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Oatp Inhibitors

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35

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1

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2

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11

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5

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-D1063
    IR-780
    5+ Cited Publications

    		 Fluorescent Dye Apoptosis Reactive Oxygen Species (ROS) Cancer
    IR-780 is a near-infrared fluorescent probe for in vivo imaging of tumor cells. IR-780 is transported into tumor cells via OATPs and ABCB10, with uptake dependent on glycolytic activity and plasma membrane potential. IR-780 preferentially accumulates in tumor cell mitochondria, including those of drug-resistant cancer cells, without chemical conjugation. IR-780 generates reactive oxygen species (ROS), induces hyperthermia and apoptosis, inhibits tumor growth and recurrence, and modulates HSP70 expression upon ultrasound or 808 nm laser exposure. IR-780 acts as a sonosensitizer, photodynamic and photothermal agent, and drug delivery carrier, with low acute imaging-dose toxicity and rapid vital organ clearance. IR-780 can be used for the research of cancer, such as breast cancer, lung cancer, and non-small cell lung cancer (NSCLC) .
    IR-780
  • HY-N3513
    Mulberrin
    5+ Cited Publications

    Kuwanon C

    		 OAT Cardiovascular Disease
    Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8?±1.5 μM.
    Mulberrin
  • HY-10466
    Daclatasvir
    Maximum Cited Publications
    47 Publications Verification

    BMS-790052; EBP 883

    		 HCV Infection
    Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively .
    Daclatasvir
  • HY-119695
    Simvastatin acid

    Tenivastatin

    		 HMG-CoA Reductase (HMGCR) Reactive Oxygen Species (ROS) Cardiovascular Disease Cancer
    Simvastatin acid (Tenivastatin), a hydrolysate of Simvastatin (HY-17502), is a HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
    Simvastatin acid
  • HY-115292
    Simvastatin hydroxy acid sodium
    1 Publications Verification

    Tenivastatin sodium; Simvastatin Impurity A sodium

    		 HMG-CoA Reductase (HMGCR) Reactive Oxygen Species (ROS) Cardiovascular Disease Inflammation/Immunology
    Simvastatin hydroxy acid (Tenivastatin) sodium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin hydroxy acid sodium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin hydroxy acid sodium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
    Simvastatin hydroxy acid sodium
  • HY-10465
    Daclatasvir dihydrochloride
    Maximum Cited Publications
    47 Publications Verification

    BMS-790052 dihydrochloride; EBP 883 dihydrochloride

    		 HCV Infection
    Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also an organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively .
    Daclatasvir dihydrochloride
  • HY-16278
    Pradigastat
    2 Publications Verification

    LCQ-908

    		 Acyltransferase BCRP OAT Infection Metabolic Disease
    Pradigastat (LCQ-908) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC50 at 0.157 µM. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC50 of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro .
    Pradigastat
  • HY-108347
    CP-100356 hydrochloride
    5+ Cited Publications

    		 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-119695A
    Simvastatin acid ammonium
    1 Publications Verification

    Tenivastatin ammonium

    		 HMG-CoA Reductase (HMGCR) Reactive Oxygen Species (ROS) Cardiovascular Disease Inflammation/Immunology
    Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
    Simvastatin acid ammonium
  • HY-137888A
    Oxidized ATP trisodium salt

    Oatp trisodium salt

    		 P2X Receptor NOD-like Receptor (NLR) Inflammation/Immunology
    Oxidized ATP (oATP) trisodium salt is a broad-spectrum P2 receptor inhibitor. Oxidized ATP trisodium salt irreversibly antagonizes P2X7R activation. Oxidized ATP trisodium salt inhibits c-reactive protein (CRP)-induced NLRP3 inflammasome activation. Oxidized ATP trisodium salt can be used for research of atherosclerosis .
    Oxidized ATP trisodium salt
  • 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-W002438
    6-Hydroxyindole

    		Biochemical Assay Reagents Endogenous Metabolite OAT Ferroptosis Neurological Disease Metabolic Disease
    6-Hydroxyindole is an orally active, endogenous long-acting OATP1B1 inhibitor. 6-Hydroxyindole does not alter the cell surface expression or subcellular localization of OATP1B1. 6-Hydroxyindole protects cells against Ferroptosis. 6-Hydroxyindole possesses intrinsic radical-trapping antioxidant activity. 6-Hydroxyindole serves as a component of oxidative hair dyes. 6-Hydroxyindole can be used in research related to renal failure and neurodegenerative diseases .
    6-Hydroxyindole
  • HY-10465R
    Daclatasvir dihydrochloride (Standard)

    BMS-790052 dihydrochloride (Standard); EBP 883 dihydrochloride (Standard)

    		 Reference Standards HCV Infection
    Daclatasvir (dihydrochloride) (Standard) is the analytical standard of Daclatasvir (dihydrochloride). This product is intended for research and analytical applications. Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also an organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively .
    Daclatasvir dihydrochloride (Standard)
  • HY-119695B
    Simvastatin acid calcium hydrate

    Tenivastatin calcium hydrate

    		 HMG-CoA Reductase (HMGCR) Reactive Oxygen Species (ROS) Cardiovascular Disease Inflammation/Immunology
    Simvastatin acid (Tenivastatin) calcium hydrate is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid calcium hydrate reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid calcium hydrate can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
    Simvastatin acid calcium hydrate
  • HY-155668
    HMG-CoA Reductase-IN-1

    		HMG-CoA Reductase (HMGCR) Metabolic Disease
    HMG-CoA Reductase-IN-1 is a HMG-CoA reductase inhibitor. HMG-CoA Reductase-IN-1has high HMGR inhibitory activity and OATP1B1 affinity with pIC50 and pKm values of 8.54 and 1.98, respectively. HMG-CoA Reductase-IN-1 can be used for the research of hypercholesterolemia .
    HMG-CoA Reductase-IN-1
  • 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-N8497
    Leoidin

    		Bacterial Infection
    Leoidin is an OATP1B1 and OATP1B3 inhibitor with Ki values of 0.08 and 1.84 μM，respectively. Leoidin inhibits sodium fluorescein uptake in CHO cells expressing the human OATP1B1 and OATP1B3. Leoidin is an antibacterial agent against both Gram-positive and Gram-negative pathogens. Leoidin inhibits phenylalanyl-tRNA synthetase (PheRS) (IC50= 42 μM) and inhibits protein synthesis in bacterial. Leoidin can be isolated from L. gangaleoides .
    Leoidin
  • HY-138142
    Euphol acetate

    		OAT Metabolic Disease
    Euphol acetate is a triterpene that can be isolated from Euphorbia broteri. Euphol acetate is an inhibitor of hepatic transport proteins organic anion-transporting polypeptide 1/3 (OATP1B1/3) .
    Euphol acetate
  • HY-N3513R
    Mulberrin (Standard)

    Kuwanon C (Standard)

    		 Reference Standards Others Cardiovascular Disease
    Mulberrin (Standard) is the analytical standard of Mulberrin. This product is intended for research and analytical applications. Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
    Mulberrin (Standard)
  • HY-10466S
    Daclatasvir-d6

    BMS-790052-d6; EBP 883-d6

    		 Isotope-Labeled Compounds HCV Infection
    Daclatasvir-d6 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively .
    Daclatasvir-d6
  • HY-10466S2
    Daclatasvir-d16

    BMS-790052-d16; EBP 883-d16

    		 Isotope-Labeled Compounds HCV Infection
    Daclatasvir-d16 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively .
    Daclatasvir-d16
  • HY-119695AR
    Simvastatin acid ammonium (Standard)

    Tenivastatin ammonium (Standard)

    		 Reference Standards HMG-CoA Reductase (HMGCR) Reactive Oxygen Species (ROS) Cardiovascular Disease Inflammation/Immunology
    Simvastatin acid (ammonium) (Standard) is the analytical standard of Simvastatin acid (ammonium). This product is intended for research and analytical applications. Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
    Simvastatin acid ammonium (Standard)
  • HY-10466R
    Daclatasvir (Standard)

    BMS-790052 (Standard); EBP 883 (Standard)

    		 Reference Standards HCV Infection
    Daclatasvir (Standard) is the analytical standard of Daclatasvir. This product is intended for research and analytical applications. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively .
    Daclatasvir (Standard)
  • HY-119695S
    Simvastatin acid-d6

    Tenivastatin-d6

    		 Isotope-Labeled Compounds HMG-CoA Reductase (HMGCR) Reactive Oxygen Species (ROS) Cardiovascular Disease Cancer
    Simvastatin acid-d6 (Tenivastatin-d6) is deuterium labeled Simvastatin acid. Simvastatin acid (Tenivastatin), a hydrolysate of Simvastatin (HY-17502), is a HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
    Simvastatin acid-d6
  • HY-119695AS1
    Simvastatin acid-d9 ammonium

    Tenivastatin-d9 ammonium

    		 HMG-CoA Reductase (HMGCR) Reactive Oxygen Species (ROS) Isotope-Labeled Compounds Cardiovascular Disease Inflammation/Immunology
    Simvastatin acid-d9 ammonium is deuterated labeled Simvastatin acid ammonium (HY-119695A). Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
    Simvastatin acid-d9 ammonium
  • HY-16278A
    Pradigastat sodium

    LCQ 908 sodium

    		 Acyltransferase BCRP OAT Infection Metabolic Disease
    Pradigastat sodium (LCQ 908 sodium) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC50 at 0.157 µM. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC50 of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro .
    Pradigastat sodium
  • HY-10466S1
    Daclatasvir-13C2,d6

    BMS-790052-13C2,d6; EBP 883-13C2,d6

    		 Isotope-Labeled Compounds HCV Infection
    Daclatasvir- 13C2,d6 (BMS-790052- 13C2,d6) is 13C and deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively .
    Daclatasvir-13C2,d6
  • HY-N15726
    Obtusichromoneside C

    		Others Others
    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 .
    Obtusichromoneside C
  • HY-W002438R
    6-Hydroxyindole (Standard)

    		Biochemical Assay Reagents Reference Standards Endogenous Metabolite Inflammation/Immunology
    6-Hydroxyindole (Standard) is the analytical standard of 6-Hydroxyindole. This product is intended for research and analytical applications. 6-Hydroxyindole is a biochemical reagent. 6-hydroxyindole is an endogenous long-lasting OATP1B1 inhibitor, and is elevated plasma of the renal failure patients .
    6-Hydroxyindole (Standard)
  • HY-16278R
    Pradigastat (Standard)

    LCQ-908 (Standard)

    		 Acyltransferase BCRP OAT Reference Standards Infection Metabolic Disease
    Pradigastat (Standard) is the analytical standard of Pradigastat. This product is intended for research and analytical applications. Pradigastat (LCQ-908) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC50 at 0.157 µM. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC50 of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro .
    Pradigastat (Standard)
  • HY-173231
    hURAT1 inhibitor 2

    		URAT1 Metabolic Disease
    hURAT1 inhibitor 2 (Compound 5) is an inhibitor of hURAT1 (uric acid transporter 1, SLC22A12) with an IC50 of 18 nM. hURAT1 inhibitor 2 also has a certain inhibitory effect on OATP1B1, with an IC50 value of 0.73 μM. hURAT1 inhibitor 2 can be used in the research of diseases related to abnormal uric acid metabolism, such as hyperuricemia and gout .
    hURAT1 inhibitor 2
  • HY-155062
    IR-251

    		Mitochondrial Metabolism Reactive Oxygen Species (ROS) β-catenin Fluorescent Dye PPAR Cancer
    IR-251 is a mitochondrion-targeting NIR fluorescent probe. IR-251 targets mitochondria via OATPs and causes mitochondrial damage in tumor cells. IR-251 IR-251 induced ROS overproduction by inhibiting PPARγ, and then inhibiting the β-catenin signaling pathway and downstream protein molecules related to the cell cycle and metastasis. IR-251 inhibits tumor proliferation and metastasis .
    IR-251
  • HY-161821
    Antitumor agent-173

    		Interleukin Related TNF Receptor MMP Cancer
    Antitumor agent-173 (Compound 4b) is a prodrug of Cycloicaritin (HY-N1940). Antitumor agent-173 is a substrate for OATP2B1. Antitumor agent-173 selectively inhibits the growth of tumor Antitumor agent-173 significantly increases the oral bioavailability of Cycloicaritin and exerts good antitumor activity and safety .
    Antitumor agent-173
  • 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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