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Results for "

Efflux pump

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) ADC Payload (2) Antibiotic (6) Apoptosis (1) Bacterial (32) Biochemical Assay Reagents (1) Calcium Channel (4) COX (2) Dopamine Receptor (2) Drug Derivative (2) Drug Metabolite (4) FOXO (2) Fungal (2) Histamine Receptor (2) Isotope-Labeled Compounds (1) MDM-2/p53 (3) Microtubule/Tubulin (1) NF-κB (4) NO Synthase (2) P-glycoprotein (12) Parasite (7) Protein Arginine Deiminase (2) Reactive Oxygen Species (ROS) (3) Reference Standards (5) Topoisomerase (1) VEGFR (1)
By Research Areas:	Cancer (11) Cardiovascular Disease (4) Infection (39) Inflammation/Immunology (9) Neurological Disease (5)

By Targets:

5-HT Receptor (2)

ADC Payload (2)

Antibiotic (6)

Apoptosis (1)

Bacterial (32)

Biochemical Assay Reagents (1)

Calcium Channel (4)

COX (2)

Dopamine Receptor (2)

Drug Derivative (2)

Drug Metabolite (4)

FOXO (2)

Fungal (2)

Histamine Receptor (2)

Isotope-Labeled Compounds (1)

MDM-2/p53 (3)

Microtubule/Tubulin (1)

NF-κB (4)

NO Synthase (2)

P-glycoprotein (12)

Parasite (7)

Protein Arginine Deiminase (2)

Reactive Oxygen Species (ROS) (3)

Reference Standards (5)

Topoisomerase (1)

VEGFR (1)

By Research Areas:

Cancer (11)

Cardiovascular Disease (4)

Infection (39)

Inflammation/Immunology (9)

Neurological Disease (5)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Proton Pump Na+/K+ ATPase

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-Y1777

2-Phenylacetophenone	Drug Derivative	Infection
2-Phenylacetophenone has broad-spectrum efflux pump inhibition activity. 2-Phenylacetophenone is a benzoin derivative used as a photoinitiator in vinyl polymerization .

HY-156753

NorA-IN-1	Bacterial	Cancer
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 .

HY-149812

AcrB-IN-4	Bacterial Parasite	Infection
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 .

HY-149811

AcrB-IN-3	Bacterial Parasite	Infection
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 .

HY-168955

Antibacterial agent 269	Bacterial	Infection Inflammation/Immunology
Antibacterial agent 269 (3.8) is an inhibitor of AdeG Efflux Pumps in Acinetobacter baumannii .

HY-Y1777R

2-Phenylacetophenone (Standard)	Drug Derivative	Infection
2-Phenylacetophenone has broad-spectrum efflux pump inhibition activity. 2-Phenylacetophenone is a benzoin derivative used as a photoinitiator in vinyl polymerization .

HY-149810

AcrB-IN-2	Bacterial Parasite	Infection
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 .

HY-N2947

Boeravinone B	P-glycoprotein	Infection Inflammation/Immunology
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 .

HY-N2947R

Boeravinone B (Standard)	Reference Standards P-glycoprotein	Infection Inflammation/Immunology
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 .

HY-163473

IITR08367	Bacterial	Infection
IITR08367 is a potent effector pump *Acinetobacter baumannii Fosfomycin Efflux* pump (AbaF) inhibitor for enhancing the antimicrobial activity of Fosfomycin (HY-B1075A) against Acinetobacter baumannii**. IITR08367 acts by interfering with Fosfomycin/H ⁺ reverse transporter activity. .

HY-101444A

PAβN dihydrochloride Maximum Cited Publications 9 Publications Verification MC-207,110 dihydrochloride; Phe-Arg-β-naphthylamide dihydrochloride	Bacterial	Infection
PAβN dihydrochloride (MC-207110 dihydrochloride) is an **efflux pump** inhibitor.

HY-13766A

Timcodar mesylate VX-853-2	Bacterial	Others
Timcodar mesylate (VX-853-2) and its analog VX-710 are mammalian multidrug-resistant bacterial efflux pump inhibitors that directly inhibit ethidium bromide efflux in Staphylococcus aureus. Timcodar mesylate has the potential to enhance antibiotic activity by inhibiting bacterial efflux pumps, effectively reducing the minimum inhibitory concentration of some antibiotics against Gram-positive pathogens such as Staphylococcus aureus, Enterococcus and Streptococcus pneumoniae .

HY-124819

D13-9001	Bacterial	Infection
D13-9001 is a potent AcrB (AcrAB-TolC efflux pump subunit) and MexB (MexAB-OprM efflux pump subunit) inhibitor with the K_D values of 1.15 μM and 3.57 μM in E. coli and P. aeruginosa, respectively . D13-9001 exhibits antibiotic activities .

HY-P10874

SMR efflux inhibitor	Bacterial	Infection
SMR efflux inhibitor targets the small multidrug resistance (SMR) efflux pump, blocks the interaction of TM4-TM4, and exhibits board-spectrum antibacterial activity .

HY-157533

AcrB-IN-5	Bacterial	Others
AcrB-IN-5 (compound 8) inhibits AcrB and blocks the efflux pump in a dose-dependent manner .

HY-119172

NSC-60339	Bacterial	Infection Inflammation/Immunology Cancer
NSC-60339, an **efflux pump** inhibitor and a substrate of AcrAB-TolC, is a polybasic terephthalic acid derivative studied as a potential cancer chemotherapeutic agent .

HY-N11697

α-Cryptoxanthin	P-glycoprotein	Cancer
α-Cryptoxanthin is a natural carotenoid with anticancer effects. α-Cryptoxanthin inhibits multidrug resistance 1 (MDR1) mediated efflux pump .

HY-163454

NorA-IN-2	Bacterial	Infection
NorA-IN-2 (compound DZ-3) is a potent NorA inhibitor. NorA-IN-2 shows NorA efflux pump inhibitors (EPI) activity .

HY-157987

MBX3135	Bacterial	Infection
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 .

HY-172348

BRD-9327	Antibiotic	Infection
BRD-9327 is an inhibitor of EfpA. BRD-9327 binds in the outer vestibule without complete blockade of the substrate path to the outside, suggesting its possible inhibition of the movement necessary for alternate access of the transporter. BRD-9327 can be used for anti-tuberculosis study .

HY-162144

BDM91288	Bacterial	Infection
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 .

HY-155048

BDM91270	Bacterial	Infection
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 .

HY-N12171

Isoreserpiline	Bacterial	Infection Neurological Disease
Isoreserpiline is an orally active and BBB-penetrable indole alkaloids with antibacterial and antipsychotic activity. Isoreserpiline is even more effective when used in combination with antibiotics and inhibits the activity of bacterial efflux pumps. Isoreserpiline improves Amphetamine-induced hyperactivity in mice .

HY-119172R

NSC-60339 (Standard)	Bacterial	Infection Inflammation/Immunology Cancer
NSC-60339 (Standard) is the analytical standard of NSC-60339. This product is intended for research and analytical applications. NSC-60339, an efflux pump inhibitor and a substrate of AcrAB-TolC, is a polybasic terephthalic acid derivative studied as a potential cancer chemotherapeutic agent .

HY-100750

Norverapamil hydrochloride 1 Publications Verification (±) -Norverapamil hydrochloride; D591 hydrochloride	Calcium Channel P-glycoprotein Drug Metabolite	Cardiovascular Disease
Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .

HY-100750R

Norverapamil hydrochloride (Standard) (±)-Norverapamil hydrochloride (Standard); D591 hydrochloride (Standard)	Reference Standards Calcium Channel P-glycoprotein Drug Metabolite	Cardiovascular Disease
Norverapamil (hydrochloride) (Standard) is the analytical standard of Norverapamil (hydrochloride). This product is intended for research and analytical applications. Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2].

HY-135328

Norverapamil (±)-Norverapamil; D591	Calcium Channel P-glycoprotein Drug Metabolite	Cardiovascular Disease
Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .

HY-42034

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

HY-17390A

Loxapine succinate	5-HT Receptor Dopamine Receptor	Infection Neurological Disease
Loxapine succinate is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistant Salmonella enterica serovar Typhimurium in macrophages .

HY-42034R

Hydroquinine (Standard) Dihydroquinine (Standard)	Reference Standards Bacterial Parasite Reactive Oxygen Species (ROS) Protein Arginine Deiminase	Inflammation/Immunology
Hydroquinine (Standard) is the analytical standard of Hydroquinine. 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 .

HY-162822

P-gp modulator-5	P-glycoprotein	Cancer
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 .

HY-W107077

INF55	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-174454

Antitrypanosomal agent 24	P-glycoprotein	Infection
Antitrypanosomal agent 24 is a benzothiazole amidoxime with strong and selective antitrypanosomal activity (IC₅₀ = 0.92 μM). Antitrypanosomal agent 24 is a substrate of the P-glycoprotein efflux pump. Antitrypanosomal agent 24 has high membrane permeability and good metabolic stability. Antitrypanosomal agent 24 binds to DNA/RNA by intercalation .

HY-120574

TH1338	ADC Payload Topoisomerase	Cancer
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 .

HY-146389

Anticancer agent 50	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-135328S

Norverapamil-d7 (±)-Norverapamil-d₇; D591-d₇	Isotope-Labeled Compounds Calcium Channel P-glycoprotein Drug Metabolite	Cardiovascular Disease
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 .

HY-N12320

Majoranaquinone	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-N10069

Bonducellin	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-102008

LBM-415 NVP-PDF 713; VIC-104959	Bacterial Antibiotic	Infection
LBM-415 (NVP-PDF 713) is a peptide deformylase (PDF) inhibitor that exhibits inhibitory activity against various antimicrobial-resistant gram-positive cocci, with a MIC₉₀ range of 0.12-8 µg/ml. Additionally, inhibiting efflux pump activity can enhance bacterial sensitivity to LBM415, thereby improving its antibacterial efficacy .

HY-144880

SC209 3-Aminophenyl Hemiasterlin	ADC Payload Microtubule/Tubulin P-glycoprotein	Cancer
SC209 (3-Aminophenyl Hemiasterlin) is a 3-aminophenyl hemiasterlin derivative that serves as a cytotoxin for ADCs, targeting tubulin. SC209 has reduced potential for drug efflux via P-glycoprotein 1 drug pump compared with other tubulin-targeting payloads. SC209 exhibits antitumor activity and can be used in the synthesis of ADC molecules .

HY-17390AR

Loxapine succinate (Standard)	Reference Standards 5-HT Receptor Dopamine Receptor	Infection Neurological Disease
Loxapine (succinate) (Standard) is the analytical standard of Loxapine (succinate). This product is intended for research and analytical applications. Loxapine succinate is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistant Salmonella enterica serovar Typhimurium in macrophages .

HY-107566

Conessine	Histamine Receptor Parasite MDM-2/p53 NF-κB FOXO Bacterial	Infection Neurological Disease
Conessine is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pK_i 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 .

HY-P5589

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

HY-107566A

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

HY-P1649B

SPR741 acetate 3 Publications Verification 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-P1649

SPR741 3 Publications Verification 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

SPR741 TFA 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-155198

Antifungal agent 72	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 (K_i: 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-19895

DS-8587	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-168077

Antibiofilm agent-12	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 .

Cat. No.	Product Name

HY-L048

Antifungal Compound Library

453 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 453 compounds with validated antifungal activities. MCE antifungal compound library is an effective tool for drug repurposing screening, combination screening and biological investigation.

HY-L919

MCE CNS BBB Lead-like Library

28,715 compounds

With the aging population and increasing competitive pressures, neurodegenerative diseases of the central nervous system (CNS) have become a serious medical challenge in modern society, including Parkinson's disease, Alzheimer's disease, brain tumors, and multiple sclerosis. However, the success rate of CNS drug development remains remarkably low, primarily due to the blood-brain barrier (BBB). The blood-brain barrier (BBB) is a semipermeable barrier structure that surrounds the microvasculature of the CNS. In capillaries, the wedged endothelial cells are tightly packed and wedge-shaped, lining the interior of the vessels to form extensive tight junctions. Along with a range of receptors, transporters, efflux pumps, and other cellular components, this barrier regulates the entry and exit of molecules between the bloodstream and the brain. The intact BBB blocks the passage of most blood-borne substances into the brain, preventing nearly 100% of large-molecule drugs and over 98% of small-molecule drugs from entering. Compared to non-CNS drugs, physicochemical properties such as hydrogen bonds, lipophilicity, and molecular weight significantly influence a compound's ability to cross the BBB. Using artificial intelligence (AI) algorithms to predict BBB permeability, a predicted value greater than 0.75 indicates that the compound has strong potential to cross the BBB, providing a promising starting point for CNS drug discovery.

Cat. No.	Product Name	Type

HY-W127487

N-Octadecanoyl-L-homoserine lactone

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