p-glycoprotein

Valspodar (PSC 833) is a small-molecule inhibitor and a P-glycoprotein (P-gp) inhibitor with high selectivity and chemosensitizing properties. This compound can effectively reverse P-gp-mediated multidrug resistance (MDR) and is used in experimental research on drug-resistant tumors such as advanced epithelial ovarian cancer.

Elacridar (GG918) is a potent inhibitor of P-glycoprotein and BCRP.

Celiprolol hydrochloride (Selectrol) is a cardioselective beta-1 adrenergic antagonist that has intrinsic sympathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION.

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.

PGP-4008 is a selective and potent P-glycoprotein (Pgp) inhibitor that inhibits tumor growth by co-administration with Doxorubicin.

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.

Atazanavir sulfate (BMS-232632 sulfate) is an azapeptide and HIV-protease inhibitor used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents.

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

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

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

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

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.

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.

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

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

Pristinamycin IA (Mikamycin B) is a cyclo-peptidic macrolactone antibiotic and a substrate for the P-glycoprotein.

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

Larotaxel (XRP9881) is a taxane analogue with anticancer activity that promotes tubulin assembly and stabilizes microtubules, inducing apoptosis. It crosses the blood-brain barrier and has a higher affinity for Docetaxel than P-glycoprotein 1, making it useful for studying breast and bladder cancer.

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.

NSC23925 is a selective and effective inhibitor of P-glycoprotein (Pgp).