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P-gp

P-glycoprotein (P-gp) is a plasma membrane protein which acts as a localized drug transport mechanism, actively exporting drugs out of the cell. The effects of P-gp on the distribution, metabolism and excretion of drugs — including protease inhibitors — in the body is great.

  • Elacridar
    T2657143664-11-3
    Elacridar (GG918) (GF120918) is an effective BCRP and P-gp (MDR-1) inhibitor.
    • $35
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  • HM-30181 mesylate monohydrate
    T91732097125-58-9
    HM-30181 mesylate monohydrate is an oral P-glycoprotein (P-gp) inhibitor, used to enhance the oral bioavailability of P-gp substrate drugs.
    • $63
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  • Tepotinib hydrochloride(1 : x)
    T96011103508-80-0
    Tepotinib hydrochloride(1 : x) is an orally bioavailable, mesenchymal-epithelial transition (MET) TKI developed mainly for selected NSCLC patients with METex14 skipping mutations.
    • $148
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  • Alisol F 24-acetate
    TMA2270443683-76-9
    Alisol F 24-acetate is a natural product isolated from Alisma plantago-aquatica Linn[1]. Alisol F 24 Acetate enhances chemosensitivity and apoptosis of MCF-7/DOX Cells by inhibiting P-Glycoprotein-Mediated drug efflux[2].
    • $179
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  • Laniquidar TFA
    T64133L
    Laniquidar TFA (R101933) is a novel orally available non-competitive P-glycoprotein (P-gp) inhibitor with an IC50 value of 0.51 μM.Laniquidar has limited bioavailability and can be used to modulate the multidrug resistance transporter.Laniquidar can be used for the study of AML and myelodysplastic syndrome (MDS). Laniquidar is used to study acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS).
    • $350
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  • FM04
    T720551807320-40-6In house
    FM04 is an orally active and highly potent inhibitor of P-glycoprotein (P-gp) with an EC50 value of 83 nM. FM04 can interact with Q1193 and I1115 in human P-gp nucleotide binding domain 2 (NBD2). Thereby disrupting the R262-Q1081-Q1118 interaction pocket and uncoupling the ICL2-NBD2 interaction, thereby inhibiting P-gp. FM04 can be used in the treatment of cancer and tumors.
    • $195
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  • Phellamurin
    TN476152589-11-4
    Phellamurin inhibits intestinal P-glycoprotein in a dose-dependent manner, there is a serious interaction occurred between Phellamurin with cyclosporin, to ensure the efficacy of cyclosporin, we suggest that the coadministration of Phellamurin or Phellode
    • $166
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  • MCI826
    T16026140646-80-6
    MCI826 is a potent and selective antagonist of P-glycoprotein (P-gp) and peptide leukotrienes (p-LTs), showing anti-asthmatic activity in a guinea pig model of advanced asthma.
    • $700
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  • P-gb-IN-1
    T775752632874-49-6
    P-gb-IN-1 is a potent P-glycoprotein (P-gp) inhibitor that exhibits reverse activity by inhibiting P-gp outflow. P-gb-IN-1 has been shown to inhibit P-gp by hydrogen bonding with residues Asn 721 and Met 986. P-gb-IN-1 showed low toxicity in MCF-7/ADR cells.
    • $195
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  • PGP-4008
    T28396365565-02-2In house
    PGP-4008 is a selective and potent P-glycoprotein (Pgp) inhibitor that inhibits tumor growth by co-administration with Doxorubicin.
    • $64
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  • Piperine
    T300294-62-2
    Piperine (Bioperine) , a alkaloid, has been used in trials studying the treatment of multiple myeloma and deglutition disorders.
    • $29
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    TargetMol | Citations Cited
  • Muscone
    T2893541-91-3
    Muscone (3-Methylcyclopentadecanone) is an organic compound that is the primary contributor to the odor of musk.
    • $39
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  • Selamectin
    T4059220119-17-5
    Selamectin (UK-124114) is a macrocyclic lactone derivative of ivermectin, an anthelmintic that potentiates glutamate- and GABA-gated chloride channel opening in nematodes. In an H. contortus larval development assay, selamectin (0.1 μg/ml) shows the effect of growth inhibition.
    • $30
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  • Trifluoperazine
    T8389117-89-5
    Trifluoperazine (trifluoroperazine) is a Dopamine D2 receptor inhibitor(IC50 : 1.2 nM), and Treatment of schizophrenia.
    • $41
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  • Glibenclamide
    T163410238-21-8
    Glibenclamide (Glyburide) is an antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.
    • $45
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  • Verapamil
    T2065652-53-9
    Verapamil (CP-16533-1) is a calcium channel blocker and an orally active and effective inhibitor of P-gp. Verapamil inhibits CYP3A4 and can be used in studies about the treatment of high blood pressure, heart arrhythmias, and angina research.
    • $30
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  • Trifluoperazine dihydrochloride
    T1222440-17-5
    Trifluoperazine dihydrochloride (SKF5019) is a potent dopamine D2 receptor inhibitor used as an antipsychotic and an antiemetic.
    • $50
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  • Sinapine
    T2S120018696-26-9
    1. Sinapine, an alkaloid from seeds of the cruciferous species, can be used as an effective natural compound for chemo-resistance. 2. Sinapine has antioxidant and radio-protective activities.
    • $72
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  • Cinchonine
    T0012118-10-5
    Cinchonine (LA40221), a local anesthetic of the amide type, now generally used for surface anesthesia. It is one of the most potent and toxic of the long-acting local narcotics and its parenteral use is restricted to spinal anesthesia.
    • $44
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  • Atazanavir
    T0100L198904-31-3
    Atazanavir (BMS-232632)(BMS-232632) is an highly effective HIV-1 protease inhibitor.
    • $39
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  • Risperidone
    T0351106266-06-2
    Risperidone (R 64 766) is a selective blocker of dopamine D2 receptors and serotonin 5-HT2 receptors that act as an atypical antipsychotic agent.
    • $43
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    TargetMol | Citations Cited
  • Jatrophane 5
    TN2726210108-89-7
    Jatrophane 5 demonstrates the most powerful inhibition of P-gp, higher than R(+)-verapamil and tariquidar in colorectal multi-drug resistant (MDR) cells (DLD1-TxR).
    • $2,210
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  • Polyoxyethylene stearate
    T165619004-99-3
    Polyoxyethylene stearate (POES) is an agent of non-ionic emulsifying.
    • $30
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  • Tanshinone IIB
    TN225717397-93-2
    Co-treatment with Tanshinone IIB (TSB) significantly inhibits the DNA laddering, cytotoxicity and apoptosis of rat cortical neurons induced by staurosporine in a concentration-dependent manner; TSB also suppresses the elevated Bax protein and decreased bc
    • $2,098
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  • Lappaol C
    TN441064855-00-1
    Lappaol C has antioxidant and antiaging properties, it may promote the C. elegans longevity and stress resistance through a JNK-1-DAF-16 cascade. Lappaol C also has potential chemosensitizing activity, it may be candidates for developing novel adjuvant an
    • $730
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  • Pepluanin A
    TN4749670257-89-3
    Pepluanin A, shows a very high activity for a jatrophane diterpene, outperforming cyclosporin A by a factor of at least 2 in the inhibition of Pgp-mediated daunomycin transport.
    • $2,210
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  • Taxinine
    TN51143835-52-7
    Taxinine and Taxinine B can inhibit the drug transport by P-glycoprotein in multidrug-resistant cells.
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  • Ganoderenic acid B
    T2S1120100665-41-6
    Ganoderenic acid B, a natural product derived from Ganoderma lucidum, can work by inhibiting the transport function of ABCB1 and enhancing the cytotoxicity of chemotherapy drugs against AbCB1-mediated multidrug resistant cancer cells.
    • $89
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  • Lappaol F
    TN441169394-17-8
    1. Lappaol F has antioxidant and antiaging properties, it may promote the C. elegans longevity and stress resistance through a JNK-1-DAF-16 cascade.
    2. Lappaol F has potential chemosensitizing activity, it may be candidates for developing novel adju
    • $361
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  • YS-370
    T600092470908-79-1
    YS-370 is an orally active inhibitor of P-gp and shows moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance to paclitaxel and colchicine and exhibits stronger antitumor activity in combination with paclitaxel.
    • $58
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  • Hypophyllanthin
    TN175733676-00-5
    Hypophyllanthin and phyllanthin have antitumour effects against Ehrlich Ascites Carcinoma in mice.
    • $98
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  • Isosinensetin
    T2S022317290-70-9
    1. Isosinensetin (6-Demethoxynobiletin) shows antioxidant and HIV-1 protease inhibiting activities.
    • $60
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  • P-gp inhibitor 1
    T123412050747-49-2
    P-gp inhibitor 1 inhibits reversing P-glycoprotein-mediated multidrug resistance with an EC50 of 57.9 nM (K562/A02 cells).
    • $31
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  • (-)-Praeruptorin A
    TN481914017-71-1
    (-)-Praeruptorin A has anti-inflammatory, anti-contractile and anti-hyperplasia activities, it exerts distinct relaxant effects on isolated rat aorta rings dependent on endothelium and nitric oxide synthesis;it also can significantly suppress airway inflammation and airway remodeling induced by ovalbumin challenge, and is a potential candidate for the treatment of asthma. (-)-Praeruptorin A resensitizes Pgp-mediated MDR (Pgp-MDR) cancer cells to cancer drugs.
    • $320
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  • Dofequidar fumarate
    T11071153653-30-6
    Dofequidar fumarate (MS-209)(MS-209 fumarate), a quinoline-based compound administered orally, is known for counteracting multidrug resistance (MDR) through the inhibition of ABCB1/P-glycoprotein (P-gp) and ABCC1/MDR-associated protein 1.
    • $33
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  • Pristinamycin IA
    T125403131-03-1
    Pristinamycin IA (Mikamycin B) is a substrate for the P-glycoprotein and a cyclo-peptidic macrolactone antibiotic.
    • $97
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  • Larotaxel
    T15713156294-36-9
    Larotaxel (XRP9881) is a taxane analogue that has anticancer activity, exerts its cytotoxic effects by promoting tubulin assembly and stabilizing microtubules, and ultimately induces cell death through apoptosis. Larotaxel (XRP9881) is a compound that crosses the blood-brain barrier and has a higher affinity for Docetaxel than P-glycoprotein 1, which can be used to study breast and bladder cancer.
    • $123
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  • Pafenolol
    T6812475949-61-0
    Pafenolol is a P-glycoprotein modulator with a Ki value of 5.5 µM. pafenolol is an orally available and selective beta-adrenergic receptor antagonist.
    • $86
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  • Taxuspine X
    TN5124194782-02-0
    Taxuspine X may have p-glycoprotein inhibitory activity.
    • $680
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  • Bacoside A3
    TN1425157408-08-7
    Bacoside A3 has antioxidant potential, it shows comparatively higher neuroprotective response analysed as higher cell viability and decreased intracellular ROS.
    • $68
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  • 7beta-Hydroxylathyrol
    T2S201834208-98-5
    7β-Hydroxylathyrol is a diterpenoid extract from the seed oil of Caper Spurge and displays P-gp inhibition resulting in cytotoxic properties.
    • $66
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  • Norverapamil hydrochloride
    T1633967812-42-4
    Norverapamil hydrochloride (D591 hydrochloride) ((±)-Norverapamil hydrochloride) is an N-demethylated metabolite of Verapamil and it is an L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
    • $31
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  • Jatrophane 2
    TN2727210108-86-4
    2,5,7,8,9,14-Hexaacetoxy-3-benzoyloxy-15-hydroxyjatropha-6(17),11E-diene (Jatrophane 2 ) exhibits significant antifeedant activity against a generalist plant-feeding insect, the cotton bollworm (Helicoverpa armigera). Jatrophane 2 also demonstrates the mo
    • $740
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  • Verapamil hydrochloride
    T1010152-11-4
    Verapamil hydrochloride (Verapamil HCl) is a calcium channel blocker that is a class IV anti-arrhythmia agent.
    • $41
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  • Sinapine thiocyanate
    T33927431-77-8
    Sinapine Thiocyanate, is a derivative of Sinapine (S486605), an alkaloidal amine found in black mustard seeds. It is the choline ester of Sinapic Acid (S486800). It is also a phenolic-chloine conjugates, acting as anti-oxidants and acetylcholinesterase inhibitors, that can be used for the treatment of Alzheimer's disease (AD).
    • $55
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  • Zosuquidar trihydrochloride
    T6018167465-36-3
    Zosuquidar trihydrochloride (LY-335979 trihydrochloride) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.
    • $30
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  • Chrysosplenetin
    TJS1159603-56-5
    Chrysosplenetin is a metabolic inhibitor of artemisinin.
    • $55
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  • Cinobufotalin
    T4A23991108-68-5
    Cinobufotalin is a main cardiac toxin in toad, it is a novel anti-HCC agent, it induces growth inhibition and apoptosis in cultured HCC cells through ceramide production. Cinobufotalin is also an effective reversal agent for the multidrug resistance of tu
    • $44
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  • Furanodiene
    TN165119912-61-9
    Furanodiene has anti-inflammatory and antioxidant activities, it is active against gram-positive bacteria and Candida albicans.
    • $52
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  • Solamargine
    T403420311-51-7
    Solamargine (δ-Solanigrine) is a major steroidal alkaloid glycoside extracted from a traditional Chinese medicine herb, Solanum nigrum L. (SNL); has been shown to inhibit growth and induce apoptosis of various cancer cells.
    • $54
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