Elacridar (GG918) (GF120918) is an effective BCRP and P-gp (MDR-1) inhibitor.

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

Glibenclamide (Glyburide) is an antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.

Trifluoperazine (trifluoroperazine) is a Dopamine D2 receptor inhibitor(IC50 : 1.2 nM), and Treatment of schizophrenia.

Atazanavir (BMS-232632)(BMS-232632) is an highly effective HIV-1 protease inhibitor.

Risperidone (R 64 766) is a selective blocker of dopamine D2 receptors and serotonin 5-HT2 receptors that act as an atypical antipsychotic agent.

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.

Polyoxyethylene stearate (POES) is an agent of non-ionic emulsifying.

1. Evodine has antinociceptive activity.

Hypophyllanthin and phyllanthin have antitumour effects against Ehrlich Ascites Carcinoma in mice.

P-gp inhibitor 1 inhibits reversing P-glycoprotein-mediated multidrug resistance with an EC50 of 57.9 nM (K562/A02 cells).

Piperine (Bioperine) , a alkaloid, has been used in trials studying the treatment of multiple myeloma and deglutition disorders.

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.

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.

1. Isosinensetin (6-Demethoxynobiletin) shows antioxidant and HIV-1 protease inhibiting activities.

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.

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).

Zosuquidar trihydrochloride (LY-335979 trihydrochloride) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.

Verapamil hydrochloride (Verapamil HCl) is a calcium channel blocker that is a class IV anti-arrhythmia agent.

Coniferyl ferulate is a strong inhibitor of glutathione S-transferase (GST) isolated from Radix Angelicae sinensis. It shows strong inhibition of human placental GST (IC50: 0.3 μM). It also reverses multidrug resistance and downregulates P-glycoprotein.

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.

Atazanavir sulfate (BMS-232632 sulfate) is an azapeptide and HIV-PROTEASE INHIBITOR that is used in the treatment of HIV INFECTIONS and AIDS in combination with other ANTI-HIV AGENTS.

Encequidar (HM30181A) is a potent and selective P-glycoprotein inhibitor.

Trifluoperazine dihydrochloride (SKF5019) is a potent dopamine D2 receptor inhibitor used as an antipsychotic and an antiemetic.

Zamicastat (BIA 5-1058) is an inhibitor of dopamine β-hydroxylase (DBH), and is also a concentration-dependent dual inhibitor of P-gp and BCRP(IC50 values of 73.8 μM and 17.0 μM, respectively).

Convallatoxin is a natural product

Voacamine (Voacanginine) is an indole alkaloid. Voacamine exhibits potent cannabinoid CB1 receptor antagonistic activity. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells.Voacanginine may have rhythmic effects.

Paris saponin VII (Dioscini) shows inhibitory effects on cell proliferation.

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.

Encequidar mesylate (HM30181A mesylate) is a competitive P-glycoprotein inhibitor.

Furanodiene has anti-inflammatory and antioxidant activities, it is active against gram-positive bacteria and Candida albicans.

Chrysosplenetin is a metabolic inhibitor of artemisinin.

Tariquidar (XR9576)(Kd=5.1 nM) is a specific and effective non-competitive inhibitor of P-glycoprotein. It can reverse drug resistance in MDR cell Lines.