Search Result
Results for "
efflux
" in MedChemExpress (MCE) Product Catalog:
4
Biochemical Assay Reagents
5
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-112505
-
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BCRP
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Cancer
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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 .
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- HY-P2576
-
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Bacterial
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Infection
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Polistes mastoparan is an antimicrobial peptide. Polistes mastoparan increases S. aureus cell K + efflux and inhibits cell viability with EC50 of 5 μM .
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-
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- HY-Y1777
-
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Drug Derivative
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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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-
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- HY-156753
-
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Bacterial
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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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-
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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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-
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- HY-P10874
-
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Bacterial
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Infection
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SMR efflux inhibitor targets the small multidrug resistance (SMR) efflux pump, blocks the interaction of TM4-TM4, and exhibits board-spectrum antibacterial activity .
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-
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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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-
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- HY-158264
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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-161246
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5-HT Receptor
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Neurological Disease
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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 .
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- HY-128773
-
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Bacterial
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Infection
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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 .
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- HY-128773A
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Bacterial
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Infection
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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 .
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- HY-162447
-
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P-glycoprotein
Apoptosis
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Cancer
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P-gp inhibitor 22 is a P-glycoprotein (P-gp) inhibitor that effectively inhibits P-pg and efflux function. P-gp inhibitor 22 induces apoptosis and accumulation of MCF-7/ADR cells processed in the S phase .
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- HY-144393
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BCRP
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Cancer
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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) .
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- HY-143792
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P-glycoprotein
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Neurological Disease
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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 .
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- HY-139665
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VB124
1 Publications Verification
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Monocarboxylate Transporter
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Cardiovascular Disease
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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 .
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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-122416
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Lonchocarpol A; Senegalensin
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BCRP
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Metabolic Disease
Cancer
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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 .
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- HY-P10551
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Transmembrane Glycoprotein
NF-κB
TNF Receptor
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Cardiovascular Disease
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Apo A-I mimetic 5A peptide is a synthetic peptide molecule designed based on the structure and function of naturally occurring apolipoprotein A-I (Apo A-I). Apo A-I mimetic 5A peptide can promote the efflux of cholesterol from cells and help reduce the accumulation of cholesterol in cells. Apo A-I mimetic 5A peptide also shows anti-inflammatory activity and can reduce inflammatory markers in blood and tissues. Apo A-I mimetic 5A peptide can be used in the study of cardiovascular diseases .
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- HY-132301
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MCT4-IN-1
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Monocarboxylate Transporter
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Cancer
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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.
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- HY-B0388
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-
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- HY-13766A
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VX-853-2
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Bacterial
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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-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-B0193A
-
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Adrenergic Receptor
Autophagy
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Cardiovascular Disease
Endocrinology
Cancer
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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 .
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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-100390
-
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BCRP
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Cancer
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(S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
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-
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- HY-119172
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-
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- HY-N11697
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P-glycoprotein
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Cancer
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α-Cryptoxanthin is a natural carotenoid with anticancer effects. α-Cryptoxanthin inhibits multidrug resistance 1 (MDR1) mediated efflux pump .
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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-N9947
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Bacterial
Antibiotic
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Infection
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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 .
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-
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- HY-N3308
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Apoptosis
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Cancer
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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 .
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- HY-112220
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Ferroportin
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Metabolic Disease
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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 .
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- HY-129279
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Farnesyl Transferase
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Cancer
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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 .
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- HY-158556
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2,3-Dmec hydrochloride
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Drug Derivative
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Neurological Disease
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2,3-Dimethylethcathinone (2,3-Dmec) hydrochloride, a cathinone, is an analog of Ethcathinone. Ethcathinone increases the peak dopamine efflux after electrical stimulation and slows dopamine reuptake in rats .
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- HY-50879
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Elacridar
Maximum Cited Publications
27 Publications Verification
GF120918; GW0918; GG918; GW120918
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P-glycoprotein
BCRP
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Cancer
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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 .
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- HY-N2419
-
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Endogenous Metabolite
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Metabolic Disease
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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 .
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- HY-129098
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DMHCA
1 Publications Verification
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LXR
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Metabolic Disease
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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 .
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- HY-163079
-
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FAP
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Cancer
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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 .
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-
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- HY-128038
-
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Opioid Receptor
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Neurological Disease
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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 .
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- HY-E70511
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Cytochrome P450
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Metabolic Disease
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Human CYP46A1, High-Reductase, a recombinant CYP46A1, is a member of the CYP enzyme family. CYP46A1 is expressed mainly in brain neurons and is responsible for brain cholesterol homeostasis by regulating the cholesterol efflux .
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- HY-E70510
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Cytochrome P450
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Metabolic Disease
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Human CYP46A1, Low-Reductase, a recombinant CYP46A1, is a member of the CYP enzyme family. CYP46A1 is expressed mainly in brain neurons and is responsible for brain cholesterol homeostasis by regulating the cholesterol efflux .
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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-157483
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P-glycoprotein
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Cancer
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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 .
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-
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- HY-W590664
-
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Endogenous Metabolite
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Cardiovascular Disease
|
C2 Dihydroceramide is a derivative of C2 Ceramide (HY-101180). C2 Dihydroceramide enhances the ABCA1-mediated cholesterol efflux to apolipoprotein A-I (apoA-I) without causing cytotoxicity .
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- HY-50880
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GF120918A
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P-glycoprotein
BCRP
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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 .
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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-19846
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PRX-03140 potassium salt
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5-HT Receptor
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Others
|
VRX-03011 (PRX-03140 (potassium salt)) is a compound with the potential to enhance memory and regulate acetylcholine release. It is a 5-HT? agonist that can enhance memory, regulate hippocampal acetylcholine efflux, and regulate APP metabolism without gastrointestinal side effects.
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- HY-N12171
-
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Bacterial
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Infection
Neurological Disease
|
Isoreserpiline is an orally active and BBB-penatrable indole alkaloids with antibacterial and antipsychotic activity. Isoreserpiline is even more effective when used in combination with antibiotics and inhibits the activity of bacterial efflux pumps. Isoreserpiline improves Amphetamine-induced hyperactivity in mice .
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- HY-162714
-
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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 .
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- HY-P3156
-
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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 .
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- HY-171195
-
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5-HT Receptor
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Metabolic Disease
|
VU0631019 is a potent antagonist of 5-HT2B, with the IC50 of 29 nM. VU0631019 is predicted to have very limited potential for brain penetration in human subjects, as is predicted to be substrates for P-gp-mediated efflux in humans .
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- HY-B0501
-
CP 76136-27
|
P-glycoprotein
Bacterial
Antibiotic
|
Infection
|
Danofloxacin mesylate (CP 76136-27) is a fluoroquinolone used as a veterinary drug. Danofloxacin mesylate has a broad spectrum of bactericidal activity, mainly inhibiting the DNA cycloenzyme of the bacteria. In addition, Danofloxacin mesylate is a substrate for ATP-dependent efflux transporters (P-gp and MRP2) .
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- HY-171194
-
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5-HT Receptor
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Metabolic Disease
|
VU0530244 is a potent antagonist of 5-HT2B, with the IC50 of 17.3 nM. VU0530244 is predicted to have very limited potential for brain penetration in human subjects, as is predicted to be substrates for P-gp-mediated efflux in humans .
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- HY-D2261
-
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Fluorescent Dye
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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).
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- HY-N0406
-
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P-glycoprotein
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Inflammation/Immunology
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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 .
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- HY-126940
-
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Reactive Oxygen Species
P-glycoprotein
Apoptosis
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Cancer
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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 .
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- HY-146067
-
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Fungal
Reactive Oxygen Species
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Infection
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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 .
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- HY-P10811
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XIP
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Na+/Ca2+ Exchanger
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Neurological Disease
|
Na +-Ca 2+ Exchanger inhibitory peptide (XIP) is a Na +-Ca 2+ exchanger inhibitor with a Ki of 200 nM. Na +-Ca 2+ Exchanger inhibitory peptide inhibits the Na +-dependent Ca 2+ uptake and the Na +-dependent Ca 2+ efflux of sarcolemmal vesicles in a noncompetitive manner .
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- HY-P2624
-
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PAK
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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 .
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- HY-P5878
-
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Biochemical Assay Reagents
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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) .
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- HY-D2262
-
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Fluorescent Dye
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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) .
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- HY-14942
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RTA 744 free base; WP 744 free base; WP 769
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P-glycoprotein
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Cancer
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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 .
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- HY-N2419R
-
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Endogenous Metabolite
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Metabolic Disease
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Erythrodiol (Standard) is the analytical standard of Erythrodiol. This product is intended for research and analytical applications. 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 .
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- HY-100750
-
-
- HY-135328
-
-
- HY-146117
-
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P-glycoprotein
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Cancer
|
P-gp modulator 2 (Compound 27) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator .
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- HY-146118
-
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P-glycoprotein
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Cancer
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P-gp modulator 3 (Compound 37) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator .
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- HY-16688A
-
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5-HT Receptor
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Neurological Disease
|
RU 24969 succinate is a 5-HT receptor agonist with Ki values of 0.38 and 2.5 nM for 5-HT1B and 5-HT1A, respectively. RU 24969 decreases fluid consumption and increases forward locomotion. RU 24969 succinate can be used for the research of neurological disease .
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- HY-100750R
-
-
- 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-100928
-
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Calcium Channel
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Neurological Disease
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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 .
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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-W040150
-
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LXR
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Neurological Disease
Inflammation/Immunology
Cancer
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24S,25-Epoxycholesterol is an agonist for Liver X Receptor (LXR). 24S,25-Epoxycholesterol exhibits properties in regulating the cholesterol efflux , inhibiting tumor growth against gastric cancer and glioblastoma and inducing apoptosis in BMMC cells .
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- HY-B0777
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CL301423
|
Antibiotic
BCRP
P-glycoprotein
Parasite
|
Infection
|
Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
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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-144366
-
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P-glycoprotein
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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 .
|
-
- HY-146389
-
|
MDM-2/p53
P-glycoprotein
|
Cancer
|
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 .
|
-
- HY-N10512
-
Gg4
|
Others
|
Neurological Disease
|
Gangliotetraose (Gg4) is a tetrasccharide, exhibits major components including GM1 and its sialylated derivatives. GM1 facilitates efflux of nuclear Ca 2+ and reduces the level of nuclear Ca 2+ that characterizes the differentiated neuron. GM1 affects neuronal plasticity and repair mechanisms, as well as neurotrophin release in the brain .
|
-
- HY-157484
-
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 19 (Compound 6i) is a P-gp inhibitor. P-gp inhibitor 19 can inhibit the efflux of rhodamine 123 (HY-D0816) in P-gp-overexpressing leukemia cells K562/Dox and also restore the sensitivity of DOX-resistant cells .
|
-
- HY-P2624A
-
|
PAK
|
Metabolic Disease
|
st-Ht31 ammonium is a membrane-permeable peptide inhibitor of?protein kinase A (PKA) anchoring. st-Ht31 ammonium induces robust cholesterol/phospholipid efflux. st-Ht31 ammonium completely reverses foam cell formation and restores the metabolic health of macrophage .
|
-
- HY-161645
-
|
P-glycoprotein
|
Cancer
|
P-gp modulator-4 (compound 4c) inhibits the efflux function of P-glycoprotein (P-gp). P-gp modulator-4 shows multidrug resistance (MDR) in cancer reversal activity (IC50 of Paclitaxel (HY-B0015) = 8.80, reversal fold = 211.8) .
|
-
- HY-N4104
-
Agaricinic Acid
|
Mitochondrial Metabolism
|
Metabolic Disease
|
Agaric acid (Agaricinic Acid) is obtained from various plants of the fungous tribe, i.e. Polyporus officinalis and Polyporus igniarius. Agaric acid induces mitochondrial permeability transition through its interaction with the adenine nucleotide translocase. Agaric acid promotes efflux of accumulated Ca 2+, collapse of transmembrane potential, and mitochondrial swelling. Agaric acid is used to regulate lipid metabolism .
|
-
- HY-113365S
-
4-Cholesten-3-one-d5
|
Endogenous Metabolite
|
Metabolic Disease
|
Cholestenone-d5 is the deuterium labeled Cholestenone. 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[1][2][3].
|
-
- HY-113365S1
-
4-Cholesten-3-one-13C
|
Endogenous Metabolite
|
Metabolic Disease
|
Cholestenone- 13C is the 13C labeled Cholestenone. 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[1][2][3].
|
-
- HY-N10069
-
|
Bacterial
|
Infection
|
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) .
|
-
- HY-N12320
-
|
Antibiotic
|
Infection
|
Majoranaquinone exhibits a high antibacterial effect against 4 Staphylococcus, 1 Moraxella, and 1 Enterococcus strains. Majoranaquinone shows substantial efflux pump inhibitory activity in Escherichia coliATCC 25922 strain. Majoranaquinone is found to be an effective biofilm formation inhibitor on E.coli, ATCC 25922 and E. coli K-12 AG100 bacteria .
|
-
- HY-159085
-
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 24 (Compound 10) is an inhibitor for P-glycoprotein (P-gp)), that inhibits the P-gp mediated fluorescent dye efflux. P-gp inhibitor 24 exhibits multidrug resistance (MDR) reversal effect, enhances the cytotoxicity of Vincristine (HY-N0488) and Etoposide (HY-13629) in cancer cells .
|
-
- HY-B0501R
-
|
Bacterial
Antibiotic
|
Infection
|
Danofloxacin mesylate (Standard) is the analytical standard of Danofloxacin mesylate. This product is intended for research and analytical applications. Danofloxacin mesylate (CP 76136-27) is a fluoroquinolone used as a veterinary drug. Danofloxacin mesylate has a broad spectrum of bactericidal activity, mainly inhibiting the DNA cycloenzyme of the bacteria. In addition, Danofloxacin mesylate is a substrate for ATP-dependent efflux transporters (P-gp and MRP2) .
|
-
- HY-135328S
-
-
- HY-N0076
-
(-)-Bilobalide
|
Apoptosis
Autophagy
Endogenous Metabolite
|
Neurological Disease
|
Bilobalide, a sesquiterpene trilactone constituent of Ginkgo biloba, inhibits the NMDA-induced efflux of choline with an IC50 value of 2.3 µM. Bilobalide prevents apoptosis through activation of the PI3K/Akt pathway in SH-SY5Y cells. Exerts protective and trophic effects on neurons .
|
-
- HY-N0246
-
|
LXR
Bacterial
|
Inflammation/Immunology
Cancer
|
Saikosaponin A is the main active ingredient in Bupleurum chinense, which can regulate lipid metabolism and promote cholesterol efflux in early atherosclerosis. In addition, Saikosaponin A may also serve as a potential peroxisome proliferator-activated receptor γ (PPAR-γ) agonist, significantly promoting the expression of PPAR-γ. Saikosaponin A can be used in the study of hyperlipidemic pancreatitis .
|
-
- HY-117203A
-
|
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 .
|
-
- HY-113365S2
-
4-Cholesten-3-one-13C2
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Metabolic Disease
|
Cholestenone- 13C2 is the 13C labeled Cholestenone. 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[1][2][3].
|
-
- HY-N12235
-
|
Caspase
|
Inflammation/Immunology
|
Sarglaroids F (compound 6) is an anti-inflammatory agent isolated from the roots of Grass Coral. Sarglaroids F inhibits LPS/ATP-induced IL-1β release by affecting K+ efflux and reducing Caspase-1(P20) levels. Sarglaroids F is not cytotoxic to RAW264.7 cells .
|
-
- HY-102008
-
NVP-PDF 713; VIC-104959
|
Bacterial
Antibiotic
|
Infection
|
LBM-415 (NVP-PDF 713) is a peptide deformylase (PDF) inhibitor that exhibits inhibitory activity against various antimicrobial-resistant gram-positive cocci, with a MIC90 range of 0.12-8 µg/ml. Additionally, inhibiting efflux pump activity can enhance bacterial sensitivity to LBM415, thereby improving its antibacterial efficacy .
|
-
- HY-N9947A
-
|
Antibiotic
Bacterial
|
Infection
|
(rac)-Methyl-6-gingerol (Compound 14) is the racemate of Methyl-6-gingerol (HY-N9947). Methyl-6-gingerol is an antibiotic that can be isolated from Aframomum melegueta. Methyl-6-gingerol exhibits anti-mycobacterial activity by inhibiting the efflux of toxins within Mycobacterium species .
|
-
- HY-101511
-
|
P-glycoprotein
|
Cancer
|
TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1 .
|
-
- HY-130244
-
|
Beta-secretase
|
Neurological Disease
|
BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux .
|
-
- HY-123402
-
GSK3987
1 Publications Verification
|
LXR
|
Metabolic Disease
|
GSK3987 is a pan LXRα/β agonist with EC50s of 50 nM, 40 nM for LXRα-SRC1 and LXRβ-SRC1, respectively. GSK3987 increases the expression of ABCA1 and SREBP-1c. GSK3987 induces cellular cholesterol efflux and triglyceride accumulation .
|
-
- HY-147397
-
|
Pyruvate Kinase
|
Cancer
|
PKM2 activator 3 is a potent PKM2 activator with an AC50 value of 90 nM. PKM2 activator 3 has good Caco-2 permeability, a low efflux ratio and high microsomal stability. PKM2 activator 3 can be used for researching anticancer .
(AC50: the concentration which gives 50% activation of enzyme.)
|
-
- HY-119229
-
|
CFTR
|
Others
|
VRT-325 is a novel small molecule discovered by screening a compound library designed to address the genetic defect in cystic fibrosis (CF) caused by the ΔF508 mutation in CFTR. VRT-325 belongs to a class of compounds that promote ΔF508-CFTR efflux from the endoplasmic reticulum and restores chloride transport levels in epithelial cells of CF-derived bronchi .
|
-
- HY-117763
-
|
Calcium Channel
|
Others
|
A-39355 is a compound that can overcome multidrug resistance and has the activity of reversing multidrug resistance. A-39355 can enhance the cytotoxicity of antitumor compounds in multidrug-resistant cells, increase the accumulation of compounds in cells, inhibit the efflux of compounds, and compared with calcium antagonists, it has no serious hypotensive effect. Its activity may be unrelated to the ability to block calcium transport.
|
-
- HY-120768
-
|
Drug Derivative
|
Others
|
A-30312 is a compound that can overcome multidrug resistance and has the activity of reversing multidrug resistance. A-30312 can enhance the cytotoxicity of antitumor compounds in multidrug-resistant cells, increase the accumulation of compounds in cells, inhibit the efflux of compounds, and compared with calcium antagonists, it has no serious hypotensive effect. Its activity may be unrelated to the ability to block calcium transport.
|
-
- HY-130282
-
|
Bacterial
|
Infection
|
Ianthelliformisamine C ditrifluoroacetate is an antibiotic enhancer with activity against resistant Gram-negative bacteria. Ianthelliformisamine C ditrifluoroacetate has been shown to improve the efficacy of doxycycline against Pseudomonas aeruginosa. Ianthelliformisamine C ditrifluoroacetate was prepared using peptide coupling, resulting in high chemical yields of 27 to 91%. Ianthelliformisamine C ditrifluoroacetate exhibits its mechanism of action by inducing ATP efflux and causing membrane depolarization in bacterial cells.
|
-
- HY-172365
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
P7-2302 inhibits PDE7 and PDE4B with IC50 of 0.18 nM and 77.3 nM. P7-2302 inhibits the efflux of P-gp and BCRP (breast cancer resistance protein), exhibits low uptake in rats brain. P7-2302 can be used as a PET tracer when labeled with 18F .
|
-
- HY-147758
-
|
Beta-secretase
Amyloid-β
|
Neurological Disease
|
BACE1/2-IN-1 (compound 34) is a potent BACE1 and BACE2 inhibitor, with an IC50 of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 shows a combination of lower Pgp efflux ratio and improved passive permeability. BACE1/2-IN-1 displays reduced liver microsomal metabolic stability .
|
-
- HY-155032
-
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity,and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015),inhibits tumor progress in nude mice KBV xenograft tumors model .
|
-
- HY-157876
-
|
P-glycoprotein
BCRP
|
Cancer
|
Anticancer agent 191 (Compound 2) is a derivative of probenecid (HY-B0545). As a cancer cell efflux inhibitor, Anticancer agent 191 is designed to inhibit P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and/or multiple multidrug resistance proteins (MRPs). Anticancer agent 191 increases the accumulation of vinblastine in cancer cells, which is used for cancer research .
|
-
- HY-17390AR
-
|
5-HT Receptor
Dopamine Receptor
|
Infection
Neurological Disease
|
Loxapine (succinate) (Standard) is the analytical standard of Loxapine (succinate). This product is intended for research and analytical applications. Loxapine succinate is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistant Salmonella enterica serovar Typhimurium in macrophages .
|
-
- HY-124273
-
L-threo Cer(d18:1/2:0); L-threo Ceramide (d18:1/2:0); N-acetyl-L-threo-Sphingosine
|
Endogenous Metabolite
|
Cardiovascular Disease
|
C2 L-threo Ceramide (d18:1/2:0) (L-threo Cer(d18:1/2:0); L-threo Ceramide (d18:1/2:0)) is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It stimulates cholesterol efflux in CHO cells expressing the human ABCA1 receptor when used at a concentration of 10 μM, however, this efflux is 50% less than that stimulated by C2 ceramide. C2 L-threo Ceramide inhibits IL-4 production by 17% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. It also induces cell cycle arrest in the G0/G1 phase and a 7-fold increase in sphingosine accumulation as well as inhibits growth of HL-60 leukemia cells.
|
-
- HY-U00244A
-
P2647 hydrochloride; BZQ hydrochloride; Benzoquinamide hydrochloride
|
Adrenergic Receptor
|
Cancer
|
Benzquinamide (P2647) is an antiemetic which can bind to the α2A, α2B, and α2C adrenergic receptors (α2-AR) with Ki values of 1,365, 691, and 545 nM, respectively. Benzquinamide also inhibits P-glycoprotein mediated drug efflux and potentiates anticancer agent cytotoxicity in multidrug resistant cells .
|
-
- HY-B0777R
-
CL301423 (Standard)
|
Antibiotic
BCRP
P-glycoprotein
Parasite
|
Infection
|
Moxidectin (Standard) is the analytical standard of Moxidectin. This product is intended for research and analytical applications. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
|
-
- HY-N15297
-
|
P-glycoprotein
|
Cancer
|
Isotenulin inhibits the efflux function of P-glycoprotein by stimulation of P-glycoprotein ATPase, thereby overcoming the multidrug resistance (MDR) of cancer cells. Isotenulin exhibits cytotoxicity in multidrug-resistant cancer cell KB-vin and sensitive cancer cell HeLaS3. Isotenulin exhibits synergistic effect with Paclitaxel (HY-B0015), Vinblastine (HY-13780) and Doxorubicin (HY-15142) .
|
-
- HY-N0406R
-
|
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 .
|
-
- HY-NP011A
-
|
Biochemical Assay Reagents
|
Others
|
Apo-Human transferrin (suitable for cell culture) refers to iron free Transferrin (HY-P3267), serves as Transferrin receptor ligand and mediates iron release from endothelial cells. Apo-Transferrin indicates an iron deficient environment, can directly bind to hephaestin, which can convert Fe 2+ to Fe 3+. Apo-Transferrin mediates iron efflux most likely in cooperation with ferroportin 1 .
|
-
- HY-161260
-
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 20 (compound H27) is a low cytotoxicity P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 20 inhibits the efflux function of P-gp in a dose-dependent manner (without affecting the expression of P-gp), thereby reversing the multidrug resistance (MDR) of MCF-7/ADR cells, with an IC50 value of 46.6 nM. P-gp inhibitor 20 can be used for cancer research .
|
-
- HY-N0076R
-
|
Apoptosis
Autophagy
Endogenous Metabolite
|
Neurological Disease
|
Bilobalide (Standard) is the analytical standard of Bilobalide. This product is intended for research and analytical applications. Bilobalide, a sesquiterpene trilactone constituent of Ginkgo biloba, inhibits the NMDA-induced efflux of choline with an IC50 value of 2.3 μM. Bilobalide prevents apoptosis through activation of the PI3K/Akt pathway in SH-SY5Y cells. Exerts protective and trophic effects on neurons .
|
-
- HY-N0246R
-
|
LXR
Bacterial
|
Metabolic Disease
Inflammation/Immunology
|
Saikosaponin A (Standard) is the analytical standard of Saikosaponin A. This product is intended for research and analytical applications. Saikosaponin A is the main active ingredient in Bupleurum chinense, which can regulate lipid metabolism and promote cholesterol efflux in early atherosclerosis. In addition, Saikosaponin A may also act as a potential peroxisome proliferator-activated receptor-γ (PPAR-γ) agonist, significantly promoting the expression of PPAR-γ. Saikosaponin A can be used in the study of hyperlipidemic pancreatitis .
|
-
- HY-136071
-
-
- HY-136070
-
-
- HY-128129
-
|
Urea Transporter
|
Metabolic Disease
|
UT-B-IN-1 (UTBINH-14) is a reversible, competitive and selective urea transporter-B (UT-B) inhibitor with IC50 values of 10 and 25 nM for human and mouse UT-B, respectively. UT-B-IN-1 shows low toxicity and high selectivity for UT-B over UT-A isoforms. UT-B-IN-1 increases urine output and reduces urine osmolality of mice. UT-B-IN-1 can be used for diuretic mechanism research .
|
-
- HY-149053
-
|
P-glycoprotein
|
Cancer
|
OY-101 is an orally active, potent and specific P-glycoprotein (P-gp) inhibitor. OY-101 can sensitize drug-resistant tumors and effectively reverse tumor multidrug resistance. OY-101 is improvements in water-solubility, cytotoxicity, and reversal activity compared to Tetrandrine (HY-13764) .
|
-
- HY-151517
-
|
Ras
|
Cancer
|
SOS1-IN-14 is a potent, selective and orally active SOS1 inhibitor with an IC50 value of 3.9 nM. SOS1-IN-14 can be absorbed in the intestine via a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 can be used to research KRAS-mutated cancers. SOS1-IN-14 has better potent tumor suppression than BI-3406 (HY-125817) .
|
-
- HY-P3267A
-
|
Ferroportin
Transferrin Receptor
|
Others
Neurological Disease
|
Apo-Bovine Transferrin refers to iron free Transferrin (HY-P3267), serves as Transferrin receptor ligand and mediates iron release from endothelial cells. Apo-Transferrin indicates an iron deficient environment, can directly bind to hephaestin, which can convert Fe 2+ to Fe 3+. Apo-Transferrin mediates iron efflux most likely in cooperation with ferroportin 1. Apo-Bovine Transferrin can be used in neuroretinal research .
|
-
- HY-156965
-
|
Fluorescent Dye
|
Metabolic Disease
Cancer
|
BAY-771, a structurally close pyrimidinedione, is a chemical probe with good lead-like properties and high permeability in Caco-2 cells (no hint of efflux). BAY-771 shows very weak inhibitory activity in the BCAT1 biochemical assay and no activity in BCAT2. BAY-771 can be used as a negative control of HY-148242 BAY-069. BAY-771 can be used for the research of tumor metabolism .
|
-
- HY-D2341
-
|
Fluorescent Dye
|
Cancer
|
6FC-GABA-Taxol is a fluorescent probe with cell permeability, which is formed by connecting 6FC to the anticancer drug Taxol (HY-B0015) via γ-aminobutyric acid (GABA). 6FC-GABA-Taxol can bind to microtubules in living cells and image them through confocal microscopy. Additionally, 6FC-GABA-Taxol enables the quantification of microtubule binding using flow cytometry without the addition of efflux inhibitors .
|
-
- HY-117931
-
|
Potassium Channel
|
Neurological Disease
|
NS004 is a potassium (BK) channel activator that increases Iberiotoxin (HY-P0190) or Tetraethylammonium (HY-B1793)-sensitive whole-cell efflux currents. NS004 also significantly increased the activity of individual GH3 cell BK channels and rat brain BK channels reorganized into planar lipid bilayers, causing an increase in channel mean open time, a decrease in intermittent time, and an increase in channel voltage/calcium sensitivity .
|
-
- HY-B0777S
-
CL-301423-d3
|
Isotope-Labeled Compounds
BCRP
Parasite
Antibiotic
P-glycoprotein
|
Infection
|
Moxidectin-d3 (CL-301423-d3) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
|
-
- HY-155198
-
|
Fungal
|
Infection
|
Antifungal agent 72 (Compound B8) is a potent antifungal agent. Antifungal agent 72 suppresses the function of efflux pump and down-regulates the resistance-associated genes through blocking the Pdr1-KIX interaction (Ki: 11.7 μM). Antifungal agent 72 is active against Fluconazole (HY-B0101)-resistant with a MIC value of 63 ng/mL, and shows synergistic inhibitory activity with Fluconazole. Antifungal agent 72 can be used for C. glabrata infection research .
|
-
- HY-W107077
-
|
Bacterial
|
Infection
|
INF55 is a NoA multidrug resistance pump inhibitor with the activity of inhibiting the NoA pump. The heterocomplex formed by INF55 combined with berberine shows the potential to combat the resistance of bacterial compounds. INF55 can enhance the antibacterial activity of berberine by reducing its efflux. The structural variants of INF55 can show different NoA inhibitory activities, thereby affecting the antibacterial effect of its corresponding heterocomplexes. Different derivatives of INF55 show similar activity in terms of antibacterial dose and effectiveness .
|
-
- HY-136072
-
QPX7728 disodium
|
Bacterial
|
Infection
|
Xeruborbactam (QPX7728) disodium is a potent, ultra-broad-spectrum boronic acid beta-lactamase inhibitor. Xeruborbactam disodium inhibits key serine and metallo beta-lactamases at a nano molar range .
|
-
- HY-P1649B
-
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 .
|
-
- HY-136069
-
QPX7728
|
Bacterial
|
Infection
|
Xeruborbactam (QPX7728) is a potent, ultra-broad-spectrum boronic acid beta-lactamase inhibitor. Xeruborbactam inhibits key serine and metallo beta-lactamases at a nano molar range .
|
-
- HY-P1649
-
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 .
|
-
- HY-P1649A
-
NAB741 TFA
|
Bacterial
Antibiotic
|
Infection
|
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 .
|
-
- HY-B0193AR
-
|
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 .
|
-
- HY-168077
-
|
Fungal
|
Infection
|
Antibiofilm agent-12 (Compound C13) is an antifungal agent that belongs to the class of carbazate derivatives. Antibiofilm agent-12 exhibits significant antifungal activity against Candida auris, with a MIC90 of 237.9 μM. By inhibiting the drug efflux pump activity of Candida auris and promoting ergosterol depletion, Antibiofilm agent-12 hinders biofilm formation and reduces the metabolic flexibility of Candida auris. Additionally, Antibiofilm agent-12 demonstrates antifungal activity in a Candida auris-infected C. elegans model .
|
-
- HY-19895
-
|
Bacterial
|
Infection
|
DS-8587 is a new fluoroquinolone with significant antibacterial activity. The MIC value of DS-8587 against clinically isolated amoxicillin-resistant Bacillus strains is superior to ciprofloxacin and levofloxacin. The antibacterial activity of DS-8587 is less affected by adeA/adeB/adeC or abeM efflux pumps, and has more advantages than ciprofloxacin. DS-8587 has a lower single-step mutation frequency than ciprofloxacin. DS-8587 may be an effective drug for inhibiting amoxicillin-resistant Bacillus infections .
|
-
- HY-149360
-
|
P-glycoprotein
|
Cancer
|
P-gb-IN-1 (compound Ⅲ-8), a 2,5-disubstituted furan derivative, is a highly effective, broadspectrum P-glycoprotein (P-gp) inhibitor. P-gb-IN-1 displayed the reversal activity by inhibiting P-gp efflux. P-gb-IN-1 has a potent affinity to P-gp by forming H-bond interactions with residues Asn 721 and Met 986. P-gb-IN-1 possesses broad-spectrum reversal activity and low toxicity in MCF-7/ADR cells .
|
-
- HY-108694
-
|
Endogenous Metabolite
NF-κB
|
Metabolic Disease
Inflammation/Immunology
|
γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment .
|
-
- HY-108694R
-
|
Endogenous Metabolite
NF-κB
|
Metabolic Disease
Inflammation/Immunology
|
γ-Tocotrienol (Standard) is the analytical standard of γ-Tocotrienol. This product is intended for research and analytical applications. γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment .
|
-
- HY-165061
-
Sciadonic acid
|
Apolipoprotein
|
Inflammation/Immunology
|
5(Z),11(Z),14(Z)-Eicosatrienoic acid (Sciadonic acid), a polyunsaturated fatty acid sourced from maritime pine seed oil, gymnospermae leaves and seeds, and freshwater gastropods, has been shown to reduce high-density lipoprotein and ApoA1 levels in transgenic mice expressing human ApoA1 when included in their diet. In vitro studies indicate that it diminishes cholesterol efflux, and when applied topically in its methyl ester form, it alleviates inflammatory processes, likely by displacing arachidonic acid from phospholipid pools and lowering concentrations of downstream inflammatory mediators such as prostaglandin E2 and leukotrienes.
|
-
- HY-N0686
-
-
- HY-N0686R
-
|
Fatty Acid Synthase (FASN)
MicroRNA
|
Metabolic Disease
|
Pseudoprotodioscin (Standard) is the analytical standard of Pseudoprotodioscin. This product is intended for research and analytical applications. Pseudoprotodioscin, a furostanoside, inhibits SREBP1/2 and microRNA 33a/b levels and reduces the gene expression regarding the synthesis of cholesterol and triglycerides .
|
-
- HY-139426
-
ML-SI3
3 Publications Verification
ML-SI3 (cis/trans mix)
|
Parasite
TRP Channel
|
Cardiovascular Disease
Neurological Disease
|
ML-SI3 is a mixture of cis/trans ML-SI3 (HY-139426A), which is a TRPML1/2 channel inhibitor with IC50s of 4.7 μM and 1.7 μM, respectively. ML-SI3 also inhibits lysosomal calcium efflux and blocks downstream TRPML1-mediated autophagy. The cis/trans ML-SI3 (HY-139426A) components of ML-SI3 are TRPML2 activators with EC50s of 3.3 μM and 9.4 μM, respectively .
|
-
- HY-129262
-
|
Antibiotic
Bacterial
|
Infection
|
Deoxypheganomycin D is a specific antimycobacterial inhibitor with no cross-resistance to other antibiotics such as Paromomycin (HY-B0956), Capreomycin (HY-P3270), Viomycin (HY-A0155), Streptothricin (HY-129065), Kanamycin (HY-16566), and Streptomycin (HY-B1906). Deoxypheganomycin D (28 μM) partially inhibits the growth of Mycobacterium 607, with no significant inhibitory effects on DNA, RNA, or protein synthesis. Deoxypheganomycin D (7 μM) affects leucine influx, not thymidine, and has the opposite effect on efflux. The effects of Deoxypheganomycin D may be related to cell membrane and specific mycobacterial lipid components.
|
-
- HY-N4314
-
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) .
|
-
- HY-N4314R
-
|
Bacterial
COX
NO Synthase
NF-κB
|
Infection
Inflammation/Immunology
Cancer
|
Scutellarein tetramethyl ether (Standard) is the analytical standard of Scutellarein tetramethyl ether. This product is intended for research and analytical applications. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive compound extracted from Eupatorium odoratum. Scutellarein tetramethyl ether exhibits anti-inflammatory, antibacterial, pro-coagulant, and anti-tumor activities. Scutellarein tetramethyl ether exerts its anti-inflammatory effects by modulating the NF-κB pathway and regulates bacterial resistance through the inhibition of efflux pumps. Additionally, Scutellarein tetramethyl ether accelerates coagulation time via the endogenous coagulation pathway. Studies have shown that Scutellarein tetramethyl ether can effectively inhibit the growth of the liver cancer cell line HepG2 (IC50= 20.08 μg/mL) .
|
-
- HY-124187
-
Ethyl pinolenate
|
Biochemical Assay Reagents
|
Others
|
Pinolenic acid is a polyunsaturated fatty acid found in the seed oils of red pine (Pinus orientalis) and maritime pine (Pinus pinaster). Both oils were found to have lipid-lowering properties. A diet containing marine pine nut oil (MPSO) reduces HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to reduce cholesterol efflux in vitro. Korean pine nut oil supplements may help obesity by reducing appetite. People who take this oil experience an increase in the satiety hormones CCK and GLP-1 and a decrease in appetite. The activity of the oil is attributed to pinolenic acid. Pinolenic acid is not metabolized to arachidonic acid and can reduce the level of arachidonic acid in the phosphatidylinositol fraction of HepG2 cells from 15.9% to 7.0%. Pinolenic acid ethyl ester is a neutral, more lipophilic form of the free acid.
|
-
- HY-101453
-
|
P-glycoprotein
|
Cancer
|
Ceefourin 1 is a potent and highly selective multidrug resistance protein 4 (MRP4) inhibitor. Ceefourin 1 inhibits transport of a broad range of MRP4 substrates, yet is highly selective for MRP4 over other ABC transporters. Ceefourin 1 is a benzothiazol and primarily as a chemosensitizer for high-risk neuroblastoma .
|
-
- HY-138074
-
5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime
|
Parasite
|
Infection
|
Milbemycin A4 oxime (5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime) is a derivative of Milbemycin A4 (HY-126906) and a component of Milbemycin oxime (HY-B0778), both of which have insecticidal and nematicidal activities. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae in naturally infected dogs with D. immitis and inhibits the growth of clinical isolates of Candida glabrata (MIC80=16-32 μg/mL). Milbemycin A4 oxime (2.5 μg/mL) blocks the efflux of Fluconazole (HY-B0101) from clinical isolates of Candida glabrata. Milbemycin A4 oxime enhances doxorubicin-induced cell growth inhibition and increases the intracellular accumulation of doxorubicin and P-glycoprotein substrate Rhodamine 123 (HY-D0816) in doxorubicin-resistant but not sensitive MCF-7 breast cancer cells in a concentration-dependent manner.
|
-
- HY-W013712
-
|
Potassium Channel
|
Neurological Disease
|
GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels, with an EC50 of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect .
|
-
- HY-W127487
-
|
Biochemical Assay Reagents
|
Others
|
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.
|
-
-
-
HY-L049
-
|
1,525 compounds
|
Antibacterial agents are a group of materials that fight against pathogenic bacteria. Thus, by killing or reducing the metabolic activity of bacteria, their pathogenic effect in the biological environments will be minimized. The most widely used antibacterial agents exert their effects on bacterial cell wall synthesis, protein synthesis, DNA replication and metabolic pathways. However, resistance to antimicrobial agents has become a major source of morbidity and mortality worldwide. The main mechanisms of resistance are limiting uptake of a drug, modification of a drug target, inactivation of a drug, and active efflux of a drug. Therefore, it is an urgent need to develop new drugs targeted at resistant organisms.
MCE offers a unique collection of 1,525 compounds with validated antibacterial activities. MCE antibacterial compound library is an effective tool for drug repurposing screening, combination screening and biological investigation.
|
-
-
HY-L048
-
|
409 compounds
|
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 409 compounds with validated antifungal activities. MCE antifungal compound library is an effective tool for drug repurposing screening, combination screening and biological investigation.
|
-
-
HY-L169
-
|
456 compounds
|
Resistance refers to the decrease in the effectiveness of drugs in treating diseases or symptoms. Due to the increasing global antibiotic resistance, it may threaten our ability to treat common infectious diseases. Drug resistance is also the main cause of chemotherapy failure in malignant tumors. In approximately 50% of cases, drug resistance exists even before chemotherapy begins. There are many mechanisms of anticancer drug resistance, including increased protein expression that leads to drug removal, mutations in drug binding sites, recovery of tumor protein production, and pre-existing genetic heterogeneity in tumor cell populations. In addition, the issue of drug resistance seems to have affected the development of new anticancer drugs. Drug resistance may be caused by various conditions, such as mutations, epigenetic modifications, and upregulation of drug efflux protein expression. Overcoming multidrug resistance in cancer treatment is becoming increasingly important.
MCE designs a unique collection of 456 anti-drug-resistant compounds. It is a good tool to be used for research on cancer and other diseases.
|
Cat. No. |
Product Name |
Type |
-
- HY-D2262
-
|
Dyes
|
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) .
|
-
- HY-D2341
-
|
Fluorescent Dyes/Probes
|
6FC-GABA-Taxol is a fluorescent probe with cell permeability, which is formed by connecting 6FC to the anticancer drug Taxol (HY-B0015) via γ-aminobutyric acid (GABA). 6FC-GABA-Taxol can bind to microtubules in living cells and image them through confocal microscopy. Additionally, 6FC-GABA-Taxol enables the quantification of microtubule binding using flow cytometry without the addition of efflux inhibitors .
|
Cat. No. |
Product Name |
Type |
-
- HY-P3267A
-
|
Native Proteins
|
Apo-Bovine Transferrin refers to iron free Transferrin (HY-P3267), serves as Transferrin receptor ligand and mediates iron release from endothelial cells. Apo-Transferrin indicates an iron deficient environment, can directly bind to hephaestin, which can convert Fe 2+ to Fe 3+. Apo-Transferrin mediates iron efflux most likely in cooperation with ferroportin 1. Apo-Bovine Transferrin can be used in neuroretinal research .
|
-
- HY-124187
-
Ethyl pinolenate
|
Drug Delivery
|
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.
|
-
- HY-NP011A
-
|
Native Proteins
|
Apo-Human transferrin (suitable for cell culture) refers to iron free Transferrin (HY-P3267), serves as Transferrin receptor ligand and mediates iron release from endothelial cells. Apo-Transferrin indicates an iron deficient environment, can directly bind to hephaestin, which can convert Fe 2+ to Fe 3+. Apo-Transferrin mediates iron efflux most likely in cooperation with ferroportin 1 .
|
-
- HY-W127487
-
|
Drug Delivery
|
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.
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- 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 .
|
-
- HY-P2624A
-
|
PAK
|
Metabolic Disease
|
st-Ht31 ammonium is a membrane-permeable peptide inhibitor of?protein kinase A (PKA) anchoring. st-Ht31 ammonium induces robust cholesterol/phospholipid efflux. st-Ht31 ammonium completely reverses foam cell formation and restores the metabolic health of macrophage .
|
-
- HY-P1649B
-
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 .
|
-
- HY-P10874
-
|
Bacterial
|
Infection
|
SMR efflux inhibitor targets the small multidrug resistance (SMR) efflux pump, blocks the interaction of TM4-TM4, and exhibits board-spectrum antibacterial activity .
|
-
- HY-P10551
-
|
Transmembrane Glycoprotein
NF-κB
TNF Receptor
|
Cardiovascular Disease
|
Apo A-I mimetic 5A peptide is a synthetic peptide molecule designed based on the structure and function of naturally occurring apolipoprotein A-I (Apo A-I). Apo A-I mimetic 5A peptide can promote the efflux of cholesterol from cells and help reduce the accumulation of cholesterol in cells. Apo A-I mimetic 5A peptide also shows anti-inflammatory activity and can reduce inflammatory markers in blood and tissues. Apo A-I mimetic 5A peptide can be used in the study of cardiovascular diseases .
|
-
- HY-P5901
-
-
- 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 .
|
-
- HY-P10811
-
XIP
|
Na+/Ca2+ Exchanger
|
Neurological Disease
|
Na +-Ca 2+ Exchanger inhibitory peptide (XIP) is a Na +-Ca 2+ exchanger inhibitor with a Ki of 200 nM. Na +-Ca 2+ Exchanger inhibitory peptide inhibits the Na +-dependent Ca 2+ uptake and the Na +-dependent Ca 2+ efflux of sarcolemmal vesicles in a noncompetitive manner .
|
-
- 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 .
|
-
- 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) .
|
-
- HY-P1649
-
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 .
|
-
- HY-P1649A
-
NAB741 TFA
|
Bacterial
Antibiotic
|
Infection
|
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-N3308
-
-
-
- HY-N2419
-
-
-
- HY-N0406
-
-
-
- HY-N2947R
-
-
-
- HY-122416
-
-
-
- HY-N11697
-
-
-
- HY-N9947
-
-
-
- HY-129279
-
-
-
- HY-N12171
-
-
-
- HY-126940
-
-
-
- HY-N2419R
-
-
-
- HY-N10512
-
-
-
- HY-N4104
-
-
-
- HY-N10069
-
-
-
- HY-N12320
-
-
-
- HY-N0076
-
-
-
- HY-N0246
-
-
-
- HY-N12235
-
-
-
- HY-N9947A
-
-
-
- HY-N15297
-
-
-
- HY-N0406R
-
|
Structural Classification
Flavonoids
other families
Source classification
Plants
Isoflavones
|
Others
|
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 .
|
-
-
- HY-N0076R
-
-
-
- HY-N0246R
-
-
-
- HY-108694
-
-
-
- HY-108694R
-
-
-
- HY-N0686
-
-
-
- HY-N0686R
-
-
-
- HY-N4314
-
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) .
|
-
-
- HY-N4314R
-
|
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) .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-113365S
-
|
Cholestenone-d5 is the deuterium labeled Cholestenone. 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[1][2][3].
|
-
-
- HY-113365S1
-
|
Cholestenone- 13C is the 13C labeled Cholestenone. 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[1][2][3].
|
-
-
- HY-135328S
-
|
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].
|
-
-
- HY-113365S2
-
|
Cholestenone- 13C2 is the 13C labeled Cholestenone. 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[1][2][3].
|
-
-
- HY-B0777S
-
|
Moxidectin-d3 (CL-301423-d3) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
|
-
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