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Results for "

P-gp/MDR1

" in MedChemExpress (MCE) Product Catalog:

22

Inhibitors & Agonists

3

Natural
Products

6

Antibodies

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Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-17013
    Dofequidar
    2 Publications Verification

    MS-209 free base

    		 P-glycoprotein Cancer
    Dofequidar (MS-209 free base) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
    Dofequidar
  • HY-101511
    TTT-28

    		P-glycoprotein Cancer
    TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1 .
    TTT-28
  • HY-162495
    IDOR-1117-2520

    		CCR Calcium Channel Arrestin P-glycoprotein Inflammation/Immunology Cancer
    IDOR-1117-2520 is an orally active, potent, selective and reversible CCR6 antagonist. IDOR-1117-2520 antagonizes the CCL20-mediated calcium flow (IC50 = 63 nM) and inhibits β-arrestin recruitment to human CCR6 (IC50 = 30 nM) in cells expressing recombinant human CCR6. IDOR-1117-2520 is found to be a substrate of P-gp/MDR1. IDOR-1117-2520 can be used in the research of autoimmune diseases and skin inflammation .
    IDOR-1117-2520
  • HY-N1941
    Isosinensetin

    		P-glycoprotein Bacterial HIV Protease Phosphatase Reactive Oxygen Species (ROS) NF-κB p38 MAPK ERK JNK Calcium Channel Infection Metabolic Disease Inflammation/Immunology Cancer
    Isosinensetin is a flavonoid compound and an inhibitor of HIV-1 protease and PTP1B (IC50: 2.61 µM; Ki: 0.92 µM). Isosinensetin inhibits P-glycoprotein (P-gp) in MDR1-MDCKII cells. Isosinensetin has multiple activities such as anti-tumor, anti-viral, anti-inflammatory, and antioxidant effects. Isosinensetin can be used in the research of various diseases including cancer, inflammation, osteoporosis, diabetes, etc .
    Isosinensetin
  • HY-108694
    γ-Tocotrienol
    4 Publications Verification

    		 Endogenous Metabolite NF-κB Metabolic Disease Inflammation/Immunology
    γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment .
    γ-Tocotrienol
  • HY-W018791
    Bifendate
    2 Publications Verification

    DDB

    		 HBV Autophagy Cytochrome P450 Atg8/LC3 p62 P-glycoprotein Infection Cardiovascular Disease Cancer
    Bifendate (DDB), extracted from Schisandrae chinensis, is an orally active anti-HBV agent against chronic hepatitis B. Bifendate inhibits ATG5-dependent autophagy and attenuates oleic acid-induced lipid accumulation with anti-oxidant properties in vitro. Bifendate can decrease alanine transaminase (ALT) level in mice. Bifendate attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Bifendate potently increases the activity of cytochrome proteins (CYPs) and reverse P-gp-mediated multi-drug resistance (MDR) .
    Bifendate
  • HY-17013A
    Dofequidar fumarate
    2 Publications Verification

    MS-209

    		 P-glycoprotein Cancer
    Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar fumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar fumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
    Dofequidar fumarate
  • 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-13646B
    Encequidar hydrochloride

    HM30181 hydrochloride; HM30181A hydrochloride

    		 P-glycoprotein Others
    Encequidar hydrochloride (HM30181 hydrochloride) is an oral P-glycoprotein (P-gp) inhibitor with the activity of enhancing the oral bioavailability of P-gp substrate drugs. Encequidar shows the highest potency among various MDR1 inhibitors, with IC50=0.63nM. Encequidar effectively blocks the transepithelial transport of paclitaxel in MDCK monolayer cells, with IC50=35.4nM .
    Encequidar hydrochloride
  • HY-17013D
    Dofequidar sesquifumarate

    MS-209 sesquifumarate

    		 P-glycoprotein Cancer
    Dofequidar (MS-209) sesquifumarate is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar sesquifumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar sesquifumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
    Dofequidar sesquifumarate
  • HY-155152
    P-gp/BCRP-IN-2

    		P-glycoprotein BCRP Cancer
    P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells .
    P-gp/BCRP-IN-2
  • HY-108694R
    γ-Tocotrienol (Standard)

    		Reference Standards Endogenous Metabolite NF-κB Metabolic Disease Inflammation/Immunology
    γ-Tocotrienol (Standard) is the analytical standard of γ-Tocotrienol. This product is intended for research and analytical applications. γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment .
    γ-Tocotrienol (Standard)
  • HY-W018791R
    Bifendate (Standard)

    DDB (Standard)

    		 Reference Standards HBV Autophagy Cytochrome P450 Atg8/LC3 p62 P-glycoprotein Infection Cardiovascular Disease Cancer
    Bifendate (DDB), extracted from Schisandrae chinensis, is an orally active anti-HBV agent against chronic hepatitis B. Bifendate inhibits ATG5-dependent autophagy and attenuates oleic acid-induced lipid accumulation with anti-oxidant properties in vitro. Bifendate can decrease alanine transaminase (ALT) level in mice. Bifendate attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Bifendate potently increases the activity of cytochrome proteins (CYPs) and reverse P-gp-mediated multi-drug resistance (MDR) .
    Bifendate (Standard)
  • HY-112912
    P-gp modulator 1

    		P-glycoprotein Cancer
    P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR) .
    P-gp modulator 1
  • HY-162495A
    (S)-IDOR-1117-2520

    		Drug Isomer CCR Calcium Channel Arrestin P-glycoprotein Inflammation/Immunology
    (S)-IDOR-1117-2520 is the S-isomer of IDOR-1117-2520 (HY-162495). IDOR-1117-2520 is an orally active, potent, selective and reversible CCR6 antagonist. IDOR-1117-2520 antagonizes the CCL20-mediated calcium flow (IC50 = 63 nM) and inhibits β-arrestin recruitment to human CCR6 (IC50 = 30 nM) in cells expressing recombinant human CCR6. IDOR-1117-2520 is found to be a substrate of P-gp/MDR1. IDOR-1117-2520 can be used in the research of autoimmune diseases and skin inflammation .
    (S)-IDOR-1117-2520
  • HY-181114
    P-gp-IN-34

    		P-glycoprotein Fungal Infection
    P-gp-IN-34 (compound 4a) is an Mdr1p (Mdr1 pump) inhibitor. P-gp-IN-34 inhibits yeast to hyphal shift in Candida albicans. P-gp-IN-34 can be used for the research of candidiasis .
    P-gp-IN-34
  • HY-17013AR
    Dofequidar fumarate (Standard)

    MS-209 (Standard)

    		 P-glycoprotein Reference Standards Cancer
    Dofequidar (fumarate) (Standard) is the analytical standard of Dofequidar (fumarate). This product is intended for research and analytical applications. Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar fumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar fumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
    Dofequidar fumarate (Standard)
  • HY-183143
    Lss-11

    		Topoisomerase Apoptosis TNF Receptor PARP STAT P-glycoprotein Cancer
    Lss-11 is a topoisomerase inhibitor. LSS-11 enhances cell death in cancer cells by inducing apoptosis through increasing the DR5 protein level and PARP1 cleavage. LSS-11 dose-dependently reduces STAT3 phosphorylation, downregulates its target genes MDR1 and MRP1, reduces P-gp protein expressionwithout affecting P-gp transport function. Lss-11 is a chemosensitizer and shows synergistic anticancer effect with Paclitaxel (HY-B0015). Lss-11 can be used for the research of paclitaxel-resistant lung cancer .
    Lss-11
  • 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)
  • HY-101511R
    TTT-28 (Standard)

    		P-glycoprotein Reference Standards Cancer
    TTT-28 (Standard) is the analytical standard of TTT-28 (HY-101511). This product is intended for research and analytical applications. TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1 .
    TTT-28 (Standard)
  • HY-165444
    CP-615003

    NGD-913

    		 GABA Receptor Neurological Disease
    CP-615003 is a potent and subtype-selective partial agonist of GABAA receptor (GABAA receptor) (Ki = 1.1 μM). CP-615003 is mainly converted into the active metabolite CP-900725 through oxidative deamination in monkeys and humans, and the latter also has GABAA receptor affinity. CP-615003 is a substrate of P-glycoprotein (P-gp/MDR1), resulting in severe limitation of its penetration into the central nervous system (CNS). CP-615003 can be used for the study of CNS-related indications .
    CP-615003

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