Catalog No.
Product Name
Application
Product Information
Citations
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Anti-parkinson Agent
Budipine is an anti-Parkinson agent that acts primarily as an N-methyl-D-aspartate (NMDA) antagonist while also influencing dopaminergic activity. It enhances dopamine release and inhibits monoamine oxidase type B (MAO-B), contributing to its therapeutic effects. As a substrate of P-glycoprotein (P-gp), Budipine's uptake into the brain is mediated by this transport mechanism. This compound is valuable for research into central nervous system disorders, including Parkinson's disease. -
Anti-parkinson Agent
Budipine hydrochloride functions primarily as an anti-Parkinson agent, targeting the central nervous system. It acts as a substrate of P-glycoprotein (P-gp), facilitating its uptake into the brain. Additionally, Budipine hydrochloride serves as an NMDA antagonist and exhibits indirect dopaminergic effects by enhancing dopamine release and inhibiting monoamine oxidase type B (MAO-B). This compound is valuable for research focused on CNS disorders, particularly Parkinson's disease. -
P-glycoprotein Inhibitor
NSC 23925B is a potent inhibitor of P-glycoprotein (P-gp), which plays a critical role in multidrug resistance in cancer cells. This compound effectively reverses P-glycoprotein-mediated resistance and shows moderate inhibitory activity against CYP2B6 and CYP2D6 with IC50 values of 8.589 μM and 1.407 μM, respectively. NSC 23925B is valuable for research focused on overcoming multidrug resistance in cancer therapy and studying P-glycoprotein's role in drug disposition. -
P-glycoprotein Inhibitor
Dofequidar fumarate is a potent P-glycoprotein (P-gp) inhibitor that also targets multidrug resistance-associated protein-1 (MDR-1). This quinoline compound effectively reverses multidrug resistance in tumor cells by competitively inhibiting ABCB1/P-gp and ABCC1/MRP-1. By blocking the efflux of chemotherapeutic agents, Dofequidar fumarate increases drug concentration within cancer cells, thereby enhancing the efficacy of chemotherapy. Its application is particularly relevant in cancer research focused on overcoming drug resistance. -
P-glycoprotein Inhibitor
Reversin 121 is a potent P-glycoprotein inhibitor that enhances the ATPase activity of the MDR1 gene product. By reversing P-glycoprotein-mediated multidrug resistance, it plays a critical role in overcoming drug resistance in cancer therapies. This compound is valuable for research applications focused on enhancing the efficacy of anticancer drugs in resistant cancer cell lines. -
P-gp Inhibitor/Potassium Channel Activator
GPV0057 is a selective and potent inhibitor of P-glycoprotein (P-gp) and a specific activator of the potassium channel Kir2.1. By competitively binding to the substrate-binding site of P-gp, GPV0057 inhibits ATP-dependent drug efflux, effectively reversing multidrug resistance in tumor cells. Additionally, it stabilizes the open state of Kir2.1, facilitating potassium ion influx. This compound holds potential for research in tumors characterized by high P-gp expression and in conditions such as heart failure and Andersen-Tawil Syndrome that involve Kir2.1 deficiency. -
P-Glycoprotein Inhibitor
Boeravinone B is a dual inhibitor of the NorA efflux pump in Staphylococcus aureus and human P-glycoprotein. This compound exhibits significant anti-biofilm activity and reduces intracellular bacterial invasion. Additionally, Boeravinone B demonstrates potential anti-aging and anti-apoptotic effects under oxidative stress conditions, making it a valuable reagent for research in microbiology and cellular aging pathways. -
P-glycoprotein Inhibitor
PGP-4008 is a selective inhibitor of P-glycoprotein (Pgp), known for its role in multidrug resistance (MDR) in cancer cells. This compound demonstrates significant antitumor activity by enhancing the efficacy of chemotherapeutic agents, particularly Doxorubicin, in murine models characterized by Pgp-mediated resistance. PGP-4008 is valuable for research into overcoming drug resistance in cancer therapy and the modulation of pharmacokinetics in oncology. -
P-glycoprotein
Hypophyllanthin is a significant lignan derived from Phyllanthus species that acts as a potent inhibitor of P-glycoprotein (P-gp). This compound exhibits strong anti-inflammatory properties and selectively inhibits P-gp activity without affecting multidrug resistance protein 2 (MRP2) activity. Its unique mechanism makes it a valuable tool for research in drug resistance and inflammation-related studies. -
P-glycoprotein Inhibitor
WS-898 is a potent P-glycoprotein inhibitor that effectively reverses paclitaxel resistance in various drug-resistant cancer cell lines, including SW620/Ad300, KB-C2, and HEK293/ABCB1, with IC50 values of 5.0, 3.67, and 3.68 nM, respectively. This compound serves as a valuable tool for research focused on overcoming multidrug resistance in cancer therapeutics. Its ability to inhibit ABCB1 transport activity makes it an important reagent for studies aimed at enhancing the efficacy of chemotherapeutic agents. -
P-gp Inhibitor
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. -
P-gp Inhibitor
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. -
P-gp Inhibitor
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. -
ABCB1 Inhibitor
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. -
P-glycoprotein Inhibitor
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
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
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. -
P-glycoprotein Substrate
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
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. -
P-gp Inhibitor
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. -
Vitamin E
γ-Tocotrienol is an active form of vitamin E that primarily targets the signaling pathway of NF-κB and P-glycoprotein (P-gp). It demonstrates significant biological activity by reversing multidrug resistance (MDR) in breast cancer cells, enhancing the efficacy of chemotherapeutic agents. Additionally, γ-tocotrienol serves as a radioprotective agent, effectively mitigating bone marrow radiation damage associated with targeted radionuclide treatments. Research applications include cancer therapy and protection against radiation-induced injury. -
Calcium Channel Blocker
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. -
Stable Isotope
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. -
Antimicrobial Agent
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. -
Mycotoxin
Deoxynivalenol, an orally active mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors. -
NF-kβ Agonist
Berubicin hydrochloride is an NF-kB agonist and a Doxorubicin analog with the ability to cross the blood-brain barrier. It inhibits P-glycoprotein (P-gp) and multidrug resistance-associated protein 1 (MRP1), thereby reducing efflux in glioblastoma multiforme (GBM) and exerting cytotoxic effects on leukemia cells. Additionally, Berubicin hydrochloride induces apoptosis in neuroblastoma cells, making it a valuable reagent for studying tumors of the nervous system. -
P-glycoprotein Inhibitor
1-Monopalmitin, also known as Glyceryl palmitate, functions as an inhibitor of P-glycoprotein (P-gp) and modulates the PI3K/Akt signaling pathway. It has been shown to induce G2/M phase arrest and promote caspase-dependent apoptosis in cancer cells, while also downregulating inhibitor of apoptosis proteins (IAPs). Additionally, 1-Monopalmitin enhances drug accumulation in intestinal Caco-2 cells by inhibiting P-gp activity and has demonstrated the ability to induce protective autophagy and apoptosis in lung cancer cells with an IC50 of 50-58 μg/mL, exhibiting low toxicity towards normal cells. -
HIV-1 protease/PTP1B inhibitor
Isosinensetin is a bioactive flavonoid compound with diverse pharmacological properties. It acts as a dual inhibitor of HIV-1 protease and protein tyrosine phosphatase 1B (PTP1B), with an IC₅₀ of 2.61 µM and a Kᵢ of 0.92 µM for PTP1B, indicating its potential in antiviral and metabolic disease research. Additionally, isosinensetin inhibits P-glycoprotein (P-gp) activity in MDR1-MDCKII cells, suggesting its utility in overcoming multidrug resistance. Isosinensetin exhibits multiple therapeutic effects, including anti-tumor, anti-viral, anti-inflammatory, and antioxidant activities. These properties support its application in the research of various conditions such as cancer, chronic inflammation, osteoporosis, diabetes, and infectious diseases. -
CB1/P-gp Inhibitor
Voacamine is an indole alkaloid that acts as an antagonist of the cannabinoid receptor 1 (CB1) and also functions as a P-glycoprotein (P-gp) inhibitor. This compound enhances the efficacy of Doxorubicin by modulating P-gp activity, promoting apoptosis-independent autophagic cell death in human osteosarcoma cells. Additionally, Voacamine activates mitochondrial-associated apoptosis signaling pathways while inhibiting the PI3K/Akt/mTOR pathway, thus suppressing breast cancer progression. Moreover, it demonstrates oncogenic activity against colorectal cancer by inhibiting epidermal growth factor receptor (EGFR). -
Mdr1p Inhibitor
P-gp-IN-34 is a potent inhibitor of the Mdr1p pump, targeting multidrug resistance in various biological contexts. It has demonstrated efficacy in inhibiting the yeast-to-hyphal transition in Candida albicans, a critical process in its pathogenicity. This compound is suitable for research applications focused on candidiasis and the mechanisms of antifungal resistance. -
MDR Reversal Agent
Hydrocinchonine is a multidrug resistance (MDR) reversal agent that functions primarily by inhibiting the activity and expression of P-glycoprotein (P-gp). This inhibition plays a critical role in overcoming drug resistance in cancer treatment. Hydrocinchonine has demonstrated a synergistic apoptotic effect when combined with Paclitaxel in MES-SA/DX5 cells, making it a valuable tool for research aimed at addressing drug-resistant gynecological malignancies, such as uterine sarcoma. - Selamectin is a topical parasiticide and antihelminthic used on dogs and cats to treat and prevent infections of heartworms, fleas, ear mites, sarcoptic mange, and certain types of ticks in dogs as well as prevent heartworms, fleas, ear mites, hookworms, and roundworms in cats.
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non-ionic emulsifying agent
Polyoxyethylene stearate (POES) is a non-ionic emulsifying agent. -
P-gp inhibitor
Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor. -
P-gp inhibitor
P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance. -
P-gp inhibitor
Laniquidar is a third-generation P-gp inhibitor, which has been used in clinic trials for modulating multidrug resistance transporters. -
P-gp modulator
Biricodar dicitrate (VX-710 dicitrate) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells. -
P-glycoprotein inhibitor
Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor. -
sphingomyelin synthase inhibitor
Dofequidar, also known as MS-209, is a quinolone-derived sphingomyelin synthase inhibitor that blocks P-glycoprotein and multidrug resistance-associated protein-1, is under development by Schering for the potential treatment of multidrug resistant tumors. -
anticancer agent
Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition.
