Search Result
Results for "
transport substrate
" in MedChemExpress (MCE) Product Catalog:
4
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N0455
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- HY-N0455A
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(S)-(+)-Arginine hydrochloride
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NO Synthase
Endogenous Metabolite
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Cardiovascular Disease
Inflammation/Immunology
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L-Arginine ((S)-(+)-Arginine) is the substrate for the endothelial nitric oxide synthase (eNOS) to generate NO. L-Arginine is transported into vascular smooth muscle cells by the cationic amino acid transporter family of proteins where it is metabolized to nitric oxide (NO), polyamines, or L-proline. L-Arginine is a potent vasodilator, and can be used to induce experimental acute pancreatitis .
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- HY-134452
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MeAIB
4 Publications Verification
α-(Methylamino)isobutyric acid
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Amino acid Transporter
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Cancer
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MeAIB (α-(Methylamino)isobutyric acid) is a specific?substrate for amino acid transport system A (ATA1). ATA mediate the uptake of short-chain neutral amino acids in a Na +-dependent manner .
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- HY-B0804
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Nadolol
5 Publications Verification
SQ-11725
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Adrenergic Receptor
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Cardiovascular Disease
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Nadolol (SQ-11725) is a non-selective and orally active β-adrenergic receptors blocker and is a substrate of organic anion transporting polypeptide 1A2 (OATP1A2). Nadolol has the the potential for high blood pressure, angina pectoris and vascular headaches research .
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- HY-134427
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Palmitoyl CoA lithium
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Endogenous Metabolite
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Metabolic Disease
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Palmitoyl coenzyme A lithium is an acyl-CoA thioester that can be transported into the mitochondrial matrix via the carnitine shuttle system and is involved in β-oxidation. Palmitoyl coenzyme A lithium can also be used as a substrate for sphingosine biosynthesis .
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- HY-A0080
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Sodium p-aminohippurate; p-Aminohippuric acid sodium salt
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Biochemical Assay Reagents
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Aminohippurate sodium is a renal tubular transport inhibitor and a substrate for organic anion transporters. Aminohippurate sodium inhibits renal tubular reabsorption of phosphate and promotes increased urinary phosphate excretion. Aminohippurate sodium inhibits renal tubular reabsorption of vitamin C as well as the transport of glucose .
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- HY-10873
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SU-12662
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Drug Metabolite
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Cancer
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N-Desethyl Sunitinib (SU-12662) is a metabolite of Sunitinib (HY-10255A). N-Desethyl Sunitinib serves as a good transport substrate for human ABCB1, ABCG2 and murine ABCG2 .
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- HY-170316
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Ras
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Cancer
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Ibetazol is a Importin β1 (KPNB1) inhibitor and nucleocytoplasmic transport disruptor. Ibetazol binds covalently to Cys585 of Importin β1, blocks both Importin β1-mediated direct transport and Importin α-dependent nuclear import processes, without affecting transport mediated by other nucleocytoplasmic transport proteins. Ibetazol induces cytoplasmic accumulation of Importin α1, and inhibits nuclear import of substrates carrying nuclear localization signals (NLS), including the NLS-cMyc reporter gene, RelA/p65 and SREBP1. Ibetazol triggers spindle malformation and chromosome misalignment by disrupting the mitotic function of Importin β1. Ibetazol inhibits the proliferation of cells expressing wild-type Importin β1. Ibetazol has a high activity-cytotoxicity window, lacks intrinsic fluorescence, and acts rapidly on nucleocytoplasmic transport processes. Ibetazol serves as a tool compound for investigating nuclear import processes specifically mediated by Importin β1 .
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- HY-D0180
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18C6; 1,4,7,10,13,16-Hexaoxacyclooctadecane
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Bacterial
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Infection
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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 .
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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-N0455R
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Reference Standards
NO Synthase
Endogenous Metabolite
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Cardiovascular Disease
Cancer
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L-Arginine (Standard) is the analytical standard of L-Arginine. This product is intended for research and analytical applications. L-Arginine ((S)-(+)-Arginine) is the substrate for the endothelial nitric oxide synthase (eNOS) to generate NO. L-Arginine is transported into vascular smooth muscle cells by the cationic amino acid transporter family of proteins where it is metabolized to nitric oxide (NO), polyamines, or L-proline. L-Arginine is a potent vasodilator, and can be used to induce experimental acute pancreatitis .
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- HY-113291
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Nucleoside Antimetabolite/Analog
Phosphorylase
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Others
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5'-Deoxyadenosine is a 5'-methylthioadenosine phosphorylase substrate and deoxyadenosine. 5'-Deoxyadenosine serves as a non-metabolizable substrate for nucleoside transport assays only in cells lacking 5'-methylthioadenosine phosphorylase .
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- HY-P10856
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P-glycoprotein
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Cancer
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CPI1 is a multidrug resistance protein 1 (MRP1) inhibitor with a Ki value of 100 nM. CPI1 binds to the same substrate-binding site as leukotriene C4, stabilizes MRP1 in an apo-like inward-facing conformation, blocks the conformational changes required for ATP hydrolysis and substrate transport, and inhibits the ATPase activity of human and bovine MRP1. CPI1 serves as a tool for investigating the substrate transport mechanism of MRP1. CPI1 is applicable to research related to cancer multidrug resistance .
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- HY-D1078
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Fluorescent Dye
Reactive Oxygen Species (ROS)
P-glycoprotein
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Others
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5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate is a fluorescein-based reactive oxygen species (ROS) probe and also a MRP2 substrate. 5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate serves as a substrate for intracellular esterases, which cleave its acetate groups to generate a fluorescent product capable of detecting intracellular ROS. 5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate is ATP-dependent and is transported via a single MRP2 binding site; it competes with LTC4 for MRP2 binding sites and inhibits MRP2-mediated LTC4 transport (Ex/Em = 496/525 nm) .
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- HY-101453
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P-glycoprotein
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Cancer
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Ceefourin 1 is a potent and highly selective multidrug resistance protein 4 (MRP4) inhibitor. Ceefourin 1 inhibits transport of a broad range of MRP4 substrates, yet is highly selective for MRP4 over other ABC transporters. Ceefourin 1 is a benzothiazol and primarily as a chemosensitizer for high-risk neuroblastoma .
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- HY-W353102
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Endogenous Metabolite
P-glycoprotein
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Metabolic Disease
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Estradiol 17-(β-D-Glucuronide) is a D-ring glucuronide metabolite of natural estrogen formed in the liver. Estradiol 17-(β-D-Glucuronide) is a substrate of the organic anion-transporting polypeptide family (Oatp) and multidrug resistance-associated protein 2 (Mrp2). Estradiol 17-(β-D-Glucuronide) regulates MRP8-mediated transport processes and inhibits MRP8-mediated transport of dehydroepiandrosterone 3-sulfate and taurocholic acid. Estradiol 17-(β-D-Glucuronide) induces immediate, reversible reduction of bile flow and acute intrahepatic cholestasis in female rats without altering the bile acid composition in bile. Estradiol 17-(β-D-Glucuronide) can be used in studies related to intrahepatic cholestasis .
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- HY-129987
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Endogenous Metabolite
P-glycoprotein
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Metabolic Disease
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Estradiol 17-(β-D-Glucuronide) sodium is a D-ring glucuronide metabolite of natural estrogen formed in the liver. Estradiol 17-(β-D-Glucuronide) sodium is a substrate of the organic anion-transporting polypeptide family (Oatp) and multidrug resistance-associated protein 2 (Mrp2). Estradiol 17-(β-D-Glucuronide) sodium regulates MRP8-mediated transport processes and inhibits MRP8-mediated transport of dehydroepiandrosterone 3-sulfate and taurocholic acid. Estradiol 17-(β-D-Glucuronide) sodium induces immediate, reversible reduction of bile flow and acute intrahepatic cholestasis in female rats without altering the bile acid composition in bile. Estradiol 17-(β-D-Glucuronide) sodium can be used in studies related to intrahepatic cholestasis .
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- HY-101310
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iGluR
EAAT
Bcl-2 Family
Caspase
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Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
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SYM 2081 is a kainate receptor agonist. SYM 2081 is a substrate of EAAT1 (Km of 54 μM). SYM 2081 inhibits EAAT2-mediated glutamate transport (Kb is 3.4 μM in Xenopus oocytes), modulates Apoptotic signaling pathways (increases Bcl-2 and decreases Bax/caspase-3 expression). SYM 2081 exhibits neuroprotective activity. SYM 2081 can be used in the study of hypoxic-ischemic brain damage and inflammatory or neuropathic pain .
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- HY-148123
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Biochemical Assay Reagents
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Neurological Disease
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Glycerophospholipids and cephalins are a class of phospholipid compounds and important components of neural membranes. Glycerophospholipids and cephalins are hydrolysis substrates of phospholipase (such as PLA2, PLC, and PLD). After complete hydrolysis, they produce 1 mol of glycerol, phosphate, ethanolamine, and 2 mol of fatty acids, respectively. Glycerophospholipids and cephalins can maintain membrane structure, fluidity, and ion permeability, and serve as precursors of second messengers such as arachidonic acid and diacylglycerol. Glycerophospholipids and cephalins can regulate signal transduction, cell apoptosis, and membrane transport, and are used in the study of neurodegenerative diseases (such as Alzheimer's disease) .
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- HY-D0194
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P-glycoprotein
Fluorescent Dye
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Others
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5(6)-Carboxy-2',7'-dichlorofluorescein is an ideal substrate for MRP2 vesicular transport assay, with excellent detection and transport properties .
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- HY-B0399S
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(R)-Carnitine-d9; Levocarnitine-d9
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Isotope-Labeled Compounds
Endogenous Metabolite
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Neurological Disease
Metabolic Disease
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L-Carnitine-d9 is the deuterium labeled L-Carnitine. L-Carnitine (Levocarnitine) is an endogenous molecule involved in fatty acid metabolism, biosynthesized within the human body using amino acids: L-lysine and L-methionine, as substrates. L-Carnitine functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-carnitine can ameliorate metabolic imbalances in many inborn errors of metabolism .
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- HY-N7755
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Endogenous Metabolite
ATP-binding cassette (ABC) transporters
OAT
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Others
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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 .
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- HY-111956B
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Fluorescent Dye
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Cancer
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D-Ala-Lys-AMCA hydrochloride is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA hydrochloride may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA hydrochloride can be used for characterizing PEPT1-specific substrates or inhibitors (Ex/Em = 390/480 nm) .
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- HY-138559
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Mitochondrial Metabolism
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Neurological Disease
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GW604714X is a potent inhibitor of mitochondrial respiration supported by pyruvate but not other substrates. GW604714X is a highly specific mitochondrial pyruvate carrier (MPC) inhibitor with a Ki <0.1 nM. GW604714X also inhibits L-lactate transport by the plasma membrane monocarboxylate transporter (MCT1), but at concentrations more than 4 orders of magnitude greater than the MPC .
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- HY-126584
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Val-Val
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Drug Intermediate
Oligopeptide Cotransporter
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Others
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H-Val-Val-OH (Val-Val) is a stereochemistry-dependent substrate and inhibitor of apical oligopeptide transporters. H-Val-Val-OH undergoes apical intracellular accumulation in human intestinal cells via carrier-mediated transport, and inhibits the uptake of Cephalexin (HY-B0200) through interaction with transporters. Substitution of L-valine with D-valine in H-Val-Val-OH abolishes its binding ability to apical oligopeptide transporters .
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- HY-W585842
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Endogenous Metabolite
ATP-binding cassette (ABC) transporters
OAT
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Others
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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 .
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- HY-119101
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CCR
Potassium Channel
P-glycoprotein
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Inflammation/Immunology
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AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis .
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- HY-124009
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Endogenous Metabolite
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Metabolic Disease
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L-Cysteic acid is the oxidation product of L-cystine. L-Cysteic acid is a substrate of GADCase/CADCaseII. L-Cysteic acid has high affinity with CADCase I (Km = 0.22 mM). L-Cysteic acid is taken up by the synaptosome through a high affinity, Na +-dependent transport system .
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- HY-D1584
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Phospholipase
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Others
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C12 NBD sphingomyelin is an active derivative of Sphingomyelin (HY-113498) that is tagged with fluorescent C12 nitrobenzoxadiazole (C12 NBD). C12 NBD sphingomyelin can be used as a sphingomyelinase substrate for studying the metabolism and transport of sphingomyelins (Ex=470 nm, Em=525 nm) .
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- HY-121088
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P-glycoprotein
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Cardiovascular Disease
Others
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Ceefourin 2 is a potent and highly selective inhibitor of MRP4. Ceefourin 2 inhibits the transport of MRP4 substrates but is not selective for other ABC transporters. Ceefourin 2 shows lower cytotoxicity and higher microsomal and acid stability .
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- HY-111956
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Fluorescent Dye
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Cancer
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D-Ala-Lys-AMCA is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA can be used for characterizing PEPT1-specific substrates or inhibitors (Ex/Em = 390/480 nm) .
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- HY-116055
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3-O-β-D-Galactopyranosyl-sn-glycerol
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Biochemical Assay Reagents
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Others
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(2R)-Glycerol-O-β-D-galactopyranoside (3-O-β-D-Galactopyranosyl-sn-glycerol) is a good substrate for all three components of the lac operon, i.e. β-galactosidase, the lactose transporter and thiogalactoside transacetylase .
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- HY-W854295
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PtdIns-(1,2-dioctanoyl) sodium
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P-glycoprotein
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Cancer
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Phosphatidylinositol-1,2-dioctanoyl sodium significantly inhibits transmembrane P-gp transport in a reproducible, cell line-independent, and substrate-independent manner. Phosphatidylinositol-1,2-dioctanoyl sodium plays an important role in signal transduction and cell movement .
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- HY-N0455C
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NO Synthase
Endogenous Metabolite
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Cardiovascular Disease
Inflammation/Immunology
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L-Arginine arginine is the substrate for the endothelial nitric oxide synthase (eNOS) to generate NO. L-Arginine is transported into vascular smooth muscle cells by the cationic amino acid transporter family of proteins where it is metabolized to nitric oxide (NO), polyamines, or L-proline. L-Arginine is a potent vasodilator, and can be used to induce experimental acute pancreatitis .
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- HY-B0804R
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SQ-11725 (Standard)
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Reference Standards
Adrenergic Receptor
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Cardiovascular Disease
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Nadolol (Standard) is the analytical standard of Nadolol. This product is intended for research and analytical applications. Nadolol (SQ-11725) is a non-selective and orally active β-adrenergic receptors blocker and is a substrate of organic anion transporting polypeptide 1A2 (OATP1A2). Nadolol has the the potential for high blood pressure, angina pectoris and vascular headaches research .
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- HY-17648
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BCRP
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Cancer
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MBL-II-141 is potent ABCG2 inhibitor with an IC50 of 0.11 μM. MBL-II-141 inhibits the transport function of ABCG2 in a non-competitive manner, preventing ABCG2 from pumping substrates (such as Irinotecan (HY-16562)) out of the cells, thereby increasing the accumulation of drugs within the cells. MBL-II-141 has no effect on ABCB1 (P-gp) and ABCC1 (MRP1) and has extremely low cytotoxicity (IG50 > 100 μM). MBL-II-141 can be used for the study of multidrug resistance (MDR) cancers .
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- HY-164401
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EAAT
DNA/RNA Synthesis
DNA Alkylator/Crosslinker
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Neurological Disease
Cancer
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QBS10072S is a bifunctional chemotherapeutic agent that can cross the blood-brain barrier (BBB), comprising a LAT1-targeting domain and a cytotoxic domain. QBS10072S exhibits inhibitory potency against LAT1-mediated substrate uptake (IC50 = 21 μM) of approximately 50-fold higher than that against LAT2 (IC50 = 1100 μM). QBS10072S enters LAT1-expressing tumor cells via LAT1-mediated active transport, induces DNA interstrand crosslinking, and causes DNA damage and cell death. QBS10072S can be used for the research of glioblastoma and aggressive T-cell lymphoma .
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- HY-N15726
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Others
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Others
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Obtusichromoneside C is a chromone C-glycoside found in the seeds of Cassia obtusifolia. Obtusichromoneside C regulates substance transport by inhibiting substrate uptake of specific transporters (e.g., OAT3, OATP1B3). Obtusichromoneside C is promising for research of drug transport .
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- HY-120649
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Biochemical Assay Reagents
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Others
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SKM 4-45-1 is an analog of Anandamide (AEA)(HY-10863). SKM 4-45-1 is a fluorescent substrate, that can be used to study the transmembrane carrier-mediated transport of AEA across cell membranes .
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- HY-134452R
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α-(Methylamino)isobutyric acid (Standard)
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Amino acid Transporter
Reference Standards
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Cancer
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MeAIB (Standard) is the analytical standard of MeAIB. This product is intended for research and analytical applications. MeAIB (α-(Methylamino)isobutyric acid) is a specific substrate for amino acid transport system A (ATA1). ATA mediate the uptake of short-chain neutral amino acids in a Na+-dependent manner .
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- HY-111956A
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Fluorescent Dye
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Cancer
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D-Ala-Lys-AMCA TFA is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA TFA may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA TFA can be used for characterizing PEPT1-specific substrates or inhibitors (Ex/Em = 390/480 nm) .
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- HY-100838
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L-CCG III
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EAAT
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Neurological Disease
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cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. cis-α-(Carboxycyclopropyl)glycine is a substrate of glutamate transporters (GluT) (EC50: 13 μM, 2 μM for EAAT 1 and EAAT 2, respectively). cis-α-(Carboxycyclopropyl)glycine inhibits a Na +-dependent high-affinity L-glutamate uptake in glial plasmalemmal vesicles (GPV) and synaptosomes .
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- HY-13646B
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HM30181 hydrochloride; HM30181A hydrochloride
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P-glycoprotein
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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-124009R
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Reference Standards
Endogenous Metabolite
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Others
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L-Cysteic acid (Standard) is the analytical standard of L-Cysteic acid. This product is intended for research and analytical applications. L-Cysteic acid is the oxidation product of L-cystine. L-Cysteic acid is a substrate of GADCase/CADCaseII. L-Cysteic acid has high affinity with CADCase I (Km = 0.22 mM). L-Cysteic acid is taken up by the synaptosome through a high affinity, Na +-dependent transport system .
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- HY-N0455AR
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(S)-(+)-Arginine hydrochloride (Standard)
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Reference Standards
NO Synthase
Endogenous Metabolite
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Cancer
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L-Arginine (hydrochloride) (Standard) is the analytical standard of L-Arginine (hydrochloride). This product is intended for research and analytical applications. L-Arginine ((S)-(+)-Arginine) is the substrate for the endothelial nitric oxide synthase (eNOS) to generate NO. L-Arginine is transported into vascular smooth muscle cells by the cationic amino acid transporter family of proteins where it is metabolized to nitric oxide (NO), polyamines, or L-proline. L-Arginine is a potent vasodilator, and can be used to induce experimental acute pancreatitis .
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- HY-N2453R
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Reference Standards
PPAR
NF-κB
P-glycoprotein
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Inflammation/Immunology
Cancer
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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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- HY-N9440
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Drug Metabolite
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Inflammation/Immunology
Cancer
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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.
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- HY-W736050
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Drug Derivative
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Others
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D-Cysteic acid is a competitive inhibitor of the aspartate:alanine antiporter (AspT) from Tetragenococcus halophilus. For L-aspartate self-exchange, D-Cysteic acid has a Ki of 0.14 mM and an IC50 of 0.19 mM; for L-alanine self-exchange, it has a Ki of 5.0 mM and an IC50 of 9.0 mM . D-Cysteic acid occupies a distinct substrate-binding site within the substrate transport pathway of AspT, preventing the binding of natural substrates to the transporter . D-Cysteic acid can be used in studies related to substrate recognition and transport mechanisms of transporters .
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- HY-181802
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BCRP
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Cancer
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MRS8431 is an ABCG2 inhibitor with a IC50 of 160 nM against human ABCG2. MRS8432 partially inhibits ABCG2-mediated substrate transport. MRS8432 is applicable to research related to cancer multidrug resistance .
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- HY-181803
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BCRP
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Cancer
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MRS8432 is an ABCG2 modulator with an EC50 of 7.5 nM against human ABCG2. MRS8432 activates ABCG2 ATPase activity. MRS8432 partially inhibits ABCG2-mediated substrate transport. MRS8432 is applicable to research related to cancer multidrug resistance .
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- HY-181804
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BCRP
P-glycoprotein
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Cancer
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MRS8288 is a ABCG2 and P-glycoprotein inhibitor, with an IC50 of 0.96 μM against ABCG2 and an IC50 of 1.39 μM against P-glycoprotein. MRS8288 inhibits the ATPase activity of ABCG2 and P-glycoprotein, and suppresses ABCG2-mediated substrate transport. MRS8288 is applicable for cancer research .
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- HY-101453R
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P-glycoprotein
Reference Standards
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Cancer
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Ceefourin 1 (Standard) is the analytical standard of Ceefourin 1 (HY-101453). This product is intended for research and analytical applications. Ceefourin 1 is a potent and highly selective multidrug resistance protein 4 (MRP4) inhibitor. Ceefourin 1 inhibits transport of a broad range of MRP4 substrates, yet is highly selective for MRP4 over other ABC transporters. Ceefourin 1 is a benzothiazol and primarily as a chemosensitizer for high-risk neuroblastoma .
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-
- HY-137846A
-
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Acetyl-CoA Carboxylase
OAT
|
Metabolic Disease
Inflammation/Immunology
|
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PF-05221304 tromethamine is an orally active, liver-directed and dual ACC1/ACC2 inhibitor with IC50s of 7.5 nM for rat ACC1, 8.2 nM for rat ACC2. PF-05221304 tromethamine is a substrate for organic anion transport polypeptides. PF-05221304 tromethamine directly improves a variety of non-alcoholic fatty liver (NAFL) and non-alcoholic steatohepatitis (NASH) pathogenic factors .
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- HY-N18471
-
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5,7-DHP
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Monoamine Oxidase
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
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5,7-Dihydroxytryptamine (5,7-DHP) is an autofluorescent (λex≈365 nm), selective neurotoxin and a transport substrate for MAO-A and 5-HT. 5,7-Dihydroxytryptamine can specifically target and damage central and peripheral 5-HTergic neurons, while affecting 5-HT-related pathways and neurotransmitter balance. 5,7-Dihydroxytryptamine can be used to establish 5-HTergic neuron injury models for studies on neural development, neurodegenerative diseases, as well as mechanisms related to platelet function and retinal neurons .
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- HY-N18471A
-
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5,7-DHP hydrobromide
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Monoamine Oxidase
5-HT Receptor
|
Neurological Disease
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5,7-Dihydroxytryptamine (5,7-DHT) hydrobromide is an autofluorescent (Ex ≈ 365 nm), selective neurotoxin and a transport substrate for MAO-A and 5-HT. 5,7-Dihydroxytryptamine hydrobromide can specifically target and damage central and peripheral 5-HTergic neurons, while affecting 5-HT-related pathways and neurotransmitter balance. 5,7-Dihydroxytryptamine hydrobromide can be used to establish 5-HTergic neuron injury models for studies on neural development, neurodegenerative diseases, as well as mechanisms related to platelet function and retinal neurons .
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- HY-N18471B
-
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5,7-DHP creatinine sulfate
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Monoamine Oxidase
5-HT Receptor
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Cardiovascular Disease
Neurological Disease
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5,7-Dihydroxytryptamine creatinine sulfate (5,7-DHT) is an autofluorescent (Ex ≈ 365 nm), selective neurotoxin and a transport substrate for MAO-A and 5-HT. 5,7-Dihydroxytryptamine creatinine sulfate can specifically target and damage central and peripheral 5-HTergic neurons, while affecting 5-HT-related pathways and neurotransmitter balance. 5,7-Dihydroxytryptamine creatinine sulfate can be used to establish 5-HTergic neuron injury models for studies on neural development, neurodegenerative diseases, as well as mechanisms related to platelet function and retinal neurons .
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- HY-101310R
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iGluR
Reference Standards
EAAT
Bcl-2 Family
Caspase
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Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
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SYM 2081 (Standard) is the analytical standard of SYM 2081 (HY-101310). This product is intended for research and analytical applications. SYM 2081 is a kainate receptor agonist. SYM 2081 is a substrate of EAAT1 (Km of 54 μM). SYM 2081 inhibits EAAT2-mediated glutamate transport (Kb is 3.4 μM in Xenopus oocytes), modulates Apoptotic signaling pathways (increases Bcl-2 and decreases Bax/caspase-3 expression). SYM 2081 exhibits neuroprotective activity. SYM 2081 can be used in the study of hypoxic-ischemic brain damage and inflammatory or neuropathic pain .
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- HY-137357
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NSC 305986; γ-MBMTX
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Dihydrofolate reductase (DHFR)
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Cancer
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5-Monobutyl methotrexate (NSC 305986; γ-MBMTX) is a dihydrofolate reductase (DHFR) inhibitor and esterase substrate. 5-Monobutyl methotrexate is hydrolyzed by esterases to produce methotrexate. In rhesus monkeys, 5-Monobutyl methotrexate clears more slowly from cerebrospinal fluid than from serum, and its serum protein binding rate exceeds 99%. At the same dose rate, 5-Monobutyl methotrexate achieves cerebrospinal fluid concentrations comparable to those of Methotrexate (HY-14519), and exhibits activity against Methotrexate-resistant cells (with transport defects) that is comparable to that against sensitive parental cells. 5-Monobutyl methotrexate can be used in studies related to Methotrexate-resistant tumors .
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- HY-164401A
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EAAT
DNA/RNA Synthesis
DNA Alkylator/Crosslinker
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Neurological Disease
Cancer
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QBS10072S dihydrochloride is a bifunctional chemotherapeutic agent that can cross the blood-brain barrier (BBB), comprising a LAT1-targeting domain and a cytotoxic domain. QBS10072S dihydrochloride exhibits inhibitory potency against LAT1-mediated substrate uptake (IC50 = 21 μM) of approximately 50-fold higher than that against LAT2 (IC50 = 1100 μM). QBS10072S dihydrochloride enters LAT1-expressing tumor cells via LAT1-mediated active transport, induces DNA interstrand crosslinking, and causes DNA damage and cell death. QBS10072S dihydrochloride can be used for the research of glioblastoma and aggressive T-cell lymphoma .
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| Cat. No. |
Product Name |
Type |
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- HY-D1078
-
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Fluorescent Dye
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5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate is a fluorescein-based reactive oxygen species (ROS) probe and also a MRP2 substrate. 5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate serves as a substrate for intracellular esterases, which cleave its acetate groups to generate a fluorescent product capable of detecting intracellular ROS. 5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate is ATP-dependent and is transported via a single MRP2 binding site; it competes with LTC4 for MRP2 binding sites and inhibits MRP2-mediated LTC4 transport (Ex/Em = 496/525 nm) .
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- HY-111956B
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Fluorescent Dye
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D-Ala-Lys-AMCA hydrochloride is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA hydrochloride may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA hydrochloride can be used for characterizing PEPT1-specific substrates or inhibitors (Ex/Em = 390/480 nm) .
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- HY-D1584
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Fluorescent Dye
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C12 NBD sphingomyelin is an active derivative of Sphingomyelin (HY-113498) that is tagged with fluorescent C12 nitrobenzoxadiazole (C12 NBD). C12 NBD sphingomyelin can be used as a sphingomyelinase substrate for studying the metabolism and transport of sphingomyelins (Ex=470 nm, Em=525 nm) .
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- HY-111956
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Fluorescent Dye
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D-Ala-Lys-AMCA is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA can be used for characterizing PEPT1-specific substrates or inhibitors (Ex/Em = 390/480 nm) .
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- HY-120649
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Fluorescent Dye
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SKM 4-45-1 is an analog of Anandamide (AEA)(HY-10863). SKM 4-45-1 is a fluorescent substrate, that can be used to study the transmembrane carrier-mediated transport of AEA across cell membranes .
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- HY-111956A
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Fluorescent Dye
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D-Ala-Lys-AMCA TFA is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA TFA may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA TFA can be used for characterizing PEPT1-specific substrates or inhibitors (Ex/Em = 390/480 nm) .
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| Cat. No. |
Product Name |
Type |
-
- HY-134427
-
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Palmitoyl CoA lithium
|
Biochemical Assay Reagents
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Palmitoyl coenzyme A lithium is an acyl-CoA thioester that can be transported into the mitochondrial matrix via the carnitine shuttle system and is involved in β-oxidation. Palmitoyl coenzyme A lithium can also be used as a substrate for sphingosine biosynthesis .
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- HY-D0180
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18C6; 1,4,7,10,13,16-Hexaoxacyclooctadecane
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Biochemical Assay Reagents
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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 .
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- HY-D1078
-
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Biochemical Assay Reagents
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5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate is a fluorescein-based reactive oxygen species (ROS) probe and also a MRP2 substrate. 5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate serves as a substrate for intracellular esterases, which cleave its acetate groups to generate a fluorescent product capable of detecting intracellular ROS. 5 (6)-Carboxy-2',7'-dichlorofluorescein diacetate is ATP-dependent and is transported via a single MRP2 binding site; it competes with LTC4 for MRP2 binding sites and inhibits MRP2-mediated LTC4 transport (Ex/Em = 496/525 nm) .
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- HY-148123
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Biochemical Assay Reagents
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Glycerophospholipids and cephalins are a class of phospholipid compounds and important components of neural membranes. Glycerophospholipids and cephalins are hydrolysis substrates of phospholipase (such as PLA2, PLC, and PLD). After complete hydrolysis, they produce 1 mol of glycerol, phosphate, ethanolamine, and 2 mol of fatty acids, respectively. Glycerophospholipids and cephalins can maintain membrane structure, fluidity, and ion permeability, and serve as precursors of second messengers such as arachidonic acid and diacylglycerol. Glycerophospholipids and cephalins can regulate signal transduction, cell apoptosis, and membrane transport, and are used in the study of neurodegenerative diseases (such as Alzheimer's disease) .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P10856
-
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P-glycoprotein
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Cancer
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CPI1 is a multidrug resistance protein 1 (MRP1) inhibitor with a Ki value of 100 nM. CPI1 binds to the same substrate-binding site as leukotriene C4, stabilizes MRP1 in an apo-like inward-facing conformation, blocks the conformational changes required for ATP hydrolysis and substrate transport, and inhibits the ATPase activity of human and bovine MRP1. CPI1 serves as a tool for investigating the substrate transport mechanism of MRP1. CPI1 is applicable to research related to cancer multidrug resistance .
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- HY-111956B
-
|
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Fluorescent Dye
|
Cancer
|
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D-Ala-Lys-AMCA hydrochloride is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA hydrochloride may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA hydrochloride can be used for characterizing PEPT1-specific substrates or inhibitors (Ex/Em = 390/480 nm) .
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-
- HY-126584
-
|
Val-Val
|
Drug Intermediate
Oligopeptide Cotransporter
|
Others
|
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H-Val-Val-OH (Val-Val) is a stereochemistry-dependent substrate and inhibitor of apical oligopeptide transporters. H-Val-Val-OH undergoes apical intracellular accumulation in human intestinal cells via carrier-mediated transport, and inhibits the uptake of Cephalexin (HY-B0200) through interaction with transporters. Substitution of L-valine with D-valine in H-Val-Val-OH abolishes its binding ability to apical oligopeptide transporters .
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- HY-111956
-
|
|
Fluorescent Dye
|
Cancer
|
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D-Ala-Lys-AMCA is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA can be used for characterizing PEPT1-specific substrates or inhibitors (Ex/Em = 390/480 nm) .
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-
- HY-111956A
-
|
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Fluorescent Dye
|
Cancer
|
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D-Ala-Lys-AMCA TFA is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA TFA may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA TFA can be used for characterizing PEPT1-specific substrates or inhibitors (Ex/Em = 390/480 nm) .
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-
- HY-100838
-
|
L-CCG III
|
EAAT
|
Neurological Disease
|
|
cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. cis-α-(Carboxycyclopropyl)glycine is a substrate of glutamate transporters (GluT) (EC50: 13 μM, 2 μM for EAAT 1 and EAAT 2, respectively). cis-α-(Carboxycyclopropyl)glycine inhibits a Na +-dependent high-affinity L-glutamate uptake in glial plasmalemmal vesicles (GPV) and synaptosomes .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0455
-
-
-
- HY-N0455A
-
-
-
- HY-N2453
-
-
-
- HY-N0455R
-
-
-
- HY-113291
-
-
-
- HY-W353102
-
-
-
- HY-129987
-
-
-
- HY-124009
-
-
-
- HY-N15726
-
-
-
- HY-124009R
-
-
-
- HY-N0455AR
-
|
(S)-(+)-Arginine hydrochloride (Standard)
|
Structural Classification
Natural Products
Endogenous metabolite
Source Classification
|
Reference Standards
NO Synthase
Endogenous Metabolite
|
|
L-Arginine (hydrochloride) (Standard) is the analytical standard of L-Arginine (hydrochloride). This product is intended for research and analytical applications. L-Arginine ((S)-(+)-Arginine) is the substrate for the endothelial nitric oxide synthase (eNOS) to generate NO. L-Arginine is transported into vascular smooth muscle cells by the cationic amino acid transporter family of proteins where it is metabolized to nitric oxide (NO), polyamines, or L-proline. L-Arginine is a potent vasodilator, and can be used to induce experimental acute pancreatitis .
|
-
-
- HY-N2453R
-
|
|
Structural Classification
Ranunculaceae
Adonis amurensis Regel et Radde
Plants
Steroids
|
Reference Standards
PPAR
NF-κB
P-glycoprotein
|
|
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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-
-
- HY-N18471
-
|
5,7-DHP
|
Structural Classification
Alkaloids
Animals
Indole Alkaloids
Source Classification
|
Monoamine Oxidase
5-HT Receptor
|
|
5,7-Dihydroxytryptamine (5,7-DHP) is an autofluorescent (λex≈365 nm), selective neurotoxin and a transport substrate for MAO-A and 5-HT. 5,7-Dihydroxytryptamine can specifically target and damage central and peripheral 5-HTergic neurons, while affecting 5-HT-related pathways and neurotransmitter balance. 5,7-Dihydroxytryptamine can be used to establish 5-HTergic neuron injury models for studies on neural development, neurodegenerative diseases, as well as mechanisms related to platelet function and retinal neurons .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0399S
-
1 Publications Verification
|
|
L-Carnitine-d9 is the deuterium labeled L-Carnitine. L-Carnitine (Levocarnitine) is an endogenous molecule involved in fatty acid metabolism, biosynthesized within the human body using amino acids: L-lysine and L-methionine, as substrates. L-Carnitine functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-carnitine can ameliorate metabolic imbalances in many inborn errors of metabolism .
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-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-N0455
-
|
|
|
Solubilizing Agents
|
|
L-Arginine ((S)-(+)-Arginine) is the substrate for the endothelial nitric oxide synthase (eNOS) to generate NO. L-Arginine is transported into vascular smooth muscle cells by the cationic amino acid transporter family of proteins where it is metabolized to nitric oxide (NO), polyamines, or L-proline. L-Arginine is a potent vasodilator, and can be used to induce experimental acute pancreatitis .
|
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