Search Result
Results for "
glycoprotein substrate
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
6
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P3008
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-
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- HY-107212
-
|
Parasite
Chloride Channel
P-glycoprotein
Bacterial
|
Infection
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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 .
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- HY-A0279A
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Mikamycin B; Mikamycin IA
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Bacterial
Antibiotic
|
Infection
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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 .
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- HY-16191
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Microtubule/Tubulin
Apoptosis
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Cancer
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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.
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- HY-E70054
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CgtB
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Others
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Others
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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 .
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- HY-P10282
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CaMK
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Neurological Disease
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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 .
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- HY-107212R
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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 .
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- HY-128038
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Opioid Receptor
|
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-N3197
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(+)-Neostenine
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P-glycoprotein
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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 .
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- HY-137261
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Others
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Metabolic Disease
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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 .
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- HY-108286
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Cordanum
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Adrenergic Receptor
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Cardiovascular Disease
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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 .
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- HY-A0279AR
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Mikamycin B (Standard); Mikamycin IA (Standard)
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Bacterial
Antibiotic
|
Infection
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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].
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- HY-107903
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Thyroglobulin from bovine
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Biochemical Assay Reagents
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Cancer
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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 .
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- HY-170569
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Dipeptidyl Peptidase
Cytochrome P450
P-glycoprotein
|
Metabolic Disease
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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 .
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- HY-P2869A
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Others
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Metabolic Disease
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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 .
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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-16397
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Phenethylbiguanide
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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 .
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- HY-108286S
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|
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[1][2][3].
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- HY-E70039
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Others
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Others
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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 .
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- HY-10289
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RO-4876904
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Dipeptidyl Peptidase
P-glycoprotein
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Cardiovascular Disease
Metabolic Disease
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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 .
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- HY-13646B
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HM30181 hydrochloride; HM30181A hydrochloride
|
P-glycoprotein
|
Others
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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 .
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- HY-W001601
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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 .
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- HY-W001601A
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|
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 .
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- HY-14895
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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 .
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- HY-B0777R
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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 .
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- HY-123934
-
|
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 .
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- HY-P10856
-
|
P-glycoprotein
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Cancer
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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 .
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- HY-N2453
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|
PPAR
NF-κB
P-glycoprotein
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Inflammation/Immunology
Cancer
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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 .
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- HY-17367
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- HY-W001601R
-
|
iGluR
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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 .
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- HY-17367S4
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- HY-17367S3
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- HY-17367S2
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- HY-17367A
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- HY-17367AR
-
|
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 .
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- HY-B0777S
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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 .
|
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- HY-N2453R
-
|
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 .
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-
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- HY-17367R
-
|
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 .
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- HY-17367S5
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-
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- HY-138074
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5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime
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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.
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Cat. No. |
Product Name |
Type |
-
- HY-P3008
-
|
Native Proteins
|
Submandibular mucin is a high molecular weight glycoprotein that is used as a substrate for the viral enzyme neuraminidase .
|
-
- HY-107903
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Thyroglobulin from bovine
|
Native Proteins
|
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 .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3008
-
-
- HY-P10282
-
|
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 .
|
-
- HY-P10856
-
|
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 .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-17367S4
-
|
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[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
|
-
-
- HY-108286S
-
|
(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[1][2][3].
|
-
-
- HY-17367S3
-
|
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[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
|
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-
- HY-17367S2
-
|
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[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[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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-
- HY-17367S5
-
|
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 .
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