P-gp

YS-370 is a potent and selective inhibitor of P-glycoprotein (P-gp) that exhibits oral bioavailability. It facilitates the P-gp ATPase activity while demonstrating moderate inhibition of CYP3A4. This compound effectively reverses multidrug resistance (MDR) in cell lines such as SW620/AD300 and HEK293T-ABCB1, particularly in conjunction with paclitaxel, leading to enhanced antitumor efficacy. YS-370 is valuable for research focused on overcoming drug resistance in cancer therapy.

Tariquidar dihydrochloride is a potent and selective inhibitor of P-glycoprotein (P-gp), exhibiting a high affinity with a Kd of 5.1 nM. This compound significantly enhances the bioavailability of co-administered drugs by inhibiting P-gp-mediated drug efflux. It is widely used in research to investigate the roles of P-gp in pharmacokinetics, drug-drug interactions, and multidrug resistance in cancer therapies.

OY-101 is a potent and orally active inhibitor of P-glycoprotein (P-gp). This compound demonstrates the ability to sensitize drug-resistant tumors, effectively reversing multidrug resistance in cancer cells. With improvements in water solubility, cytotoxicity, and reversal activity compared to Tetrandrine, OY-101 represents a valuable tool in cancer research and development of therapeutic strategies for overcoming drug resistance.

Tariquidar dimesylate is a potent ABCB1 inhibitor targeting P-glycoprotein (P-gp). By binding to P-glycoprotein, it effectively increases the concentration of therapeutic agents within the brain, inhibiting their active transport out of cerebral tissue. This compound is invaluable for investigating blood-brain barrier permeability and understanding mechanisms of multidrug resistance in cancer and neurological research.

Encequidar mesylate hydrochloride is a selective inhibitor of P-glycoprotein (MDR1), which plays a crucial role in drug resistance. This compound enhances the anti-tumor efficacy of Paclitaxel in various mouse tumor models, making it valuable for cancer research. Encequidar mesylate hydrochloride is primarily utilized to study drug interactions and to evaluate therapeutic strategies aimed at overcoming multidrug resistance in cancer treatment.

P-gp Inhibitor 17 is a selective inhibitor of P-glycoprotein (P-gp), directly targeting its transmembrane domain to modulate its activity. This compound is particularly useful for investigating P-gp-mediated multidrug resistance in cancer cells, providing insights into therapeutic strategies for overcoming resistance in oncology research. Its role in enhancing drug bioavailability and efficacy makes it a valuable tool for studying tumor cell behavior and treatment response.

P-gp Inhibitor 13 specifically targets P-glycoprotein (P-gp), functioning as an inhibitor to reverse P-glycoprotein-mediated drug resistance. This compound has demonstrated effectiveness in overcoming paclitaxel resistance in A2780/T cells, making it a valuable tool in cancer research. Its applications extend to the study of advanced acute myeloid leukemia, providing insights into therapeutic strategies for overcoming resistance in this malignancy.

Neostenine is a stenine-type Stemona alkaloid that acts as a substrate for P-glycoprotein. It exhibits notable antitussive activity and demonstrates high absorptive permeability in Caco-2 monolayer models. Additionally, Neostenine shows oral bioactivity, making it relevant for research applications involving intestinal absorption and therapeutic potential in cough-related conditions.

P-gp inhibitor 14 is a potent inhibitor of P-glycoprotein (P-gp), effectively reversing P-gp-mediated multidrug resistance with an EC50 value of 48.74 nM. This compound demonstrates a weak inhibitory effect on CYP3A4 activity, making it a useful agent for enhancing the efficacy of chemotherapeutics in resistant cancer cells. Its primary applications include studies on drug transport mechanisms and overcoming resistance in multidrug-resistant tumors.

Clausarin is a selective P-glycoprotein (P-gp) inhibitor that effectively obstructs the P-gp-mediated efflux of chemotherapeutic agents. It demonstrates significant inhibition of daunorubicin efflux in K562/R7 human leukemia cells that overexpress P-gp, with Cyclosporin A serving as a positive control. Isolated from the roots of Citrus sinensis (sweet orange), Clausarin is a valuable reagent for research focused on overcoming multidrug resistance (MDR) in cancer therapies.

P-gp/BCRP-IN-1 is a potent inhibitor targeting P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP). This compound is designed to reverse drug resistance by inhibiting the efflux activities of these pivotal transporters. P-gp/BCRP-IN-1 enhances the oral bioavailability of chemotherapeutic agents, such as Paclitaxel (PTX), making it a valuable tool in cancer research and therapeutic development. Its efficacy and oral activity suggest a promising utility in overcoming drug resistance in various cancer models.

Verapamil-d3 hydrochloride is a deuterium-labeled derivative of the calcium channel blocker, verapamil hydrochloride. It serves as a potent inhibitor of P-glycoprotein (P-gp) and CYP3A4, facilitating detailed pharmacological studies. This stable isotope is primarily utilized in research related to hypertension, cardiac arrhythmias, and angina, providing insight into drug metabolism and transport mechanisms in various biological systems.

Norverapamil-d7 is a deuterium-labeled derivative of Norverapamil, which selectively targets L-type calcium channels. As an N-demethylated metabolite of Verapamil, it functions as an effective calcium channel blocker and inhibits P-glycoprotein (P-gp) activity. This reagent is suitable for research applications related to cardiovascular physiology, drug absorption studies, and pharmacokinetics involving P-gp transport mechanisms.

Verapamil-d7 is a deuterium-labeled derivative of Verapamil, a calcium channel blocker and a potent inhibitor of the P-glycoprotein (P-gp) transporter. This isotope-labeled compound is utilized in pharmacokinetic studies and metabolic research, providing insights into drug interactions and transport mechanisms. Its applications extend to investigating conditions such as hypertension, cardiac arrhythmias, and angina, making it a valuable tool in cardiovascular research.

Verapamil-d3 is a deuterium-labeled form of Verapamil, a calcium channel blocker that serves as a potent, orally active first-generation inhibitor of P-glycoprotein (P-gp) and CYP3A4. This stable isotope variant is utilized in pharmacokinetic studies and metabolic research, aiding in the investigation of cardiovascular diseases such as hypertension, arrhythmias, and angina. Verapamil-d3's unique properties make it an invaluable tool for studying drug interactions and bioavailability in various biological systems.

Norverapamil-d6 hydrochloride is a stable isotope-labeled version of Norverapamil, an N-demethylated metabolite of Verapamil. This compound acts as a blocker of L-type calcium channels and inhibits P-glycoprotein (P-gp) function. It is primarily utilized in pharmacokinetic studies, drug metabolism research, and for tracing metabolic pathways in biological systems.

Norverapamil, an N-demethylated metabolite of Verapamil, acts as an L-type calcium channel blocker and inhibits P-glycoprotein (P-gp) function. This compound is primarily utilized in research to study calcium ion dynamics and assess the role of P-gp in drug transport and resistance mechanisms. Its ability to modulate calcium influx makes it valuable for applications in cardiovascular and neuropharmacological investigations.

Verapamil-d6 hydrochloride is a deuterated derivative of Verapamil, a selective calcium channel blocker. It exhibits potent inhibition of P-glycoprotein (P-gp) and CYP3A4, making it valuable in cardiovascular research, particularly for conditions such as hypertension, arrhythmias, and angina. This isotopically labeled compound aids in pharmacokinetic studies and offers insights into drug metabolism and transport mechanisms.

Atazanavir-d9 is a deuterated analog of Atazanavir, a highly selective HIV-1 protease inhibitor. This compound targets the HIV-1 protease enzyme, facilitating the treatment of HIV infections with its ability to inhibit viral replication. Additionally, Atazanavir acts as both a substrate and inhibitor of CYP3A4, as well as an inducer of P-glycoprotein (P-gp). Furthermore, Atazanavir possesses inhibitory activity against SARS-CoV 3CLpro, with an IC50 of 3.49 μM, making it relevant for research in antiviral therapies.

Danofloxacin mesylate is a fluoroquinolone antimicrobial agent that exerts its bactericidal activity primarily through the inhibition of bacterial DNA gyrase, a crucial enzyme for DNA replication. This compound displays a broad spectrum of effectiveness against various bacterial strains. Additionally, Danofloxacin mesylate is recognized as a substrate for ATP-dependent efflux transporters, including P-glycoprotein (P-gp) and multidrug resistance protein 2 (MRP2), making it relevant for studies on drug resistance mechanisms in bacteria. This agent is primarily utilized in veterinary medicine and research on antibiotic efficacy and resistance.