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Results for "

efflux transporter

" in MedChemExpress (MCE) Product Catalog:

32

Inhibitors & Agonists

1

Screening Libraries

1

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1

Biochemical Assay Reagents

8

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Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-50879
    Elacridar
    Maximum Cited Publications
    31 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-B0193A
    Prazosin hydrochloride
    15+ 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-50880
    Elacridar hydrochloride
    Maximum Cited Publications
    31 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-132301
    MSC-4381

    MCT4-IN-1

    		 Monocarboxylate Transporter Cancer
    MSC-4381 (MCT4-IN-1), a chemical probe, 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-D0180
    18-Crown-6-ether

    18C6; 1,4,7,10,13,16-Hexaoxacyclooctadecane

    		 Bacterial Infection
    18-Crown-6-ether is a type of crown ether compound and a specific structure dissociating agent. 18-Crown-6-ether can compete with K + for binding to G-quadruplexes, disrupting their stable structure to regulate the functions of related systems. 18-Crown-6-ether combines with K + and other metal ions to achieve precise ion transmembrane transport. 18-Crown-6-ether can act as an "susceptibility substrate" for the multi-drug efflux pump EmrE (a bacterial multidrug resistance transporter), ultimately inhibiting bacterial growth. 18-Crown-6-ether can be used in microcapsule controlled release and the research on developing antibacterial enhancers .
    18-Crown-6-ether
  • HY-N0468
    Rebaudioside D
    1 Publications Verification

    		 FXR Acetyl-CoA Carboxylase Metabolic Disease
    Rebaudioside D is an orally active sweetener that targets and activates FXR, modulates Acetyl-CoA Carboxylase, and inhibits 3-hydroxy-3-methylglutaryl-CoA reductase. Rebaudioside D regulates bile acid homeostasis and lipid metabolism, reduces the synthesis rates of fatty acids and cholesterol, and exerts multiple effects including anti-adipogenesis, hepatoprotection, anti-steatosis, gut microbiota modulation, enhancement of secondary bile acid metabolism, anti-endotoxin activity, regulation of bile acid transport, and inhibition of bile acid efflux. Rebaudioside D also reduces body weight gain, visceral fat accumulation, hepatic triglyceride and cholesterol accumulation, hepatic lipid peroxidation, and decreases the circulating level of lipopolysaccharide-binding protein. Rebaudioside D additionally enhances the secondary bile acid metabolic pathway of intestinal bacteria, upregulates the gene expression of ileal organic solute transporter α, and downregulates the gene expression of hepatic bile salt export pump. Rebaudioside D does not affect glucose homeostasis, alter total caloric intake or fecal energy excretion, induce weight gain, exacerbate obesity, promote hepatic steatosis, impair brown adipose tissue function, nor change skeletal muscle metabolism-related proteins. Rebaudioside D can be used in diet-induced obesity and obesity-related research .
    Rebaudioside D
  • HY-B0501
    Danofloxacin mesylate

    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-13451
    Finafloxacin
    1 Publications Verification

    		 Antibiotic Bacterial Infection
    Finafloxacin is an orally active fourth-generation fluoroquinolone broad-spectrum antibiotic. Finafloxacin exhibits stronger antibacterial activity in acidic pH environments and is not easily affected by bacterial multidrug efflux transporters. Finafloxacin is effective against a variety of extracellular pathogenic bacteria, and can also accumulate in macrophages, showing excellent antibacterial activity against intracellular Staphylococcus aureus, Listeria monocytogenes, Legionella pneumophila, Burkholderia pseudomallei, and other pathogens. Finafloxacin has been approved by the U.S. FDA for research on acute otitis externa mediated by Pseudomonas aeruginosa. Finafloxacin is also used in studies related to diseases such as melioidosis, inhalational tularemia, and inhalational plague .
    Finafloxacin
  • 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-117203A
    CDK12-IN-E9
    1 Publications Verification

    		 CDK Cancer
    CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM .
    CDK12-IN-E9
  • HY-W014118
    α-Hexylcinnamaldehyde

    		Environmental Pollutants Inflammation/Immunology Cancer
    α-Hexylcinnamaldehyde is an O-acetyltransferase (OAT) inhibitor. α-Hexylcinnamaldehyde inhibits OAT-mediated bioactivation of nitroarene mutagens, exerts antimutagenic activity through demutagenic and bioantimutagenic mechanisms, and interferes with ATP-binding cassette (ABC) transporter function to reduce substrate efflux. α-Hexylcinnamaldehyde alters membrane permeability, fluidizes phospholipid membranes, exerts antioxidant effects, and enhances the antiproliferative effect of Doxorubicin on human cancer cells. α-Hexylcinnamaldehyde can be used in the research of colorectal adenocarcinoma, T-cell leukemia, and multidrug-resistant cancers .
    α-Hexylcinnamaldehyde
  • HY-N0406
    2"-O-beta-L-galactopyranosylorientin

    		P-glycoprotein 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-50879R
    Elacridar (Standard)

    GF120918 (Standard); GW0918 (Standard); GG918 (Standard); GW120918 (Standard)

    		 P-glycoprotein BCRP Reference Standards 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-161246
    uPSEM792

    		5-HT Receptor 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-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-156807
    LY 367265

    		Serotonin Transporter 5-HT Receptor Neurological Disease
    LY 367265 is a 5-hydroxytryptamine transporter (SERT) inhibitor (IC₅₀ = 3.1 nM) and a 5-HT₂A receptor antagonist (Kᵢ = 0.81 nM). LY 367265 has the inhibitory activity on the norepinephrine transporter (NET) of extremely weak (IC₅₀ > 1000 nM); it has low affinity for subtypes such as 5-HT₁B (Kᵢ = 490 nM) and 5-HT₁D (Kᵢ = 81 nM), showing high selectivity. LY 367265 concentration-dependently enhances of [³H]5-HT efflux (EC₅₀ = 250 nM). LY 367265 antagonizes the contraction response of Sumatriptan (HY-B0121B), indicating its functional antagonistic activity on 5-HT₁D-like receptors. LY 367265 can be used for the study of diseases such as anxiety disorders and post-traumatic stress disorder .
    LY 367265
  • HY-100390
    (S)-ML753286

    		BCRP Cancer
    (S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
    (S)-ML753286
  • HY-N0468R
    Rebaudioside D (Standard)

    		Reference Standards Acetyl-CoA Carboxylase FXR Metabolic Disease
    Rebaudioside D (Standard) is the analytical standard of Rebaudioside D. This product is intended for research and analytical applications. Rebaudioside D is an orally active sweetener that targets and activates FXR, modulates Acetyl-CoA Carboxylase, and inhibits 3-hydroxy-3-methylglutaryl-CoA reductase. Rebaudioside D regulates bile acid homeostasis and lipid metabolism, reduces the synthesis rates of fatty acids and cholesterol, and exerts multiple effects including anti-adipogenesis, hepatoprotection, anti-steatosis, gut microbiota modulation, enhancement of secondary bile acid metabolism, anti-endotoxin activity, regulation of bile acid transport, and inhibition of bile acid efflux. Rebaudioside D also reduces body weight gain, visceral fat accumulation, hepatic triglyceride and cholesterol accumulation, hepatic lipid peroxidation, and decreases the circulating level of lipopolysaccharide-binding protein. Rebaudioside D additionally enhances the secondary bile acid metabolic pathway of intestinal bacteria, upregulates the gene expression of ileal organic solute transporter α, and downregulates the gene expression of hepatic bile salt export pump. Rebaudioside D does not affect glucose homeostasis, alter total caloric intake or fecal energy excretion, induce weight gain, exacerbate obesity, promote hepatic steatosis, impair brown adipose tissue function, nor change skeletal muscle metabolism-related proteins. Rebaudioside D can be used in diet-induced obesity and obesity-related research .
    Rebaudioside D (Standard)
  • 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) .
    P-gp/BCRP-IN-1
  • HY-163473
    IITR08367

    		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-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-50880R
    Elacridar hydrochloride (Standard)

    GF120918A (Standard)

    		 P-glycoprotein BCRP Reference Standards 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-B0501R
    Danofloxacin mesylate (Standard)

    CP 76136-27 (Standard)

    		 Reference Standards 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-162714
    C3N-Dbn-Trp2

    		P-glycoprotein Cancer
    C3N-Dbn-Trp2 is an inhibitor for ATP-binding cassette transporter ABCB1. C3N-Dbn-Trp2 inhibits the ABCB1-mediated Rhodamine 123 (HY-D0816) efflux in cells HEK293T and HCT-15 with IC50 of 5.9 µM and 2.2 µM. C3N-Dbn-Trp2 inhibits the Doxorubicin (HY-15142A) efflux, enhances the cytotoxicity of Doxorubicin in ABCB1-expressing cells .
    C3N-Dbn-Trp2
  • HY-N0406R
    2"-O-beta-L-galactopyranosylorientin (Standard)

    		Reference Standards Others Inflammation/Immunology
    2"-O-beta-L-galactopyranosylorientin (Standard) is the analytical standard of 2"-O-beta-L-galactopyranosylorientin. This product is intended for research and analytical applications. 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-115780
    E17110

    		LXR ATP-binding cassette (ABC) transporters Cardiovascular Disease
    E17110 is a liver X receptor β (LXRβ) agonist with an EC50 of 0.72 μM. E17110 can increase the expression of ATP-binding cassette transporter A1 (ABCA1) and G1 (ABCG1) in RAW264.7 macrophages. E17110 also reduce cellular lipid accumulation and promoted cholesterol efflux. E17110 can be used for the research of cardiovascular disease, such as atherosclerosis .
    E17110
  • HY-B0193AR
    Prazosin hydrochloride (Standard)

    		Reference Standards Adrenergic Receptor Autophagy Cardiovascular Disease Endocrinology Cancer
    Prazosin (hydrochloride) (Standard) is the analytical standard of Prazosin (hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • HY-W014118R
    α-Hexylcinnamaldehyde (Standard)

    		Reference Standards Environmental Pollutants Cancer
    α-Hexylcinnamaldehyde (Standard) is the analytical standard of α-Hexylcinnamaldehyde. This product is intended for research and analytical applications. α-Hexylcinnamaldehyde is an O-acetyltransferase (OAT) inhibitor. α-Hexylcinnamaldehyde inhibits OAT-mediated bioactivation of nitroarene mutagens, exerts antimutagenic activity through demutagenic and bioantimutagenic mechanisms, and interferes with ATP-binding cassette (ABC) transporter function to reduce substrate efflux. α-Hexylcinnamaldehyde alters membrane permeability, fluidizes phospholipid membranes, exerts antioxidant effects, and enhances the antiproliferative effect of Doxorubicin on human cancer cells. α-Hexylcinnamaldehyde can be used in the research of colorectal adenocarcinoma, T-cell leukemia, and multidrug-resistant cancers .
    α-Hexylcinnamaldehyde (Standard)
  • HY-100390R
    (S)-ML753286 (Standard)

    		BCRP Reference Standards Cancer
    (S)-ML753286 (Standard) is the analytical standard of (S)-ML753286 (HY-100390). This product is intended for research and analytical applications. (S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
    (S)-ML753286 (Standard)
  • HY-D3179
    CDg13

    		Fluorescent Dye BCRP Neurological Disease
    CDg13 is a fluorescent probe that specifically detects living neural stem/progenitor cells. CDg13 localizes to the endoplasmic reticulum via its dihexyl moiety, with no interaction with endoplasmic reticulum biomolecules. CDg13 undergoes selective efflux by active ABCG2 transporters, with increased intracellular accumulation following ABCG2 inhibition or knockdown. CDg13 isolates and enriches self-renewable neural stem/progenitor cells from embryonic mouse brain tissue, stains neural stem/progenitor cells brightly, and sorts ABCG2low cell populations from heterogeneous populations . (Ex/Em = 520/553 nm)
    CDg13
  • HY-182448
    TDI-11904

    		Histone Methyltransferase Cancer
    TDI-11904 is a peripherally active EZH2 inhibitor with an EZH2 IC50 of 0.9 nM. TDI-11904 inhibits EZH2 methyltransferase activity, reduces the trimethylation level of H3K27me3, and decreases intracellular H3K27me3 content. TDI-11904 inhibits the proliferation of lymphoma cells. TDI-11904 can be used for the research of lymphoma .
    TDI-11904
  • HY-179683
    MRP1-IN-2

    		P-glycoprotein Cancer
    MRP1-IN-2 (Compound 21) is a selective MRP1 inhibitor with a relatively weak inhibitory effect on P-gp. MRP1-IN-2 exhibits a strong accumulation effect of calcein, with its EC50 value being 177 nM. MRP1-IN-2 enhances the activity of Doxorubicin (HY-15142A) on drug-resistant cells. MRP1-IN-2 can be used for the study of multidrug-resistant cancers .
    MRP1-IN-2

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