101 Results for "

efflux activity

" in MedChemExpress (MCE) Product Catalog:
Products (101)

101 Results for "efflux activity" in MCE Product Catalog:

5
5 Cited Publications
Cat. No.: HY-N4314
CAS No.: 1168-42-9
Synonyms: 4',5,6,7-Tetramethoxyflavone
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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4
4 Cited Publications
Cat. No.: HY-108694
CAS No.: 14101-61-2
Purity:  99.67%
γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment .
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2
2 Cited Publications
Cat. No.: HY-107643
CAS No.: 313397-13-6
Purity:  99.90%
Synonyms: CBLC4H10
Target:  

P-glycoprotein

Research Areas:  

Cancer

Reversan (CBLC4H10) inhibits drug efflux mediated by P-glycoprotein (Pgp) and multidrug resistance protein 1 (MRP1), and exhibits oral activity. Reversan shows activity against glioblastoma multiforme and neuroblastoma models .
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2
2 Cited Publications
Cat. No.: HY-N10455
CAS No.: 72050-71-6
Synonyms: 24-epi-Castasterone
24-Epicastasterone (24-epi-Castasterone) is a bioactive brassinosteroid and a ligand of ABCB1 and ABCB19 in Arabidopsis thaliana. 24-Epicastasterone stimulates the ATPase activity of ABCB19 and the ATP hydrolysis activity of ABCB1, which drive the efflux of substances from plant cells. 24-Epicastasterone increases the activities of catalase and guaiacol peroxidase in the roots of wheat seedlings. 24-Epicastasterone alleviates heat-induced lipid peroxidation through a ROS-dependent mechanism and enhances the heat tolerance of common wheat seedlings .
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2
2 Cited Publications
Cat. No.: HY-137433
CAS No.: 1835667-63-4
Purity:  99.86%
Synonyms: D-0316
Research Areas:  

Cancer

Befotertinib (D-0316) is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib selectively targets EGFR mutations including EGFR T790M, EGFR L858R and delE746-A750, forms covalent bonds with EGFR C797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib can be used in research related to multidrug-resistant cancers and non-small cell lung cancer .
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1
1 Cited Publications
Cat. No.: HY-17390A
CAS No.: 27833-64-3
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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1
1 Cited Publications
Cat. No.: HY-N0468
CAS No.: 63279-13-0
Rebaudioside D is an orally active sweetener that targets and activates FXR, modulates Acetyl-CoA Carboxylase, and inhibits 3-hydroxy-3-methylglutaryl-CoA reductase. Rebaudioside D regulates bile acid homeostasis and lipid metabolism, reduces the synthesis rates of fatty acids and cholesterol, and exerts multiple effects including anti-adipogenesis, hepatoprotection, anti-steatosis, gut microbiota modulation, enhancement of secondary bile acid metabolism, anti-endotoxin activity, regulation of bile acid transport, and inhibition of bile acid efflux. Rebaudioside D also reduces body weight gain, visceral fat accumulation, hepatic triglyceride and cholesterol accumulation, hepatic lipid peroxidation, and decreases the circulating level of lipopolysaccharide-binding protein. Rebaudioside D additionally enhances the secondary bile acid metabolic pathway of intestinal bacteria, upregulates the gene expression of ileal organic solute transporter α, and downregulates the gene expression of hepatic bile salt export pump. Rebaudioside D does not affect glucose homeostasis, alter total caloric intake or fecal energy excretion, induce weight gain, exacerbate obesity, promote hepatic steatosis, impair brown adipose tissue function, nor change skeletal muscle metabolism-related proteins. Rebaudioside D can be used in diet-induced obesity and obesity-related research .
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1
1 Cited Publications
Cat. No.: HY-13451
CAS No.: 209342-40-5
Purity:  98.75%
Category:  

Natural Products

Target:  

Antibiotic Bacterial

Finafloxacin is an orally active fourth-generation fluoroquinolone broad-spectrum antibiotic. Finafloxacin exhibits stronger antibacterial activity in acidic pH environments and is not easily affected by bacterial multidrug efflux transporters. Finafloxacin is effective against a variety of extracellular pathogenic bacteria, and can also accumulate in macrophages, showing excellent antibacterial activity against intracellular Staphylococcus aureus, Listeria monocytogenes, Legionella pneumophila, Burkholderia pseudomallei, and other pathogens. Finafloxacin has been approved by the U.S. FDA for research on acute otitis externa mediated by Pseudomonas aeruginosa. Finafloxacin is also used in studies related to diseases such as melioidosis, inhalational tularemia, and inhalational plague .
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Cat. No.: HY-171099
CAS No.: 2245949-62-4
Synonyms: LI-2124
Target:  

IPK Superfamily

SC-919 is an orally active IP6K inhibitor, with an IC50 of < 5.2 nM against IP6K1, < 3.8 nM against IP6K2, and 0.65 nM against IP6K3. By inhibiting the activity of IP6K, SC-919 reduces intracellular IP7 levels, thereby suppressing XPR1-mediated cellular phosphate efflux. SC-919 increases intracellular phosphate and ATP levels while reducing phosphate entry into the bloodstream, thus decreasing plasma phosphate levels. SC-919 can be used in research related to chronic kidney disease and hyperphosphatemia .
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Cat. No.: HY-B0501
CAS No.: 119478-55-6
Synonyms: CP 76136-27
Research Areas:  

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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Cat. No.: HY-42034
CAS No.: 522-66-7
Synonyms: Dihydroquinine
Hydroquinine (Dihydroquinine) is an anti-bacterial agent that inhibits both Gram-positive and Gram-negative bacteria. Hydroquinine inhibits the growth of multidrug-resistant pseudomonas aeruginosa via the suppression of the arginine deiminase pathway genes. Hydroquinine inhibits Plasmodium falciparum and Plasmodium berghei. Hydroquinine displays anti-malarial and demelanizing activities. Hydroquinine effectively induces specific RND-type efflux pump systems in Pseudomonas aeruginosa, particularly the MexCD-OprJ and MexXY efflux pumps. Hydroquinine inhibits Pseudomonas aeruginosa adhesion and biofilm formation. Hydroquinine serves as a precursor for derivatives such as C9 epihydroquinine, 9-acetoxy-10,11-dihydroquinine, and 10,11-dihydroquinine monohydrochloride .
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Cat. No.: HY-107566
CAS No.: 546-06-5
Purity:  99.87%
Conessine is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pKi values of Conessine for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine has antimalarial activity. Conessine can also be used in the research of muscle atrophy .
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Cat. No.: HY-15134
CAS No.: 216227-54-2
Purity:  99.21%
Synonyms: OC 144-093; OC 144093
Target:  

P-glycoprotein

Research Areas:  

Infection Cancer

ONT-093 (OC 144-093) is a potent and orally active inhibitor of P-glycoprotein pump. ONT-093 inhibits P-gp-mediated ATPase activity with an IC50 of 0.16 μM. ONT-093 can inhibit drug efflux and increase bioavailability. ONT-093 reverses cancer cells multidrug resistance to chemotherapeutic drugs. ONT-093 can be used for the researches of cancer and infection, such as colon cancer and malarial .
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Cat. No.: HY-B0380
CAS No.: 39133-31-8
Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
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Cat. No.: HY-B0380A
CAS No.: 34140-59-5
Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
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Cat. No.: HY-P10551
ApoA-I mimetic peptide 5A is a synthetic peptide molecule designed based on the structure and function of naturally occurring apolipoprotein A-I (Apo A-I). ApoA-I mimetic peptide 5A can promote the efflux of cholesterol from cells and help reduce the accumulation of cholesterol in cells. ApoA-I mimetic peptide 5A also shows anti-inflammatory activity and can reduce inflammatory markers in blood and tissues. ApoA-I mimetic peptide 5A can be used in the study of cardiovascular diseases .
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Cat. No.: HY-124819
CAS No.: 957471-96-4
Target:  

Bacterial

Research Areas:  

Infection

D13-9001 is a potent AcrB (AcrAB-TolC efflux pump subunit) and MexB (MexAB-OprM efflux pump subunit) inhibitor with the KD values of 1.15 μM and 3.57 μM in E. coli and P. aeruginosa, respectively . D13-9001 exhibits antibiotic activities .
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Cat. No.: HY-Y1777
CAS No.: 451-40-1
Target:  

Drug Derivative

Research Areas:  

Infection

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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Cat. No.: HY-144880
CAS No.: 1977557-86-0
Purity:  99.52%
Synonyms: 3-Aminophenyl Hemiasterlin
Research Areas:  

Cancer

SC209 (3-Aminophenyl Hemiasterlin) is a 3-aminophenyl hemiasterlin derivative that serves as a cytotoxin for ADCs, targeting tubulin. SC209 has reduced potential for drug efflux via P-glycoprotein 1 drug pump compared with other tubulin-targeting payloads. SC209 exhibits antitumor activity and can be used in the synthesis of ADC molecules .
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Cat. No.: HY-P5589
CAS No.: 131463-18-8
Synonyms: PlnA
Plantaricin A is an antimicrobial peptide that can be derived from Lactobacillus plantarum. Plantaricin A has a synergistic effect with Ciprofloxacin. Plantaricin A shows anti-microbial activity. Plantaricin A increases the membrane potential of S. aureus and the level of intracellular ROS. Plantaricin A inhibits the function of the efflux pump by binding it and altering the structure of MepA, NorA, and LmrS. Plantaricin A significantly relieves inflammation, and promotes wound healing. Plantaricin A permeabilizes cancerous rat pituitary cells [1][2].
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