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Results for "

efflux activity

" in MedChemExpress (MCE) Product Catalog:

92

Inhibitors & Agonists

3

Screening Libraries

1

Biochemical Assay Reagents

3

Peptides

22

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Products

4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-107643
    Reversan

    CBLC4H10

    		 P-glycoprotein Cancer
    Reversan (CBLC4H10) inhibits drug efflux mediated by P-glycoprotein (Pgp) and multidrug resistance protein 1 (MRP1), and exhibits oral activity. Reversan shows activity against glioblastoma multiforme and neuroblastoma models .
    Reversan
  • HY-17390A
    Loxapine succinate
    1 Publications Verification

    		 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-171099
    SC-919

    LI-2124

    		 IPK Superfamily Cardiovascular Disease Endocrinology
    SC-919 is an orally active IP6K inhibitor, with an IC50 of < 5.2 nM against IP6K1, < 3.8 nM against IP6K2, and 0.65 nM against IP6K3. By inhibiting the activity of IP6K, SC-919 reduces intracellular IP7 levels, thereby suppressing XPR1-mediated cellular phosphate efflux. SC-919 increases intracellular phosphate and ATP levels while reducing phosphate entry into the bloodstream, thus decreasing plasma phosphate levels. SC-919 can be used in research related to chronic kidney disease and hyperphosphatemia .
    SC-919
  • 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-108694
    γ-Tocotrienol
    4 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 radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment .
    γ-Tocotrienol
  • 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-42034
    Hydroquinine

    Dihydroquinine

    		 Bacterial Parasite Reactive Oxygen Species (ROS) Protein Arginine Deiminase Infection
    Hydroquinine (Dihydroquinine) is an anti-bacterial agent that inhibits both Gram-positive and Gram-negative bacteria. Hydroquinine inhibits the growth of multidrug-resistant pseudomonas aeruginosa via the suppression of the arginine deiminase pathway genes. Hydroquinine inhibits Plasmodium falciparum and Plasmodium berghei. Hydroquinine displays anti-malarial and demelanizing activities. Hydroquinine effectively induces specific RND-type efflux pump systems in Pseudomonas aeruginosa, particularly the MexCD-OprJ and MexXY efflux pumps. Hydroquinine inhibits Pseudomonas aeruginosa adhesion and biofilm formation. Hydroquinine serves as a precursor for derivatives such as C9 epihydroquinine, 9-acetoxy-10,11-dihydroquinine, and 10,11-dihydroquinine monohydrochloride .
    Hydroquinine
  • HY-107566
    Conessine

    		Histamine Receptor Parasite MDM-2/p53 NF-κB FOXO Bacterial Infection Neurological Disease
    Conessine is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pKi values of Conessine for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine has antimalarial activity. Conessine can also be used in the research of muscle atrophy .
    Conessine
  • HY-N10455
    24-Epicastasterone
    2 Publications Verification

    24-epi-Castasterone

    		 Drug Derivative Others
    24-Epicastasterone (24-epi-Castasterone) is a bioactive brassinosteroid and a ligand of ABCB1 and ABCB19 in Arabidopsis thaliana. 24-Epicastasterone stimulates the ATPase activity of ABCB19 and the ATP hydrolysis activity of ABCB1, which drive the efflux of substances from plant cells. 24-Epicastasterone increases the activities of catalase and guaiacol peroxidase in the roots of wheat seedlings. 24-Epicastasterone alleviates heat-induced lipid peroxidation through a ROS-dependent mechanism and enhances the heat tolerance of common wheat seedlings .
    24-Epicastasterone
  • 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-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-137433
    Befotertinib
    2 Publications Verification

    D-0316

    		 EGFR P-glycoprotein Apoptosis Cancer
    Befotertinib (D-0316) is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib selectively targets EGFR mutations including EGFR T790M, EGFR L858R and delE746-A750, forms covalent bonds with EGFR C797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib can be used in research related to multidrug-resistant cancers and non-small cell lung cancer .
    Befotertinib
  • HY-B0380A
    Trimebutine maleate

    		Opioid Receptor Toll-like Receptor (TLR) Calcium Channel Potassium Channel IRAK ERK JNK NF-κB Akt Apoptosis Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
    Trimebutine maleate
  • HY-B0380
    Trimebutine

    		Opioid Receptor Toll-like Receptor (TLR) Calcium Channel Potassium Channel IRAK ERK JNK NF-κB Akt Apoptosis Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
    Trimebutine
  • HY-P10551
    ApoA-I mimetic peptide 5A

    		Transmembrane Glycoprotein NF-κB TNF Receptor Cardiovascular Disease
    ApoA-I mimetic peptide 5A is a synthetic peptide molecule designed based on the structure and function of naturally occurring apolipoprotein A-I (Apo A-I). ApoA-I mimetic peptide 5A can promote the efflux of cholesterol from cells and help reduce the accumulation of cholesterol in cells. ApoA-I mimetic peptide 5A also shows anti-inflammatory activity and can reduce inflammatory markers in blood and tissues. ApoA-I mimetic peptide 5A can be used in the study of cardiovascular diseases .
    ApoA-I mimetic peptide 5A
  • HY-124819
    D13-9001

    		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-Y1777
    2-Phenylacetophenone

    		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-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-P5589
    Plantaricin A

    PlnA

    		 Bacterial Reactive Oxygen Species (ROS) Infection Inflammation/Immunology
    Plantaricin A is an antimicrobial peptide that can be derived from Lactobacillus plantarum. Plantaricin A has a synergistic effect with Ciprofloxacin. Plantaricin A shows anti-microbial activity. Plantaricin A increases the membrane potential of S. aureus and the level of intracellular ROS. Plantaricin A inhibits the function of the efflux pump by binding it and altering the structure of MepA, NorA, and LmrS. Plantaricin A significantly relieves inflammation, and promotes wound healing. Plantaricin A permeabilizes cancerous rat pituitary cells [1][2].
    Plantaricin A
  • 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-N4314
    Scutellarein tetramethyl ether
    4 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-N0566
    23-Hydroxybetulinic acid

    Anemosapogenin

    		 Apoptosis Autophagy Bcl-2 Family Caspase Survivin p38 MAPK MMP Cancer
    23-Hydroxybetulinic acid (Anemosapogenin) is an orally active triterpenoid with broad-spectrum anticancer activity. 23-Hydroxybetulinic acid reduces the levels of Bcl-2 and survivin, elevates the level of Bax, promotes the cleavage/activation of caspase-3 and caspase-9, and induces apoptosis via the endogenous mitochondrial pathway involving cytochrome C release and mitochondrial membrane potential disruption. 23-Hydroxybetulinic acid arrests the cell cycle at S and G1 phases, inhibits cancer cell proliferation, blocks the MAPK signaling pathway, regulates MMP2, and induces autophagic apoptosis by upregulating beclin-1. 23-Hydroxybetulinic acid inhibits the activity and efflux function of P-gp, increases the intracellular accumulation of chemotherapeutic drugs, and synergistically enhances cytotoxicity with Doxorubicin (HY-15142). 23-Hydroxybetulinic acid inhibits the phosphorylation and nuclear translocation of STAT6, blocks M2 macrophage polarization, and reduces M2 macrophage-mediated apoptosis resistance of colon cancer cells. 23-Hydroxybetulinic acid can be used in related studies on chronic myeloid leukemia, hepatocellular carcinoma, sarcoma 180, multidrug-resistant breast cancer, leukemia, Doxorubicin-induced cardiotoxicity, and colorectal cancer .
    23-Hydroxybetulinic acid
  • HY-136450
    Triclabendazole sulfoxide

    TCBZ-SO

    		 Parasite BCRP Infection Cancer
    Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
    Triclabendazole sulfoxide
  • HY-126941
    Hecogenin acetate

    		ERK MMP Reactive Oxygen Species (ROS) NF-κB p38 MAPK NOD-like Receptor (NLR) TRP Channel TNF Receptor Interleukin Related Infection Neurological Disease Inflammation/Immunology Endocrinology
    Hecogenin acetate is an orally active steroid saponin aglycone with extensive biological activities. Hecogenin acetate inhibits the phosphorylation of NF-κB and p38 MAPK signaling pathways, antagonizes TRPA1/TRPM8 channels, inhibits the production of pro-inflammatory cytokines, and has anti-inflammatory and analgesic effects. Hecogenin acetate inhibits the production of ROS and the activation of NLRP3 inflammasome; downregulates the expression of MMP-2, and has neuroprotective and anti-tumor activities. Hecogenin acetate enhances gastric mucosal defense and promotes ulcer healing. Hecogenin acetate can be used in combination with certain antibiotics to regulate bacterial efflux pumps and restore antibiotic sensitivity .
    Hecogenin acetate
  • HY-117931
    NS004

    		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-N16577
    (S)-Tenacissoside F

    		P-glycoprotein Cancer
    (S)-Tenacissoside F (Compound P20) is a polyoxypregnane compound found in Marsdenia tenacissima. (S)-Tenacissoside F can inhibit the drug efflux activity mediated by P-glycoprotein (P-gp/ABCB1) and reverse multidrug resistance. (S)-Tenacissoside F can be used for the research of cancer, such as colon cancer .
    (S)-Tenacissoside F
  • HY-17390AR
    Loxapine succinate (Standard)

    		Reference Standards 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-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-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-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-124187
    Pinolenic acid ethyl ester

    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-178111
    AcrB-IN-6

    		Bacterial Infection
    AcrB-IN-6 is an effective AcrB inhibitor. AcrB-IN-6 The compound inhibits the function of bacterial multidrug efflux pumps, thereby significantly enhancing the antibacterial activity of various antibiotics. AcrB-IN-6 achieves 32-fold MIC reductions in wild-type E. coli BW25113. AcrB-IN-6 exhibits excellent synergistic antibacterial effects, low cytotoxicity and hemolytic properties. AcrB-IN-6 can be used for researching anti-resistant bacteria .
    AcrB-IN-6
  • HY-N9947
    Methyl-6-gingerol

    		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-108694R
    γ-Tocotrienol (Standard)

    		Reference Standards 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-102008
    LBM-415

    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-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-107566A
    Conessine dihydrobromide

    		Histamine Receptor Parasite MDM-2/p53 NF-κB FOXO Bacterial Infection Neurological Disease
    Conessine dihydrobromide is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pKi values of Conessine dihydrobromide for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine dihydrobromide is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine dihydrobromide has antimalarial activity. Conessine dihydrobromide can also be used in the research of muscle atrophy .
    Conessine dihydrobromide
  • HY-156965
    BAY-771

    		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-136940
    Ac22(Az8)2

    		BCRP Cancer
    Ac22(Az8)2​ is a selective BCRP inhibitor (EC50: 1-2 nM). Ac22(Az8)2 can restore the drug sensitivity of BCRP-overexpressing cells by inhibiting BCRP-ATPase activity, blocking drug efflux, and increasing intracellular drug accumulation. Ac22(Az8)2 can be used in the research of BCRP-mediated multidrug-resistant cancers .
    Ac22(Az8)2
  • HY-137433A
    Befotertinib mesylate

    D-0316 mesylate

    		 EGFR P-glycoprotein Apoptosis Inflammation/Immunology Cancer
    Befotertinib (D-0316) mesylate is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib mesylate selectively targets EGFR mutations including EGFR T790M, EGFR L858R and delE746-A750, forms covalent bonds with EGFR C797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib mesylate inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib mesylate can be used in research related to multidrug-resistant cancers and non-small cell lung cancer .
    Befotertinib mesylate
  • HY-178466
    Tubulin polymerization/P-gp-IN-1

    		Microtubule/Tubulin P-glycoprotein Apoptosis Cancer
    Tubulin polymerization/P-gp-IN-1 is a Tubulin polymerization/P-gp dual inhibitor. Tubulin polymerization/P-gp-IN-1 inhibits tubulin polymerization and induces G2/M arrest and apoptosis. Tubulin polymerization/P-gp-IN-1 reverses MDR by inhibiting P-gp efflux function. Tubulin polymerization/P-gp-IN-1 has dual functions: direct antitumor activity and reversal of P-gp-mediated Cisplatin (HY-17394) resistance. Tubulin polymerization/P-gp-IN-1 stable binds to the tubulin CBS (ΔG = −12.4 kcal/mol) and the P-gp hydrophobic lumen (ΔG = −10.8 kcal/mol). Tubulin polymerization/P-gp-IN-1 can be used for the study of drug-resistant cervical cancer .
    Tubulin polymerization/P-gp-IN-1
  • HY-B0380S1
    Trimebutine-d5 fumarate

    		Isotope-Labeled Compounds Opioid Receptor Toll-like Receptor (TLR) Calcium Channel Potassium Channel IRAK ERK JNK NF-κB Akt Apoptosis Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Trimebutine-d5 fumarate is deuterium labeled Trimebutine fumarate. Trimebutine fumarate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine fumarate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine fumarate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine fumarate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine fumarate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
    Trimebutine-d5 fumarate
  • HY-B0380AR
    Trimebutine maleate (Standard)

    		Reference Standards Opioid Receptor Apoptosis Potassium Channel NF-κB Akt IRAK JNK Toll-like Receptor (TLR) ERK Calcium Channel Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Trimebutine maleate (Standard) is the analytical standard of Trimebutine maleate (HY-B0380A). This product is intended for research and analytical applications. Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
    Trimebutine maleate (Standard)
  • 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-P10874
    SMR efflux inhibitor

    		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
    Timcodar mesylate

    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-Y1777R
    2-Phenylacetophenone (Standard)

    		Drug Derivative Reference Standards 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 (Standard)
  • HY-163454
    NorA-IN-2

    		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-111440
    MC-04124

    		Bacterial Infection
    MC-04124 is an efflux pump inhibitor. MC-04124 significantly enhances the activity of Levofloxacin (HY-B0330) against Pseudomonas aeruginosa .
    MC-04124
  • HY-N12171
    Isoreserpiline

    		Bacterial Infection Neurological Disease
    Isoreserpiline is an orally active and BBB-penetrable 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

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