties. A diet containing marine pine nut oil (MPSO) reduces HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to reduce cholesterol efflux in vitro. Korean pine nut oil supplements may help obesity by reducing appetite. People who take this oil experience an increase in the satiety hormones CCK and GLP-1 and a decrease in appetite. The activity of the oil is attributed to pinolenic acid. Pinolenic acid is not metabolized to arachidonic acid and can reduce the level of arachidonic acid in the phosphatidylinositol fraction of HepG2 cells from 15.9% to 7.0%. Pinolenic acid ethyl ester is a neutral, more lipophilic form of the free acid.
    Pinolenic acid ethyl ester
  • HY-138074

    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

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