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Results for "

glycoprotein substrate

" in MedChemExpress (MCE) Product Catalog:

45

Inhibitors & Agonists

2

Biochemical Assay Reagents

3

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11

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6

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P3008
    Submandibular mucin

    		Biochemical Assay Reagents Others
    Submandibular mucin is a high molecular weight glycoprotein that is used as a substrate for the viral enzyme neuraminidase .
    Submandibular mucin
  • HY-107212
    Selamectin

    		Parasite Chloride Channel P-glycoprotein Bacterial Infection
    Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM .
    Selamectin
  • HY-A0279A
    Pristinamycin IA
    1 Publications Verification

    Mikamycin B; Mikamycin IA

    		 Bacterial Antibiotic Infection
    Pristinamycin IA (Mikamycin B) is a cycle-peptidic macrolactone antibiotic. Pristinamycin IA is a substrate of P-glycoprotein and inhibits its function. Pristinamycin IA is active against StaphyloEoccus and Srreptococcus .
    Pristinamycin IA
  • HY-16191
    ELR510444
    1 Publications Verification

    		 Microtubule/Tubulin Apoptosis Cancer
    ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.
    ELR510444
  • HY-E70054
    beta-1,3-Galactosyltransferase (WbgO)

    CgtB

    		 Others Others
    beta-1,3-Galactosyltransferase (WbgO) (CgtB) acts on N-glycan substrates. beta-1,3-Galactosyltransferase (WbgO) catalyzes the formation of type 1 chains on oligosaccharide, glycopeptide, and glycoprotein substrates, including itself .
    beta-1,3-Galactosyltransferase (WbgO)
  • HY-P10282
    Synapsin I-(3-13)

    		CaMK Neurological Disease
    Synapsin I-(3-13), a substrate for CaMK1, is a glycoprotein. Synapsin I is a phosphoprotein that coats the cytoplasmic side of synaptic vesicles and regulates their trafficking within nerve terminals .
    Synapsin I-(3-13)
  • HY-107212R
    Selamectin (Standard)

    		Reference Standards Parasite Chloride Channel P-glycoprotein Bacterial Infection
    Selamectin (Standard) is the analytical standard of Selamectin. This product is intended for research and analytical applications. Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM .
    Selamectin (Standard)
  • HY-128038
    N-Desmethyl-loperamide

    		Opioid Receptor Neurological Disease
    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 .
    N-Desmethyl-loperamide
  • HY-N3197
    Neostenine

    (+)-Neostenine

    		 P-glycoprotein Cancer
    Neostenine is a stenine-type Stemona alkaloid, with antitussive activity. Neostenine is also a substrate of P-glycoprotein with high absorptive permeability in Caco-2 monolayer model. Neostenine also shows oral activity for intestinal application .
    Neostenine
  • HY-137261
    UDP-β-D-glucose disodium

    		Others Metabolic Disease
    UDP-β-D-glucose disodium is a the stereoisomer of UDP-α-D-glucose. UDP-β-D-glucose disodium is an oligosaccharide that can be used to synthesize glycoproteins and glycolipids. UDP-β-D-glucose disodium can be used as a substrate .
    UDP-β-D-glucose disodium
  • HY-108286
    Talinolol

    Cordanum

    		 Adrenergic Receptor Cardiovascular Disease
    Talinolol (Cordanum) is a long-acting, cardioselective β1-adrenergic receptor blocker. Talinolol exhibits cardioprotective and antihypertensive activities. Talinolol is also a well-known and frequently used probe substrate for P-glycoprotein (P-gp) activity .
    Talinolol
  • HY-A0279AR
    Pristinamycin IA (Standard)

    Mikamycin B (Standard); Mikamycin IA (Standard)

    		 Reference Standards Bacterial Antibiotic Infection
    Pristinamycin IA (Standard) is the analytical standard of Pristinamycin IA. This product is intended for research and analytical applications. Pristinamycin IA (Mikamycin B) is a cycle-peptidic macrolactone antibiotic. Pristinamycin IA is a substrate of P-glycoprotein and inhibits its function. Pristinamycin IA is active against StaphyloEoccus and Srreptococcus[1].
    Pristinamycin IA (Standard)
  • 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 .
    Antitrypanosomal agent 24
  • HY-107903
    Thyroglobulin

    Thyroglobulin from bovine

    		 Biochemical Assay Reagents Cancer
    Thyroglobulin is a 660 kDa, dimeric glycoprotein produced by the follicular cells of the thyroid and used entirely within the thyroid gland. Thyroglobulin acts as a substrate for the synthesis of the thyroid hormones thyroxine (T4) and triiodothyronine (T3), as well as the storage of the inactive forms of thyroid hormone and iodine within the follicular lumen of a thyroid follicle .
    Thyroglobulin
  • HY-170569
    Cetagliptin

    		Dipeptidyl Peptidase Cytochrome P450 P-glycoprotein Metabolic Disease
    Cetagliptin is an orally active inhibitor for dipeptidyl peptidase 4 (DPP-4) and CYP2D6 (IC50 of 6 µM). Cetagliptin is a substrate for P-glycoprotein. Cetagliptin reduces the GLP-1 degradation, maintains the level of postprandial blood sugar, and can be used in type 2 diabetes mellitus research .
    Cetagliptin
  • HY-B0777
    Moxidectin
    1 Publications Verification

    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 .
    Moxidectin
  • HY-108286S
    (Rac)-Talinolol-d5

    		Isotope-Labeled Compounds Adrenergic Receptor Cardiovascular Disease
    (Rac)-Talinolol-d5 is the racemate of Talinolol. Talinolol (Cordanum) is a long-acting, cardioselective β1-adrenergic receptor blocker. Talinolol exhibits cardioprotective and antihypertensive activities. Talinolol is also a well-known and frequently used probe substrate for P-glycoprotein (P-gp) activity .
    (Rac)-Talinolol-d5
  • HY-P2869A
    β1-3 Galactosidase

    		Glycosidase Metabolic Disease
    β1-3 Galactosidase is a highly specific exoglycosidase that catalyzes the hydrolysis of terminal β1-3-linked galactose from oligosaccharides and glycoprotein substrates, at a much lower rate, β1-6 linked galactose residues from oligosaccharides .
    β1-3 Galactosidase
  • HY-16397
    Phenformin
    5+ Cited Publications

    Phenethylbiguanide

    		 Mitochondrial Metabolism AMPK Apoptosis Metabolic Disease Cancer
    Phenformin (1-phenethylbiguanide) is an orally active antidiabetic and anticancer agent. Phenformin has an incidence of associated lactic acidosis. Phenformin acts through acting AMPK activation and blocking mTOR pathway. Phenformin is also a substrate of P-glycoprotein (P-gp), and an OXPHOS inhibitor. Phenformin induces cancer cell apoptosis .
    Phenformin
  • HY-E70039
    alpha-2-3,6,8-Sialidosidase (SpNanA)

    		Others Others
    alpha-2-3,6,8-Sialidosidase (SpNanA) catalyses hydrolysis of alpha-(2->3)-, alpha-(2->6)-, alpha-(2->8)- glycosidic linkages of terminal sialic acid residues in oligosaccharides, glycoproteins, glycolipids, colominic acid and synthetic substrates .
    alpha-2-3,6,8-Sialidosidase (SpNanA)
  • HY-10289
    Carmegliptin

    RO-4876904

    		 Dipeptidyl Peptidase P-glycoprotein Cardiovascular Disease Metabolic Disease
    Carmegliptin (RO-4876904) is an orally active, potent and long-acting dipeptidyl peptidase IV inhibitor. Carmegliptin is also a substrate of P-glycoprotein that synergizes with Verapamil (HY-14275). Carmegliptin improves insulin sensitivity and reduces hepatic glucose production in hyperglycemic mice. Carmegliptin is promising for research of type 2 diabetes, hypertension and cardiovascular disease .
    Carmegliptin
  • HY-13646B
    Encequidar hydrochloride

    HM30181 hydrochloride; HM30181A hydrochloride

    		 P-glycoprotein Others
    Encequidar hydrochloride (HM30181 hydrochloride) is an oral P-glycoprotein (P-gp) inhibitor with the activity of enhancing the oral bioavailability of P-gp substrate drugs. Encequidar shows the highest potency among various MDR1 inhibitors, with IC50=0.63nM. Encequidar effectively blocks the transepithelial transport of paclitaxel in MDCK monolayer cells, with IC50=35.4nM .
    Encequidar hydrochloride
  • HY-W001601
    Budipine

    		iGluR Neurological Disease
    Budipine is an anti-parkinson agent. Budipine also is a substrate of P-glycoprotein (P-gp), is mediated the uptake into the brain by P-gp. Budipine also is N-methyl-d-aspartate (NMDA) antagonist, and has indirect dopaminergic effects through an improved dopamine release, the inhibition of monoamine oxidase type B (MAO-B). Budipine can be used for the research of CNS disorders include Parkinson disease .
    Budipine
  • HY-W001601A
    Budipine hydrochloride

    		iGluR Neurological Disease
    Budipine hydrochloride is an anti-parkinson agent. Budipine hydrochloride also is a substrate of P-glycoprotein (P-gp), is mediated the uptake into the brain by P-gp. Budipine hydrochloride also is N-methyl-d-aspartate (NMDA) antagonist, and has indirect dopaminergic effects through an improved dopamine release, the inhibition of monoamine oxidase type B (MAO-B). Budipine hydrochloride can be used for the research of CNS disorders include Parkinson disease .
    Budipine hydrochloride
  • HY-14895
    Fabomotizole

    CM346

    		 Parasite Monoamine Oxidase Sigma Receptor P-glycoprotein Infection Cardiovascular Disease Neurological Disease
    Fabomotizole (CM346) is an insecticide with anxiolytic, antianxiety, and neuroprotective activities and a substrate of p-glycoprotein. Fabomotizole inhibits the ST-segment depression induced by isoproterenol in a rat model of acute subendocardial ischemia. Fabomotizole also inhibits Giardia lamblia and has the potential to inhibit giardiasis. Fabomotizole also targets Sigma1R, NRH:quinone reductase 2 (NQO2), and MAO-A to exert anxiolytic effects .
    Fabomotizole
  • HY-B0777R
    Moxidectin (Standard)

    CL301423 (Standard)

    		 Antibiotic BCRP P-glycoprotein Parasite Reference Standards 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 .
    Moxidectin (Standard)
  • HY-123934
    VU6007477

    		P-glycoprotein Neurological Disease
    VU6007477 is a brain-penetrant, selective M1 positive allosteric modulator (PAM) with an EC50 value of 230 nM. VU6007477 is also a human P-glycoprotein (P-gp) substrate with moderate permeability. VU6007477 displays improved central nervous system (CNS) penetration over the hydroxylated congeners. VU6007477 a pyranyl amide derivative, which is promising for research of robust cholinergic seizure activity .
    VU6007477
  • HY-N11287
    UDP-xylose

    		Endogenous Metabolite Others
    UDP-xylose is an endogenous sugar nucleotide and a catalytic substrate of UDP-xylose synthase (UXS). UDP-xylose is a sugar donor for the synthesis of glycoproteins, polysaccharides, various metabolites and oligosaccharides in plants, vertebrates and fungi, and participates in the synthesis of proteoglycans as a glycosyl donor. UDP-xylose participates in the regulation of the synthesis of extracellular matrix components and can be used to study the mechanism of proteoglycan biosynthesis in glycobiology and related diseases (such as connective tissue diseases)[1][2].
    UDP-xylose
  • HY-P10856
    CPI1

    		P-glycoprotein Cancer
    CPI1 is a potent and highly specific multidrug resistance protein 1 (MRP1) inhibitor. CPI1 inhibits MRP1 (Ki: 100 nM) with nanomolar potency but shows minimal inhibition of P-glycoprotein (Pgp). CPI1 and LTC4 compete to bind to the same site of MRP1, inhibiting ATP hydrolysis and substrate transport. CPI1 can be used to study drug delivery and chemotherapy resistance in cancer .
    CPI1
  • HY-N2453
    Convallatoxin

    		PPAR NF-κB P-glycoprotein Inflammation/Immunology Cancer
    Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties .
    Convallatoxin
  • HY-17367
    Atazanavir
    Maximum Cited Publications
    11 Publications Verification

    BMS-232632

    		 HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Toll-like Receptor (TLR) Infection Cardiovascular Disease Cancer
    Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .
    Atazanavir
  • HY-17367S4
    Atazanavir-d6

    BMS-232632-d6

    		 Isotope-Labeled Compounds HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Infection Cancer
    Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM .
    Atazanavir-d6
  • HY-17367S3
    Atazanavir-d5

    		Isotope-Labeled Compounds HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Infection Cancer
    Atazanavir-d5 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM .
    Atazanavir-d5
  • HY-17367S2
    Atazanavir-d9

    BMS-232632-d9

    		 Isotope-Labeled Compounds HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Infection Cancer
    Atazanavir-d9 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM .
    Atazanavir-d9
  • HY-W001601R
    Budipine (Standard)

    		Reference Standards iGluR Neurological Disease
    Budipine (Standard) is the analytical standard of Budipine. This product is intended for research and analytical applications. Budipine is an anti-parkinson agent. Budipine also is a substrate of P-glycoprotein (P-gp), is mediated the uptake into the brain by P-gp. Budipine also is N-methyl-d-aspartate (NMDA) antagonist, and has indirect dopaminergic effects through an improved dopamine release, the inhibition of monoamine oxidase type B (MAO-B). Budipine can be used for the research of CNS disorders include Parkinson disease .
    Budipine (Standard)
  • HY-N11287A
    UDP-xylose disodium

    		Endogenous Metabolite Others
    UDP-xylose disodium is an endogenous sugar nucleotide and a catalytic substrate of UDP-xylose disodium synthase (UXS). UDP-xylose disodium is a sugar donor for the synthesis of glycoproteins, polysaccharides, various metabolites and oligosaccharides in plants, vertebrates and fungi, and participates in the synthesis of proteoglycans as a glycosyl donor. UDP-xylose disodium participates in the regulation of the synthesis of extracellular matrix components and can be used to study the mechanism of proteoglycan biosynthesis in glycobiology and related diseases (such as connective tissue diseases)[1][2].
    UDP-xylose disodium
  • HY-17367A
    Atazanavir sulfate
    Maximum Cited Publications
    11 Publications Verification

    BMS-232632 sulfate

    		 HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Toll-like Receptor (TLR) Infection Cardiovascular Disease Cancer
    Atazanavir (BMS-232632) sulfate is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .
    Atazanavir sulfate
  • HY-17367AR
    Atazanavir sulfate (Standard)

    BMS-232632 sulfate (Standard)

    		 Reference Standards HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Infection Cancer
    Atazanavir (sulfate) (Standard) is the analytical standard of Atazanavir (sulfate). This product is intended for research and analytical applications. Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM .
    Atazanavir sulfate (Standard)
  • HY-B0777S
    Moxidectin-d3

    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 .
    Moxidectin-d3
  • HY-N2453R
    Convallatoxin (Standard)

    		Reference Standards PPAR NF-κB P-glycoprotein Inflammation/Immunology Cancer
    Convallatoxin (Standard) is the analytical standard of Convallatoxin. This product is intended for research and analytical applications. Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties .
    Convallatoxin (Standard)
  • HY-17367R
    Atazanavir (Standard)

    BMS-232632 (Standard)

    		 Reference Standards HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Infection Cancer
    Atazanavir (Standard) is the analytical standard of Atazanavir. This product is intended for research and analytical applications. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .
    Atazanavir (Standard)
  • HY-17367S5
    Atazanavir-d24

    BMS-232632-d24

    		 Isotope-Labeled Compounds P-glycoprotein SARS-CoV Endogenous Metabolite HIV Cytochrome P450 HIV Protease Toll-like Receptor (TLR) Infection Cardiovascular Disease Cancer
    Atazanavir-d24 (BMS-232632-d24) is deuterium labeled Atazanavir. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .
    Atazanavir-d24
  • HY-E70568
    O-GlyCORTAR protease

    		Ser/Thr Protease Others
    O-GlyCORTAR protease is recombinantly expressed from E.coli and contains a His tag. O-GlyCORTAR protease is an O-glycan-dependent protease that digests proteins carrying mucin-type O-glycans, including sialylated substrates, glycosylated Ser and Thr residues at the N terminus. O-GlyCORTAR protease digests a variety of O-glycan structures, including sialylated glycosylated core 1 and core 2 structures and Tn antigen. O-GlyCORTAR protease does not digest terminally modified serine or threonine residues, nor does it digest N-glycosylation sites on glycoproteins.
    O-GlyCORTAR protease
  • HY-173162
    GPV0057

    		P-glycoprotein Potassium Channel Cardiovascular Disease Cancer
    GPV0057 (Compound 5d) is a selective and potent P-glycoprotein (P-gp) inhibitor. GPV0057 is also a selective potassium channel Kir2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of Kir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, Kir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome .
    GPV0057
  • HY-138074
    Milbemycin A4 oxime

    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.
    Milbemycin A4 oxime

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