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Mrp2 Inhibitors

" in MedChemExpress (MCE) Product Catalog:

23

Inhibitors & Agonists

1

Fluorescent Dyes

2

Biochemical Assay Reagents

11

Natural
Products

3

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N1423
    Glycocholic acid
    3 Publications Verification

    		 P-glycoprotein Bcl-2 Family G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite Bacterial Apoptosis FXR Caspase MDM-2/p53 LPL Receptor Metabolic Disease Inflammation/Immunology Cancer
    Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA) .
    Glycocholic acid
  • HY-N0217
    Benzoylaconine
    1 Publications Verification

    Benzoylaconitine; Isaconitine; Pikraconitin

    		 Angiotensin-converting Enzyme (ACE) Reactive Oxygen Species (ROS) Toll-like Receptor (TLR) NF-κB COX NO Synthase p38 MAPK P-glycoprotein Cardiovascular Disease Inflammation/Immunology Cancer
    Benzoylaconine (Benzoylaconitine) is an orally active monoester alkaloid found in the traditional Chinese medicine Aconitum carmichaelii. Benzoylaconine is an ACE2 agonist (EC50: 1.5 μM) with antihypertensive and anti-heart failure effects. Benzoylaconine inhibits TLR-induced MAPK and NF-κB pathways to exert anti-inflammatory effects. Benzoylaconine upregulates the protein levels of P-gp, MRP2, and has anti-tumor effects .
    Benzoylaconine
  • HY-108347
    CP-100356 hydrochloride
    Maximum Cited Publications
    9 Publications Verification

    		 P-glycoprotein BCRP Metabolic Disease
    CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 µM) .
    CP-100356 hydrochloride
  • HY-N1423A
    Glycocholic acid sodium
    3 Publications Verification

    		 P-glycoprotein Bcl-2 Family G protein-coupled Bile Acid Receptor 1 Bacterial Apoptosis FXR Caspase MDM-2/p53 LPL Receptor Endogenous Metabolite Metabolic Disease Cancer
    Glycocholic acid sodium is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid sodium inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid sodium modulates related bile acid receptor signaling. Glycocholic acid sodium suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid sodium can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA) .
    Glycocholic acid sodium
  • HY-N1423S
    Glycocholic acid-d4

    		Isotope-Labeled Compounds P-glycoprotein Bcl-2 Family G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite Bacterial Apoptosis FXR Caspase MDM-2/p53 LPL Receptor Metabolic Disease Cancer
    Glycocholic acid-d4 is the deuterium labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Glycocholic acid-d4
  • HY-D1078
    5(6)-Carboxy-2',7'-dichlorofluorescein diacetate

    		Fluorescent Dye Reactive Oxygen Species (ROS) P-glycoprotein Others
    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) .
    5(6)-Carboxy-2',7'-dichlorofluorescein diacetate
  • HY-B0501
    Danofloxacin mesylate

    CP 76136-27

    		 P-glycoprotein Bacterial Antibiotic Infection
    Danofloxacin mesylate (CP 76136-27) is a fluoroquinolone used as a veterinary drug. Danofloxacin mesylate has a broad spectrum of bactericidal activity, mainly inhibiting the DNA cycloenzyme of the bacteria. In addition, Danofloxacin mesylate is a substrate for ATP-dependent efflux transporters (P-gp and MRP2) .
    Danofloxacin mesylate
  • HY-N0248
    Saikosaponin B2
    2 Publications Verification

    		 HCV P-glycoprotein Infection Cancer
    Saikosaponin B2 is an antiviral and anticancer agent that regulates multiple transporters (such as various solute carriers and ATP-binding cassette transporters including MRP1, MRP2, and OCT2). Saikosaponin B2 is isolated from the plant glycoside component of the roots of Bupleurum scorzonerifolium. Saikosaponin B2 enhances the liver targeting of anticancer drugs via vinegar-baked Radix Bupleuri. Saikosaponin B2 inhibits HCV entry, replication, and translation, is effective against Daclatasvir (HY-10466)-resistant strains, and exerts a synergistic effect when used in combination with Daclatasvir. Saikosaponin B2 is commonly used in studies related to hepatocellular carcinoma and HCV infection .
    Saikosaponin B2
  • HY-W353102
    Estradiol 17-(β-D-Glucuronide)

    		Endogenous Metabolite P-glycoprotein Metabolic Disease
    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 .
    Estradiol 17-(β-D-Glucuronide)
  • HY-129987
    Estradiol 17-(β-D-Glucuronide) sodium

    		Endogenous Metabolite P-glycoprotein Metabolic Disease
    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 .
    Estradiol 17-(β-D-Glucuronide) sodium
  • HY-W013105
    Sodium glycocholate hydrate, 98%

    N-Cholylglycine sodium salt, 98%

    		 Bcl-2 Family Caspase Endogenous Metabolite Bacterial MDM-2/p53 P-glycoprotein LPL Receptor FXR G protein-coupled Bile Acid Receptor 1 Apoptosis Others
    Sodium glycocholate hydrate, 98% is a bile acid derivative. Sodium glycocholate hydrate, 98% downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Sodium glycocholate hydrate, 98% inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Sodium glycocholate hydrate, 98% modulates related bile acid receptor signaling. Sodium glycocholate hydrate, 98% suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Sodium glycocholate hydrate, 98% can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA) .
    Sodium glycocholate hydrate, 98%
  • HY-N1423B
    Glycocholic acid hydrate
    3 Publications Verification

    		 Endogenous Metabolite Caspase G protein-coupled Bile Acid Receptor 1 LPL Receptor MDM-2/p53 Bcl-2 Family P-glycoprotein FXR Bacterial Apoptosis Metabolic Disease Inflammation/Immunology Cancer
    Glycocholic acid hydrate is a bile acid derivative. Glycocholic acid hydrate downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid hydrate inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid hydrate modulates related bile acid receptor signaling. Glycocholic acid hydrate suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid hydrate can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA) .
    Glycocholic acid hydrate
  • HY-N4108
    Hypophyllanthin

    		P-glycoprotein Inflammation/Immunology Cancer
    Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity .
    Hypophyllanthin
  • HY-16773
    Vedroprevir

    GS-9451

    		 HCV Protease BCRP P-glycoprotein Infection
    Vedroprevir (GS-9451) is an inhibitor for HCV NS3/4A protease with an IC50 of 3.2 nM. Vedroprevir is also an inhibitor for breast cancer resistant protein (BCRP) with an IC50 of 1.4 μM. Vedroprevir inhibits P-gp, MRP1 and MRP2 with IC50 of 34, 14.9 and 12 μM, respectively. Vedroprevir exhibits good pharmacokinetic characteristics in rats and dogs .
    Vedroprevir
  • HY-108347A
    CP-100356

    		P-glycoprotein BCRP Metabolic Disease
    CP-100356 is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 is also a weak inhibitor of OATP1B1 (IC50 = ∼66 µM). CP-100356 is devoid of inhibition against MRP2 and major human P450 enzymes (IC50 > 15 µM) .
    CP-100356
  • HY-W702907
    DM-4103

    		P-glycoprotein Metabolic Disease
    DM-4103 is a major metabolite of Tolvaptan (HY-17000) that is metabolized primarily by the CYP3A4 enzyme in the liver. DM-4103 inhibits the ability of human liver transporters NTCP, BSEP, MRP2, MRP3, MRP4 (IC50 values are 16.3, 4.15, 51.0, 44.6, 4.26 μM, respectively) and bile acid transport in SCHH cells. DM-4103 can be used in the study of autosomal dominant polycystic kidney disease (ADPKD) .
    DM-4103
  • HY-N1423S1
    Glycocholic acid-d5

    		Isotope-Labeled Compounds P-glycoprotein Bcl-2 Family G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite Bacterial Apoptosis FXR Caspase MDM-2/p53 LPL Receptor Metabolic Disease Cancer
    Glycocholic acid-d5 is the deuterium labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Glycocholic acid-d5
  • HY-N4108R
    Hypophyllanthin (Standard)

    		Reference Standards P-glycoprotein Inflammation/Immunology Cancer
    Hypophyllanthin (Standard) is the analytical standard of Hypophyllanthin. This product is intended for research and analytical applications. Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity .
    Hypophyllanthin (Standard)
  • HY-B0501R
    Danofloxacin mesylate (Standard)

    CP 76136-27 (Standard)

    		 Reference Standards Bacterial Antibiotic Infection
    Danofloxacin mesylate (Standard) is the analytical standard of Danofloxacin mesylate. This product is intended for research and analytical applications. Danofloxacin mesylate (CP 76136-27) is a fluoroquinolone used as a veterinary drug. Danofloxacin mesylate has a broad spectrum of bactericidal activity, mainly inhibiting the DNA cycloenzyme of the bacteria. In addition, Danofloxacin mesylate is a substrate for ATP-dependent efflux transporters (P-gp and MRP2) .
    Danofloxacin mesylate (Standard)
  • HY-N1423AR
    Glycocholic acid sodium (Standard)

    		Reference Standards P-glycoprotein Bcl-2 Family G protein-coupled Bile Acid Receptor 1 Bacterial Apoptosis FXR Caspase MDM-2/p53 LPL Receptor Endogenous Metabolite Metabolic Disease Cancer
    Glycocholic acid (sodium) (Standard) is the analytical standard of Glycocholic acid sodium (HY-N1423A). This product is intended for research and analytical applications. Glycocholic acid sodium is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid sodium inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid sodium modulates related bile acid receptor signaling. Glycocholic acid sodium suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid sodium can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Glycocholic acid sodium (Standard)
  • HY-W754548
    Glycocholic acid-13C2,d4

    		Isotope-Labeled Compounds Endogenous Metabolite P-glycoprotein Bcl-2 Family G protein-coupled Bile Acid Receptor 1 Bacterial Apoptosis FXR Caspase MDM-2/p53 LPL Receptor Metabolic Disease Cancer
    Glycocholic acid- 13C2,d4 is the deuterium labeled and 13C-labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Glycocholic acid-13C2,d4
  • HY-N0248R
    Saikosaponin B2 (Standard)

    		Reference Standards P-glycoprotein HCV Infection Cancer
    Saikosaponin B2 (Standard) is the analytical standard of Saikosaponin B2. This product is intended for research and analytical applications. Saikosaponin B2 is an antiviral and anticancer agent that regulates multiple transporters (such as various solute carriers and ATP-binding cassette transporters including MRP1, MRP2, and OCT2). Saikosaponin B2 is isolated from the plant glycoside component of the roots of Bupleurum scorzonerifolium. Saikosaponin B2 enhances the liver targeting of anticancer drugs via vinegar-baked Radix Bupleuri. Saikosaponin B2 inhibits HCV entry, replication, and translation, is effective against Daclatasvir (HY-10466)-resistant strains, and exerts a synergistic effect when used in combination with Daclatasvir. Saikosaponin B2 is commonly used in studies related to hepatocellular carcinoma and HCV infection .
    Saikosaponin B2 (Standard)
  • HY-108347R
    CP-100356 hydrochloride (Standard)

    		Reference Standards P-glycoprotein BCRP Metabolic Disease
    CP-100356 hydrochloride (Standard) is the analytical standard of CP-100356 (hydrochloride) (HY-108347). This product is intended for research and analytical applications. CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 µM) .
    CP-100356 hydrochloride (Standard)

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