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efflux

" in MedChemExpress (MCE) Product Catalog:

104

Inhibitors & Agonists

3

Screening Libraries

1

Fluorescent Dye

3

Biochemical Assay Reagents

8

Peptides

18

Natural
Products

1

Recombinant Proteins

4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-112505

    BCRP Cancer
    Efflux inhibitor-1 (compound 2) is a pyrazolo[1,5-a]pyrimidine efflux inhibitor. Efflux inhibitor-1 selectively targets toward ABCG2/BCRP over ABCB1 with IC50s of 0.45 μM and 2.17 μM, respectively .
    <em>Efflux</em> inhibitor-1
  • HY-149811

    Bacterial Parasite Infection
    Efflux pump-IN-3 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-3 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-3 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
    AcrB-IN-3
  • HY-149812

    Bacterial Parasite Infection
    Efflux pump-IN-4 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-4 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-4 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
    AcrB-IN-4
  • HY-149810

    Bacterial Parasite Infection
    AcrB-IN-2 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. AcrB-IN-22 inhibits Nile Red (a known substrate of AcrB) efflux.AcrB-IN-2 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
    AcrB-IN-2
  • HY-P2576

    Bacterial Infection
    Polistes mastoparan is an antimicrobial peptide. Polistes mastoparan increases S. aureus cell K + efflux and inhibits cell viability with EC50 of 5 μM .
    Polistes mastoparan
  • HY-Y1777

    Others 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-156753

    Others Cancer
    NorA-IN-1 (Compound 16) is a NorA inhibitor. NorA-IN-1 inhibits NorA efflux pump in everted membrane vesicles. NorA-IN-1 can be used for research of multidrug resistance .
    NorA-IN-1
  • HY-N2947

    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-161246

    Others Neurological Disease
    uPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM 4-GlyR, with an affinity of Ki of 0.7 nM. uPSEM792 is a substrate for efflux transporters in brains of wild type and dual P-gp and BCRP knockout mice. uPSEM7952 is a possible lead for developing the PET radioligand for PSAM 4-GlyR .
    uPSEM792
  • HY-128773

    Bacterial Infection
    MRL-494, an antibacterial agent, is a inhibitor of β-barrel assembly machine A (BamA) impervious to efflux and the outer membrane permeability barrier. MRL-494 can inhibits Gram-positive (MIC of 12.5 μM for Staphylococcus aureus COL) and Gram-negative (MIC of 25 μM for E. coli JCM158) bacterias .
    MRL-494
  • HY-128773A

    Bacterial Infection
    MRL-494 hydrochloride, an antibacterial agent, is a inhibitor of β-barrel assembly machine A (BamA) impervious to efflux and the outer membrane permeability barrier. MRL-494 hydrochloride can inhibits Gram-positive (MIC of 12.5 μM for Staphylococcus aureus COL) and Gram-negative (MIC of 25 μM for E. coli JCM158) bacterias .
    MRL-494 hydrochloride
  • HY-144393

    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) .
    P-gp/BCRP-IN-1
  • HY-143792

    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-139665

    Monocarboxylate Transporter Cardiovascular Disease
    VB124 is an orally active, potent, and selective MCT4 inhibitor. VB124 can specifically inhibit lactate efflux with IC50s of 8.6 nM and 19 nM for lactate import and export in MDA-MB-231 cells, respectively. VB124 is highly selective for MCT4 over MCT1. VB124 can be used for the research of cardiac hypertrophy, heart failure, and metabolism .
    VB124
  • HY-122416

    Lonchocarpol A; Senegalensin

    BCRP Metabolic Disease Cancer
    6,8-Diprenylnaringenin (Lonchocarpol A; Senegalensin), a hop prenylflavonoid, is a inhibitor of breast cancer resistance protein (BCRP/ABCG2). 6,8-Diprenylnaringenin inhibits ABCG2-mediated efflux of Mitoxantrone, and 3H-Methotrexate transport (IC50=0.41 μM) in HEK293 cells. 6,8-Diprenylnaringenin exhibits some estrogenicity, but its potency is less than 1% of that of 8-Prenylnaringenin .
    6,8-Diprenylnaringenin
  • HY-132301

    MCT4-IN-1

    Monocarboxylate Transporter Cancer
    MSC-4381 (MCT4-IN-1) is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki of 11 nM. MSC-4381 targets to the cytosolic domain of MCT4. MSC-4381 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MSC-4381 has the potential for MCT4 transporter inhibition research . MSC-4381 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MSC-4381
  • HY-101444A
    PAβN dihydrochloride
    5+ Cited Publications

    MC-207,110 dihydrochloride; Phe-Arg-β-naphthylamide dihydrochloride

    Bacterial Infection
    PAβN dihydrochloride (MC-207110 dihydrochloride) is an efflux pump inhibitor.
    PAβN dihydrochloride
  • HY-B0193A
    Prazosin hydrochloride
    5+ Cited Publications

    Adrenergic Receptor Autophagy Cardiovascular Disease Endocrinology Cancer
    Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders . Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM .Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively .
    Prazosin hydrochloride
  • 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-157533

    Bacterial Others
    AcrB-IN-5 (compound 8) inhibits AcrB and blocks the efflux pump in a dose-dependent manner .
    AcrB-IN-5
  • HY-100390

    (S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
    (S)-ML753286
  • HY-N10075

    P-glycoprotein Others
    Euphohelioscopin A is a diterpenoid can be isolated from the Euphorbia helioscopia L. plant. Euphohelioscopin A weakly inhibits P-glycoprotein-mediated efflux of mitoxantrone .
    Euphohelioscopin A
  • HY-119172

    Bacterial Infection Inflammation/Immunology Cancer
    NSC-60339, an efflux pump inhibitor and a substrate of AcrAB-TolC, is a polybasic terephthalic acid derivative studied as a potential cancer chemotherapeutic agent .
    NSC-60339
  • 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-157987

    Bacterial Infection
    MBX3135 is an efflux pump inhibitor which can enhance the effect of antibiotics through the AcrB target of bacteria. MBX3135 can be used for research of infection and antibiotics .
    MBX3135
  • HY-N3308

    Apoptosis Cancer
    Medicarpin is a flavonoid isolated from Medicago sativa. Medicarpin induces apoptosis and overcome multidrug resistance in leukemia P388 cells by modulating P-gp-mediated efflux of agents .
    Medicarpin
  • HY-112220
    VIT-2763
    1 Publications Verification

    Ferroportin Metabolic Disease
    VIT-2763, an oral ferroportin inhibitor, inhibits hepcidin binding to ferroportin and blocks iron efflux. VIT-2763 has the potential in the treatment of β-thalassemia .
    VIT-2763
  • HY-129279

    Farnesyl Transferase Cancer
    Andrastin A meroterpenoid compound, is a farnesyltransferase inhibitor. Andrastin A inhibits the efflux of anticancer compounds from multidrug-resistant cancer cells. Andrastin A can be isolated from Penicillium species .
    Andrastin A
  • HY-50879
    Elacridar
    Maximum Cited Publications
    24 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-N2419

    Endogenous Metabolite Metabolic Disease
    Erythrodiol is an olive oil component. Erythrodiol promotes Cholesterol efflux (ChE) by selectively inhibiting the degradation of ABCA1 protein. Erythrodiol is a good candidate to be further explored for therapeutic or preventive application in the context of atherosclerosis .
    Erythrodiol
  • HY-129098
    DMHCA
    1 Publications Verification

    LXR Metabolic Disease
    DMHCA, a potent and selective LXR agonist, specifically activates the cholesterol efflux arm of the LXR pathway without stimulating triglyceride synthesis. DMHCA has anti-inflammatory effects and can be used for the research of cholesterol homeostasis diabetes .
    DMHCA
  • HY-163079

    FAP Cancer
    AlF-PD-FAPI has affinity for FAP , with the IC50 of 0.13 nM, and shows a specific uptake, high internalized fraction, and low cellular efflux in vitro. AlF-PD-FAPI can be used as FAP-targeting tracer .
    AlF-PD-FAPI
  • HY-128038

    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-162144

    Bacterial Infection
    BDM91288 is an orally active AcrB efflux pump inhibitor of pyridinium piperazine. BDM91288 can enhance the in vivo efficacy of levofloxacin (HY-B0330) in the treatment of Klebsiella pneumoniae pulmonary infection in mouse models .
    BDM91288
  • HY-157483

    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 .
    P-gp inhibitor 18
  • HY-50880
    Elacridar hydrochloride
    Maximum Cited Publications
    24 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-155048

    Bacterial Infection
    BDM91270 (compound 29) is an E. coli AcrAB-TolC efflux pump inhibitor with an EC90 of 0.6 μM for wild-type E. coli AcrB. BDM91270 can be used in the study of Escherichia coli drug resistance .
    BDM91270
  • HY-D0067
    7ACC1
    5+ Cited Publications

    DEAC; Coumarin D 1421; D 1421

    Monocarboxylate Transporter Cancer
    7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.
    7ACC1
  • HY-P3156

    Fungal Infection
    Syringomycin E is an antifungal cyclic lipodepsinonapeptide. Syringomycin E exhibits growth inhibition of Saccharomyces cerevisiae through interaction with the plasma membrane. Syringomycin E causes K + efflux, Ca 2+ influx, and changes in membrane potential, and is related to channel formation .
    Syringomycin E
  • HY-113365

    4-Cholesten-3-one

    Endogenous Metabolite Metabolic Disease
    Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells .
    Cholestenone
  • HY-D2261

    Fluorescent Dye Metabolic Disease
    BODIPY-cholesterol conjugate-1 (compound 5) is a BODIPY-cholesterol conjugate. BODIPY-cholesterol conjugate-1 is a useful probe for simultaneous visualization of intracellular cholesterol pools and for monitoring cholesterol efflux from cells to extracellular acceptors . (λex 541 nm, λem 615 nm).
    BODIPY-cholesterol conjugate-1
  • HY-N0406

    Others Inflammation/Immunology
    2"-O-beta-L-galactopyranosylorientin is extracted from the flowers of Trollius ledebouri. 2"-O-beta-L-galactopyranosylorientin involves transporter mediated efflux in addition to passive diffusion and is the substrate of multidrug resistance protein 2 (MRP2). Anti-inflammatory effect .
    2
  • HY-126940

    Reactive Oxygen Species 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-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-P2624

    PAK Metabolic Disease
    st-Ht31 is a membrane-permeable peptide inhibitor of protein kinase A (PKA) anchoring. st-Ht31 induces robust cholesterol/phospholipid efflux. st-Ht31 completely reverses foam cell formation and restores the metabolic health of macrophage .
    st-Ht31
  • HY-P5878

    Biochemical Assay Reagents Metabolic Disease
    RG33 Peptide is a diabetes inhibitor that significantly improves glucose clearance in insulin-resistant mice. RG33 Peptide effectively solubilizes lipid vesicles and promotes cholesterol efflux in cultured macrophages. RG33 Peptide is used in research into type 2 diabetes (T2D) .
    RG33 Peptide
  • HY-D2262

    Fluorescent Dye Metabolic Disease
    BODIPY-cholesterol conjugate-2 (compound 6) is a BODIPY-cholesterol conjugate. BODIPY-cholesterol conjugate-2 is a useful probe for simultaneous visualization of intracellular cholesterol pools and for monitoring cholesterol efflux from cells to extracellular acceptors. (λex=589 nm, λem=638 nm) .
    BODIPY-cholesterol conjugate-2
  • HY-14942

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

    Others 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-100928

    YS 035 hydrochloride is a Ca 2+ antagonist on cellular uptake and mitochondrial efflux of calcium ions. YS 035 hydrochloride inhibits Ca 2+ uptake by muscle cells and inhibits Na +/Ca 2+ exchange (Ki=28 µM). YS 035 hydrochloride is a useful tool for research on the mitochondrial Ca 2+ transport .
    YS 035 hydrochloride

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