Search Result
Results for "
Efflux pump
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-Y1777
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Others
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Infection
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2-Phenylacetophenone has broad-spectrum efflux pump inhibition activity. 2-Phenylacetophenone is a benzoin derivative used as a photoinitiator in vinyl polymerization .
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- HY-156753
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Others
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Cancer
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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 .
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- HY-N2947
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P-glycoprotein
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Infection
Inflammation/Immunology
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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 .
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- HY-101444A
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MC-207,110 dihydrochloride; Phe-Arg-β-naphthylamide dihydrochloride
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Bacterial
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Infection
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PAβN dihydrochloride (MC-207110 dihydrochloride) is an efflux pump inhibitor.
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- HY-149811
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Bacterial
Parasite
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Infection
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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 .
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- HY-149812
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Bacterial
Parasite
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Infection
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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 .
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- HY-149810
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Bacterial
Parasite
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Infection
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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 .
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- HY-N2947R
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P-glycoprotein
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Infection
Inflammation/Immunology
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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 .
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- HY-163473
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Bacterial
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Infection
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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. .
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- HY-13766A
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VX-853-2
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Others
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Others
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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 .
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- HY-124819
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Bacterial
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Infection
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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 .
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- HY-157533
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Bacterial
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Others
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AcrB-IN-5 (compound 8) inhibits AcrB and blocks the efflux pump in a dose-dependent manner .
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- HY-119172
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- HY-163454
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Bacterial
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Infection
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NorA-IN-2 (compound DZ-3) is a potent NorA inhibitor. NorA-IN-2 shows NorA efflux pump inhibitors (EPI) activity .
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- HY-157987
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Bacterial
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Infection
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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 .
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- HY-162144
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Bacterial
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Infection
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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 .
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- HY-155048
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Bacterial
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Infection
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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 .
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- HY-100750
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- HY-135328
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- HY-17390A
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5-HT Receptor
Dopamine Receptor
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Infection
Neurological Disease
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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 .
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- HY-162822
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P-glycoprotein
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Cancer
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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 .
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- HY-W107077
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Others
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Infection
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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 .
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- HY-120574
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ADC Cytotoxin
Topoisomerase
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Cancer
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TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile .
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- HY-146389
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MDM-2/p53
P-glycoprotein
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Cancer
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Anticancer agent 50 (compound 6) is a potent ABCB1 efflux pump modulator. Anticancer agent 50 shows cytotoxic effects and antiproliferative effects. Anticancer agent 50 decreases the expression of cyclin D1 and induces p53 expression. Anticancer agent 50 has the potential for the research of T-lymphoma .
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- HY-135328S
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- HY-N10069
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Others
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Infection
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Bonducellin is a a homoisoflavonoid, which can be isolated from Caesalpinia digyna roots. Bonducellin is a potent inhibitor of efflux pump (EP), while EP induces resistance in mycobacteria and serves as a target of anti-TB (tuberculosis) agents. Bonducellin reduces MIC of EtBr by 8-fold against M. smegmatis (MIC=62.5 mg/L) .
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- HY-N12320
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Antibiotic
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Infection
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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 .
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- HY-102008
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NVP-PDF 713; VIC-104959
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Bacterial
Antibiotic
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Infection
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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 .
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- HY-17390AR
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5-HT Receptor
Dopamine Receptor
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Infection
Neurological Disease
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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 .
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- HY-P1649B
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NAB741 acetate
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Bacterial
Antibiotic
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Infection
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SPR741 acetate (NAB741 acetate) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 acetate increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 acetate inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 acetate .
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- HY-P1649
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NAB741
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Bacterial
Antibiotic
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Infection
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SPR741 (NAB741) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 .
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- HY-P1649A
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NAB741 TFA
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Bacterial
Antibiotic
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Infection
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SPR741 TFA (NAB741 TFA) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 TFA increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 TFA inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 TFA .
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- HY-155198
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Fungal
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Infection
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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 .
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- HY-168077
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Fungal
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Infection
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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 .
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- HY-19895
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Others
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Infection
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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 .
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- HY-N4314
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4',5,6,7-Tetramethoxyflavone
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Bacterial
COX
NO Synthase
NF-κB
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Infection
Inflammation/Immunology
Cancer
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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) .
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- HY-138074
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5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime
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Parasite
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Infection
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Milbemycin A4 oxime is a derivative of milbemycin A4 (Item No. 17155) and a component of Milbemycin Oxime (HY-B0778), compounds that both have insecticidal and nematocidal activity. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae of the heartworm D. immitis in naturally infested dogs. It inhibits the growth of clinical isolates of C. glabrata with MIC80 values ranging from 16 to greater than 32 μg/mL.1 Milbemycin A4 oxime (2.5 μg/mL) blocks efflux of Fluconazole (HY-B0101) from a clinical isolate of C. glabrata, but not from a strain lacking the efflux pumps CgCDR1 and PDH1, and reduces the MICs of fluconazole and 4-nitroquinoline 1-oxide in wild-type C. glabrata. It enhances adriamycin-induced inhibition of cell growth, as well as increases the intracellular accumulation of adriamycin and the P-glycoprotein substrate Rhodamine 123 (HY-D0816), in adriamycin-resistant, but not -sensitive, MCF-7 breast cancer cells in a concentration-dependent manner.
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- HY-N4314R
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Bacterial
COX
NO Synthase
NF-κB
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Infection
Inflammation/Immunology
Cancer
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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) .
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- HY-W127487
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Biochemical Assay Reagents
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Others
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Quorum sensing is a regulatory system used by bacteria to control gene expression in response to increased cell density. This regulatory process manifests itself in a variety of phenotypes, including biofilm formation and virulence factor production. Coordinated gene expression is achieved through the production, release and detection of small diffusible signaling molecules called autoinducers. N-acylated homoserine lactones (AHLs) comprise a class of such autoinducers, each of which generally consists of a fatty acid coupled to a homoserine lactone (HSL). Modulation of bacterial quorum-sensing signaling systems to suppress pathogenesis represents a new approach to antimicrobial research for infectious diseases. AHLs differ in acyl length (C4-C18), C3 substitution (hydrogen, hydroxyl, or oxo group), and the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signaling specificity through the affinity of the LuxR family of transcriptional regulators. C18-HSL, one of four lipophilic long acyl side chain AHLs produced by the LuxI AHL synthase homolog SinI, is involved in quorum-sensing signaling in strains of Rhizobium meliloti (a nitrogen-fixing bacterial symbiont of the legume M. sativa) . C18-HSL and other hydrophobic AHLs tend to localize in the relatively lipophilic environment of bacterial cells and cannot diffuse freely across the cell membrane. Long-chain N-acyl homoserine lactones can be exported from cells by efflux pumps, or can be transported between communicating cells by extracellular outer membrane vesicles.
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HY-L048
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386 compounds
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The high rates of morbidity and mortality caused by fungal infections are associated with the current limited antifungal arsenal and the high toxicity of the compounds. Additionally, identifying novel drug targets is challenging because there are many similarities between fungal and human cells. The most common antifungal targets include fungal RNA synthesis and cell wall and membrane components, though new antifungal targets are being investigated. Nonetheless, fungi have developed resistance mechanisms, such as overexpression of efflux pump proteins, overexpression and changes in drug targets and biofilm formation, emphasizing the importance of discovering new antifungal drugs and therapies. Due to the limited antifungal arsenal, researchers have sought to improve treatment via different approaches, such as the combination of antifungal drugs, development of new formulations for antifungal agents and modifications to the chemical structures of traditional antifungals, etc.
MCE offers a unique collection of 386 compounds with validated antifungal activities. MCE antifungal compound library is an effective tool for drug repurposing screening, combination screening and biological investigation.
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Cat. No. |
Product Name |
Type |
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- HY-W127487
-
|
Drug Delivery
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Quorum sensing is a regulatory system used by bacteria to control gene expression in response to increased cell density. This regulatory process manifests itself in a variety of phenotypes, including biofilm formation and virulence factor production. Coordinated gene expression is achieved through the production, release and detection of small diffusible signaling molecules called autoinducers. N-acylated homoserine lactones (AHLs) comprise a class of such autoinducers, each of which generally consists of a fatty acid coupled to a homoserine lactone (HSL). Modulation of bacterial quorum-sensing signaling systems to suppress pathogenesis represents a new approach to antimicrobial research for infectious diseases. AHLs differ in acyl length (C4-C18), C3 substitution (hydrogen, hydroxyl, or oxo group), and the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signaling specificity through the affinity of the LuxR family of transcriptional regulators. C18-HSL, one of four lipophilic long acyl side chain AHLs produced by the LuxI AHL synthase homolog SinI, is involved in quorum-sensing signaling in strains of Rhizobium meliloti (a nitrogen-fixing bacterial symbiont of the legume M. sativa) . C18-HSL and other hydrophobic AHLs tend to localize in the relatively lipophilic environment of bacterial cells and cannot diffuse freely across the cell membrane. Long-chain N-acyl homoserine lactones can be exported from cells by efflux pumps, or can be transported between communicating cells by extracellular outer membrane vesicles.
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1649B
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NAB741 acetate
|
Bacterial
Antibiotic
|
Infection
|
SPR741 acetate (NAB741 acetate) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 acetate increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 acetate inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 acetate .
|
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- HY-P1649
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NAB741
|
Bacterial
Antibiotic
|
Infection
|
SPR741 (NAB741) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 .
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- HY-P1649A
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NAB741 TFA
|
Bacterial
Antibiotic
|
Infection
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SPR741 TFA (NAB741 TFA) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 TFA increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 TFA inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 TFA .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N2947
-
-
-
- HY-N4314
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4',5,6,7-Tetramethoxyflavone
|
Infection
Structural Classification
Flavonoids
Classification of Application Fields
Flavones
Plants
Compositae
Genista maderensis (Webb & Berthel.) Lowe
Inflammation/Immunology
Disease Research Fields
|
Bacterial
COX
NO Synthase
NF-κB
|
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) .
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- HY-N2947R
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-
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- HY-N10069
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-
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- HY-N12320
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-
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- HY-N4314R
-
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Structural Classification
Flavonoids
Flavones
Plants
Compositae
Genista maderensis (Webb & Berthel.) Lowe
|
Bacterial
COX
NO Synthase
NF-κB
|
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) .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-135328S
-
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Norverapamil-d7 is a deuterium labeled Norverapamil ((±)-Norverapamil). Norverapamil, an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2].
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