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efflux transport

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20

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2

Biochemical Assay Reagents

3

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2

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-W020012
    Fluoresterol

    22-NBD Cholesterol

    		 Fluorescent Dye Metabolic Disease
    Fluoresterol (22-NBD Cholesterol) is a cholesterol-specific fluorescent probe with cholesterol-mimicking binding properties. Fluoresterol is ineffective orally and does not cross the blood-brain barrier. Fluoresterol specifically binds to cholesterol transport-related proteins (such as ABCA1 and ABCG1) and is primarily used in cholesterol metabolism research, particularly for the visualization and quantitative analysis of cholesterol absorption, efflux, intracellular transport efficiency, and reverse cholesterol transport (RCT) processes. The commonly used concentration of Fluoresterol in in vitro experiments is 0.1-10 μM, and the commonly used dose in in vivo experiments is 5-20 mg/kg (gavage or intraperitoneal injection), with excitation/emission wavelengths of 472/540 nm. Fluoresterol can be applied to the study of cholesterol metabolism mechanisms related to hyperlipidemia, atherosclerosis, and non-alcoholic fatty liver disease (NAFLD) .
    Fluoresterol
  • HY-D0180
    18-Crown-6-ether

    18C6; 1,4,7,10,13,16-Hexaoxacyclooctadecane

    		 Bacterial Infection
    18-Crown-6-ether is a type of crown ether compound and a specific structure dissociating agent. 18-Crown-6-ether can compete with K + for binding to G-quadruplexes, disrupting their stable structure to regulate the functions of related systems. 18-Crown-6-ether combines with K + and other metal ions to achieve precise ion transmembrane transport. 18-Crown-6-ether can act as an "susceptibility substrate" for the multi-drug efflux pump EmrE (a bacterial multidrug resistance transporter), ultimately inhibiting bacterial growth. 18-Crown-6-ether can be used in microcapsule controlled release and the research on developing antibacterial enhancers .
    18-Crown-6-ether
  • HY-N0468
    Rebaudioside D
    1 Publications Verification

    		 FXR Acetyl-CoA Carboxylase Metabolic Disease
    Rebaudioside D is an orally active sweetener that targets and activates FXR, modulates Acetyl-CoA Carboxylase, and inhibits 3-hydroxy-3-methylglutaryl-CoA reductase. Rebaudioside D regulates bile acid homeostasis and lipid metabolism, reduces the synthesis rates of fatty acids and cholesterol, and exerts multiple effects including anti-adipogenesis, hepatoprotection, anti-steatosis, gut microbiota modulation, enhancement of secondary bile acid metabolism, anti-endotoxin activity, regulation of bile acid transport, and inhibition of bile acid efflux. Rebaudioside D also reduces body weight gain, visceral fat accumulation, hepatic triglyceride and cholesterol accumulation, hepatic lipid peroxidation, and decreases the circulating level of lipopolysaccharide-binding protein. Rebaudioside D additionally enhances the secondary bile acid metabolic pathway of intestinal bacteria, upregulates the gene expression of ileal organic solute transporter α, and downregulates the gene expression of hepatic bile salt export pump. Rebaudioside D does not affect glucose homeostasis, alter total caloric intake or fecal energy excretion, induce weight gain, exacerbate obesity, promote hepatic steatosis, impair brown adipose tissue function, nor change skeletal muscle metabolism-related proteins. Rebaudioside D can be used in diet-induced obesity and obesity-related research .
    Rebaudioside D
  • HY-N7755
    Estradiol 3-glucuronide sodium

    		Endogenous Metabolite ATP-binding cassette (ABC) transporters OAT Others
    Estradiol 3-glucuronide sodium is an estrogen metabolite, which is a glucuronide conjugate formed by the catalysis of uridine diphosphate glucuronosyltransferase in tissues such as the liver from Estradiol (HY-B0141). Estradiol 3-glucuronide sodium is a potent substrate of Mrp2, with an S50 of 55.7 μM. Estradiol 3-glucuronide sodium achieves hepatobiliary transport in hepatocytes through basolateral uptake via OATP1B1, OATP1B3 and OATP2B1, as well as apical efflux via MRP2 and BCRP .
    Estradiol 3-glucuronide sodium
  • HY-136450
    Triclabendazole sulfoxide

    TCBZ-SO

    		 Parasite BCRP Infection Cancer
    Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
    Triclabendazole sulfoxide
  • HY-W585842
    Estradiol 3-glucuronide

    		Endogenous Metabolite ATP-binding cassette (ABC) transporters OAT Others
    Estradiol 3-glucuronide is an estrogen metabolite, which is a glucuronide conjugate formed from Estradiol (HY-B0141) via catalysis by uridine diphosphate glucuronosyltransferases in tissues such as the liver. Estradiol 3-glucuronide is a potent substrate of Mrp2, with an S50 value of 55.7 μM. Estradiol 3-glucuronide achieves hepatobiliary transport in hepatocytes through basolateral uptake via OATP1B1, OATP1B3 and OATP2B1, as well as apical efflux via MRP2 and BCRP .
    Estradiol 3-glucuronide
  • HY-100928
    YS 035 hydrochloride

    		Calcium Channel Neurological Disease
    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 .
    YS 035 hydrochloride
  • HY-N0468R
    Rebaudioside D (Standard)

    		Reference Standards Acetyl-CoA Carboxylase FXR Metabolic Disease
    Rebaudioside D (Standard) is the analytical standard of Rebaudioside D. This product is intended for research and analytical applications. Rebaudioside D is an orally active sweetener that targets and activates FXR, modulates Acetyl-CoA Carboxylase, and inhibits 3-hydroxy-3-methylglutaryl-CoA reductase. Rebaudioside D regulates bile acid homeostasis and lipid metabolism, reduces the synthesis rates of fatty acids and cholesterol, and exerts multiple effects including anti-adipogenesis, hepatoprotection, anti-steatosis, gut microbiota modulation, enhancement of secondary bile acid metabolism, anti-endotoxin activity, regulation of bile acid transport, and inhibition of bile acid efflux. Rebaudioside D also reduces body weight gain, visceral fat accumulation, hepatic triglyceride and cholesterol accumulation, hepatic lipid peroxidation, and decreases the circulating level of lipopolysaccharide-binding protein. Rebaudioside D additionally enhances the secondary bile acid metabolic pathway of intestinal bacteria, upregulates the gene expression of ileal organic solute transporter α, and downregulates the gene expression of hepatic bile salt export pump. Rebaudioside D does not affect glucose homeostasis, alter total caloric intake or fecal energy excretion, induce weight gain, exacerbate obesity, promote hepatic steatosis, impair brown adipose tissue function, nor change skeletal muscle metabolism-related proteins. Rebaudioside D can be used in diet-induced obesity and obesity-related research .
    Rebaudioside D (Standard)
  • HY-122416
    6,8-Diprenylnaringenin

    Lonchocarpol A; Senegalensin

    		 BCRP Metabolic Disease Cancer
    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 .
    6,8-Diprenylnaringenin
  • HY-117763
    A-39355

    		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.
    A-39355
  • HY-136450R
    Triclabendazole sulfoxide (Standard)

    TCBZ-SO (Standard)

    		 Reference Standards Parasite BCRP Infection
    Triclabendazole sulfoxide (Standard) is the analytical standard of Triclabendazole sulfoxide. This product is intended for research and analytical applications. Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
    Triclabendazole sulfoxide (Standard)
  • HY-136450S
    Triclabendazole sulfoxide-d3

    TCBZ-SO-d3

    		 Isotope-Labeled Compounds Parasite BCRP Infection
    Triclabendazole sulfoxide-d3 is the deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
    Triclabendazole sulfoxide-d3
  • HY-136450S1
    Triclabendazole sulfoxide-13C,d3

    TCBZ-SO-13C,d3

    		 Isotope-Labeled Compounds Parasite BCRP Infection
    Triclabendazole sulfoxide- 13C,d3 is the 13C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
    Triclabendazole sulfoxide-13C,d3
  • HY-W127487
    N-Octadecanoyl-L-homoserine lactone

    		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.
    N-Octadecanoyl-L-homoserine lactone
  • HY-N9440
    7-Hydroxycoumarin glucuronide

    		Drug Metabolite Inflammation/Immunology Cancer
    7-Hydroxycoumarin glucuronide is a transport substrate and main human coumarin metabolite. 7-Hydroxycoumarin glucuronide undergoes ATP-dependent efflux transport via MRP3 and MRP4. 7-Hydroxycoumarin glucuronide undergoes active transport processes for urinary excretion and is primarily excreted into urine in humans.
    7-Hydroxycoumarin glucuronide
  • HY-120768
    A-30312

    		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.
    A-30312
  • HY-W344531
    Indomethacin glucuronide

    		Drug Metabolite Inflammation/Immunology
    Indomethacin glucuronide is a glucuronide metabolite of Indomethacin (HY-14397) .
    Indomethacin glucuronide
  • HY-181642
    nNOS-IN-3

    		NO Synthase Neurological Disease Cancer
    nNOS-IN-3 (compound 4) is an orally active, selective, neuronal nitric oxide synthase (nNOS) inhibitor with a human hnNOS Ki of 25 nM, rat rnNOS Ki of 18 nM, human heNOS Ki of 58140 nM, human hiNOS Ki of 6422 nM. nNOS-IN-3 binds to nNOS active sites via hydrogen bonds with Glu and chalcogen bonds with Met, fails to form chalcogen bonds with heNOS, and undergoes passive transcellular transport with minimal efflux liability. nNOS-IN-3 can be used for the research of neurodegenerative diseases and melanoma .
    nNOS-IN-3
  • HY-182633
    Hapalosin

    		P-glycoprotein Cancer
    Hapalosin is a multidrug resistance reversal agent and chemosensitizer with mild cytotoxicity against cancer cells. Hapalosin inhibits the ATP-dependent drug efflux pump function of P-glycoprotein and antagonizes multidrug resistance-associated proteins. Hapalosin reverses multidrug resistance mediated by P-glycoprotein and multidrug resistance-associated proteins, increases the intracellular accumulation of drugs transported by P-glycoprotein, and enhances the cytotoxicity of these drugs against cancer cells overexpressing P-glycoprotein. Hapalosin can be used in the research of multidrug-resistant cancers .
    Hapalosin
  • HY-120433
    BLT-3

    		Scavenger Receptor Class B type I (SR-BI） Inflammation/Immunology
    BLT-3 is an inhibitor of scavenger receptor class B type I (SR-BI) that exerts reversible, non-cell-type-specific inhibitory effects on SR-BI-mediated lipid transport. BLT-3 inhibits SR-BI-mediated selective lipid uptake from HDL as well as cholesterol efflux from cells to HDL. BLT-3 enhances the binding of HDL to SR-BI. BLT-3 is applicable to research related to atherosclerosis and coronary heart disease .
    BLT-3

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