Catalog No.
Product Name
Application
Product Information
Citations
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P-gp modulator
LY335979 (Zosuquidar trihydrochloride) is a potent highly selective P-gp inhibitor.- Leo Shen, .et al. , Sci Rep, 2021, Sep 16;11(1):18516 PMID: 34531456
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MDR1/P-gp Inhibitor
PSC-833 is a kind of P-glycoprotein (P-gp) modulator that inhibits P-gp-mediated multidrug-resistance (MDR).- Somin Lee, .et al. , Methods Mol Biol, 2022, 2492:251-263 PMID: 35733049
- Somin Lee, .et al. , Biotechnol Bioeng, 2019, 10 November
- Somin Lee, .et al. , bioRxiv, 2018, Nov. 18
- Watanabe N, .et al. , Biopharm Drug Dispos, 2018, Jan;39(1):30-37 PMID: 29055041
- Higashi H, .et al. , Biol Pharm Bull, 2017, 40(8):1314-1319 PMID: 28769012
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P-gp inhibitor
Tariquidar (XR9576) is a P-glycoprotein drug efflux pump inhibitor.- Maria Joao Moreno, .et al. , Pharmaceutics, 2023, Jan 3;15(1):174 PMID: 36678803
- Yuko Sasaki, .et al. , Biol Pharm Bull, 2022, 45(9):1246-1253 PMID: 36047192
- Sugisawa N, .et al. , Mol Pharm, 2018, Sep 4;15(9):4021-4030 PMID: 30052463
- Samy A. F. Morad, .et al. , Biochem Pharmacol, 2017, Apr 15; 130: 21-33 PMID: 28189725
- Debora Petroni, .et al. , Mol Imaging Biol, 2016, Dec;18(6):916-923 PMID: 27234445
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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 & BCRP inhibitor
Elacridaris a prototypical BCRP inhibitor which inhibits the Bcrp1-mediated transport.- Leo Shen, .et al. , Sci Rep, 2021, Sep 16;11(1):18516 PMID: 34531456
- 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
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-gp inhibitor
Elacridar hydrochloride is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules. -
P-gp inhibitor
Zosuquidar is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. -
Pgp modulator
P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR). -
P-glycoprotein inhibitor
Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein. -
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. -
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. -
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. -
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. -
P-gp Inhibitor
RMS3 is a tetrandrine analogue that functions as a potent inhibitor of P-glycoprotein (P-gp). This compound exhibits significant antiproliferative and cytotoxic effects on various cancer cell lines. Notably, RMS3 induces PARP cleavage, which is indicative of cells undergoing apoptosis. Its strong anticancer properties make RMS3 a valuable tool for cancer research and therapeutic studies. -
P-gp Inhibitor
RMS5 is a potent P-glycoprotein (P-gp) inhibitor, derived from a tetrandrine analogue. It exhibits significant antiproliferative and cytotoxic effects on cancer cells, contributing to its strong anticancer properties. Additionally, RMS5 has been observed to reduce the expression of anti-apoptotic Bcl-2 family proteins Bcl-XL and Mcl-1 while inducing PARP cleavage, a hallmark of apoptosis. This compound is valuable for research applications focusing on cancer therapeutics and the modulation of multidrug resistance. -
P-gp Inhibitor
(R)-OY-101 is an orally active and selective inhibitor of P-glycoprotein (P-gp). This compound enhances the sensitivity of tumors to anticancer agents by reversing drug resistance and promoting apoptosis. It has valuable applications in cancer research, particularly in studies focused on overcoming multidrug resistance and improving therapeutic efficacy. -
P-Glycoprotein Inhibitor
(R)-Verapamil hydrochloride is an orally active P-Glycoprotein inhibitor that effectively blocks MRP1-mediated transport. This compound induces apoptosis and inhibits L-type calcium channels, including BZPcc, DHPcc, and PLLcc. Additionally, (R)-Verapamil hydrochloride demonstrates potential anti-septic shock and anti-diabetic effects, making it suitable for a range of research applications in cellular signaling and drug transport studies. -
P-glycoprotein Inhibitor
P-gp inhibitor 22 is a potent inhibitor of P-glycoprotein (P-gp), effectively blocking its efflux function. This compound has been shown to induce apoptosis and promote the accumulation of MCF-7/ADR cells in the S phase of the cell cycle. Its ability to inhibit P-gp makes it relevant in studies focused on multidrug resistance and cancer therapeutics. -
Mycotoxin
Roquefortine C is a mycotoxin derived from Penicillium species, exhibiting multiple biological activities. As an agonist of P-glycoprotein (P-gp), it inhibits cytochrome P450 enzymes, specifically P450 3A and P450 1A. This compound demonstrates antimicrobial effects against Gram-positive bacteria and possesses neurotoxic properties, along with potential antitumor activity. Roquefortine C serves as a valuable tool in research exploring microbial interactions and pharmacological mechanisms. -
P-gp Inhibitor
Milbemycin A4 is a potent inhibitor of P-glycoprotein (P-gp), effectively reversing multidrug resistance in tumor cells. As a member of the macrolide antibiotic family, Milbemycin A4 displays significant insecticidal and acaricidal properties. This compound is valuable for research focused on overcoming chemotherapy resistance and studying P-gp-related mechanisms in cellular drug transport. -
Glycoside
Bacopasaponin C is a natural glycoside with demonstrated inhibitory effects on P-glycoprotein (P-gp) ATPase activity, showing an IC50 of 57.83 μg/mL in the presence of Verapamil. Isolated from Bacopa monniera, Bacopasaponin C exhibits notable antitumor properties against sarcomas and displays antiparasitic activity against Leishmania donovani. This compound is of interest for research into cancer therapeutics and antiparasitic drug development. -
HCV Inhibitor
Vedroprevir is a potent inhibitor of the HCV NS3/4A protease, demonstrating an IC50 of 3.2 nM. In addition to its antiviral activity, Vedroprevir also inhibits the breast cancer resistant protein (BCRP) with an IC50 of 1.4 μM, as well as P-glycoprotein (P-gp), MRP1, and MRP2 with IC50 values of 34 μM, 14.9 μM, and 12 μM, respectively. These characteristics make Vedroprevir valuable for research in hepatitis C and multidrug resistance cancer studies. Its favorable pharmacokinetic profile has been observed in preclinical models, including rats and dogs. -
Stable Isotope
Atazanavir-d5 is a deuterium-labeled derivative of Atazanavir, a highly selective inhibitor of HIV-1 protease. This compound serves as a substrate and inhibitor of the cytochrome P450 enzyme CYP3A4, as well as an inhibitor and inducer of P-glycoprotein (P-gp). Additionally, Atazanavir exhibits activity against SARS-CoV 3CLpro with an IC50 of 3.49 μM, making it valuable for research into HIV and coronavirus-related mechanisms. -
Stable Isotope
Atazanavir-d6 is a deuterium-labeled form of Atazanavir, a selective inhibitor of HIV-1 protease. Recognized for its capability as a CYP3A4 substrate and inhibitor, it also exerts dual effects as both an inhibitor and inducer of P-glycoprotein (P-gp). In addition, Atazanavir demonstrates antiviral activity by inhibiting the SARS-CoV 3CLpro with an IC50 of 3.49 μM, making it a valuable tool for research in HIV and coronavirus-related studies. -
P-glycoprotein Inhibits
NIK250 is a potent inhibitor of P-glycoprotein, a key mediator of multidrug resistance (MDR) in cancer cells. By disrupting the efflux activity of P-glycoprotein, NIK250 enhances the cellular retention of chemotherapeutic agents, thereby increasing their efficacy. This compound can be utilized in research aimed at overcoming drug resistance in cancer therapies and elucidating the mechanisms of MDR in various pathological contexts. -
CCR5 Antagonist
AZD-5672 is a potent and selective antagonist of the CCR5 receptor, exhibiting an IC50 of 0.32 nM. This compound demonstrates moderate activity against the hERG ion channel with a binding IC50 of 7.3 μM and acts as a substrate for human P-glycoprotein, inhibiting P-gp-mediated digoxin transport with an IC50 of 32 μM. AZD-5672 is an effective tool for investigating the role of CCR5 in inflammatory diseases, including rheumatoid arthritis. -
Stable Isotope
(Rac)-Talinolol-d5 is a stable isotope of Talinolol, a long-acting, cardioselective β1-adrenergic receptor blocker. This compound demonstrates significant cardioprotective and antihypertensive properties. Additionally, Talinolol serves as a valuable probe substrate for investigating P-glycoprotein (P-gp) activity in pharmacokinetic studies.
