Catalog No.
Product Name
Application
Product Information
Citations
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H+/K+ ATPase Inhibitor
SK&F 97574 hydrochloride is a reversible inhibitor of the H+/K+ ATPase enzyme, demonstrating significant efficacy in reducing gastric acid secretion. Its primary biological activity supports the healing of acid-related upper gastrointestinal ulcers, making it valuable for research into gastrointestinal disorders and acid secretion regulation. This reagent is essential for studies focused on the pharmacological modulation of gastric acid dynamics. -
Na+/K+ ATPase Inhibitor
Rs-029 is a selective inhibitor of Na+/K+ ATPase and an activator of Mg2+ ATPase. It effectively reduces ATP levels in red blood cells, which can be critical for studying energy metabolism and ion balance in cellular systems. This compound is valuable for research applications focused on membrane transport mechanisms and investigating cellular responses to altered energy states. -
Na+/K+ ATPase Control
Ro18-5362 is a proagent of Ro18-5364 that targets Na+/K+ ATPase. While it exhibits limited activity on (H++K+)-ATPase at concentrations up to 0.1 mM, it serves as a useful tool for understanding ATPase mechanisms and probing related physiological processes. This compound is valuable in research focusing on ion transport regulation and cellular homeostasis. -
KATP Opener
Iptakalim hydrochloride is a selective ATP-sensitive potassium channel (KATP) opener that exhibits significant lipophilicity. In addition to its primary mechanism, it also acts as an antagonist of α4β2-containing nicotinic acetylcholine receptors (nAChRs). This dual activity positions Iptakalim hydrochloride as a valuable tool for research in cardiovascular physiology and neuropharmacology, providing insights into potassium channel regulation and cholinergic signaling. -
KCC2 Antagonist
ML077 is a selective antagonist of the potassium-chloride co-transporter 2 (KCC2), with an IC50 of 537 nM for KCC2, while exhibiting minimal activity on KCC1 (IC50 > 50 μM). By inhibiting the chloride ion excretion function of KCC2, ML077 increases intracellular chloride concentrations, resulting in enhanced depolarization through chloride channels. This compound has demonstrated the ability to promote glucose-stimulated insulin secretion (GSIS) independent of KATP channels and is valuable for studying the physiological processes related to pain, epilepsy, and insulin secretion. -
Adenosine reuptake inhibitor
Dilazep dihydrochloride is an adenosine uptake inhibitor that promotes vasodilation in cerebral and coronary circulation by enhancing the effects of adenosine. This compound exhibits protective properties against ischemic damage, reduces platelet aggregation, and interferes with the membrane transport of nucleosides. It is valuable in research applications focused on cardiovascular physiology and neurological protection. -
human ENT4 inhibitor
hENT4-IN-1 is a selective inhibitor of the human equilibrative nucleoside transporter 4 (ENT4), exhibiting an IC50 of 74.4 nM. This compound is crucial for investigating the biological roles of ENT4 in cellular nucleoside transport and metabolism. Its application extends to studies evaluating the impact of ENT4 inhibition on various physiological and pathological processes, making it a valuable tool for research in cancer biology and therapeutic development. -
ENT2 Inhibitor
FPMINT is a potent, irreversible, and non-competitive inhibitor of Equilibrative Nucleoside Transporters (ENTs), with a higher selectivity for ENT2 compared to ENT1. By effectively blocking ENT2, FPMINT significantly impacts uridine uptake, making it a valuable tool in studies related to nucleoside transport mechanisms. Its application in research can aid in elucidating the physiological roles of ENT2 in various biological processes. -
Adenosine reuptake inhibitor
Dilazep is an adenosine uptake inhibitor that enhances the effects of adenosine, leading to cerebral and coronary vasodilation. This compound not only reduces ischemic damage but also inhibits platelet aggregation and the membrane transport of nucleosides. Dilazep is useful in research applications focused on cardiovascular physiology and neuroprotection. -
hCNT1 Inhibitor
dMeThPmR is a selective inhibitor of the human nucleoside transporter 1 (hCNT1), exhibiting a potent inhibitory constant (Ki) in the range of 0.3-0.98 μM. While dMeThPmR shows minimal inhibition of hCNT2 (IC50 = 133 μM) and hCNT3 (Ki = 32.7 μM), it effectively protects cells from the cytotoxic effects of nucleoside drugs. This compound is valuable for research on cancer and related therapies, providing insights into nucleoside transport mechanisms and drug interactions. -
hCNT1 Inhibitor
MeThPmR is a potent and selective inhibitor of the human nucleoside transporter 1 (hCNT1) with a Ki ranging from 0.16 to 0.69 μM. It exhibits minimal inhibitory activity on hCNT2 (IC50 = 360 μM) and hCNT3 (Ki = 4.7 μM). MeThPmR has been demonstrated to provide protection against the cytotoxic effects of nucleoside drugs, making it a valuable tool for cancer research applications. -
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. -
Calcium Channel Antagonist
CP-060 is a potent calcium channel antagonist that effectively inhibits calcium overload in cells. This compound also exhibits notable antioxidant properties and offers cardioprotective effects. CP-060 is valuable for research applications focused on cardiovascular diseases and cellular stress responses. -
Calcium Channel Inhibitor
McN5691 is a voltage-sensitive calcium channel inhibitor that selectively blocks calcium influx through L-type calcium channels. This action leads to reduced calcium-dependent cellular events, making it a valuable tool for investigating calcium signaling pathways. McN5691 is particularly useful in research focused on cardiovascular physiology and the modulation of muscle contraction mechanisms. -
Calcium Channel Chemical
α2δ ligand 1 selectively interacts with the α2δ-1 subunit of voltage-gated calcium channels. This compound is known to modulate calcium influx, which plays a crucial role in neuronal excitability and synaptic transmission. It is utilized in research applications focused on pain management, neurological disorders, and the exploration of synaptic plasticity. -
Calcium Channel Antagonist
Dopropidil is a calcium channel antagonist that modulates intracellular calcium levels. It exhibits anti-anginal properties and demonstrates significant anti-ischemic effects in various predictive animal models. This compound is valuable for research in cardiovascular pharmacology, particularly in the study of angina and ischemic heart disorders. -
Calcium Channel Antagonist
Darodipine is a potent calcium channel antagonist that selectively inhibits L-type calcium channels. This compound demonstrates significant biological activity by decreasing intracellular calcium levels, which can effectively reduce vascular smooth muscle contraction. Darodipine is primarily utilized in research applications focused on cardiovascular physiology, hypertension studies, and the exploration of calcium signaling pathways. -
CFTR Activator
SRI-41315 is a CFTR (cystic fibrosis transmembrane conductance regulator) activator that induces a prolonged pause at stop codons and suppresses premature termination codons (PTCs) associated with cystic fibrosis. This compound restores CFTR expression and function in both immortalized and primary human bronchial epithelial cells by decreasing the levels of the termination factor eRF1. Additionally, SRI-41315 enhances aminoglycoside-mediated readthrough, resulting in synergistic increases in CFTR activity, making it a valuable tool for research into cystic fibrosis and related therapies. -
CFTR Modulator
Vanzacaftor is a novel CFTR modulator that acts as a corrector of the cystic fibrosis transmembrane conductance regulator (CFTR) protein. It enhances the proper processing and trafficking of CFTR, thereby promoting increased chloride ion transport in combination with Tezacaftor and Deutivacaftor. This combination has shown efficacy in improving lung function and alleviating respiratory symptoms in cystic fibrosis patients, making it a valuable tool for research aimed at understanding and treating cystic fibrosis-related conditions. -
CFTR Modulator
Ivacaftor-d9 is a potent CFTR modulator that enhances CFTR function, demonstrating an EC50 value of 255 nM for potentiation in G551D/F508del human bronchial epithelial cells. As a deuterated analog of Ivacaftor, it exhibits improved stability and pharmacokinetic properties, making it a valuable tool for cystic fibrosis research. Ivacaftor-d9 is suitable for studies aimed at understanding CFTR modulation and its implications in therapeutic development for cystic fibrosis. -
CFTR Modulator
NJH-2-057 is a CFTR modulator that functions as an EN523 OTUB1 recruiter. It is designed to enhance the activity of the ΔF508-CFTR mutant protein, which is associated with cystic fibrosis. This compound has potential applications in studying CFTR modulation and offers insights into therapeutic strategies for cystic fibrosis treatment. -
CFTR Regulator
(R)-Vanzacaftor is a selective regulator of the cystic fibrosis transmembrane conductance regulator (CFTR) protein. It enhances CFTR activity, which plays a crucial role in chloride ion transport across epithelial cell membranes. This compound is primarily utilized in research applications aimed at understanding and treating cystic fibrosis, particularly in studies focusing on CFTR modulation and function. -
CFTR Potentiator
Icenticaftor is an orally active potentiator of the cystic fibrosis transmembrane conductance regulator (CFTR) channel, demonstrating EC50 values of 79 nM and 497 nM for the F508del and G551D CFTR mutations, respectively. This compound is valuable for research focused on chronic obstructive pulmonary disease (COPD) and cystic fibrosis, facilitating the study of disease mechanisms and potential therapeutic strategies. -
CFTR Corrector
IDOR-4 is a type IV CFTR corrector that enhances the trafficking of the F508del-CFTR mutant to the cell surface. This compound is crucial for restoring functional chloride ion transport in cystic fibrosis research and can be utilized to study the dynamics of CFTR correction mechanisms in cellular models. Its application may contribute to the development of therapeutic strategies for patients with cystic fibrosis caused by the F508del mutation. -
CFTR Corrector
Galicaftor is a potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector. It plays a crucial role in restoring the function of the CFTR protein, which is often impaired in cystic fibrosis patients. This compound is primarily utilized in research focusing on cystic fibrosis therapies and the modulation of ion transport involved in this condition. -
CFTR Modulator
Posenacaftor sodium is a modulator of the cystic fibrosis transmembrane conductance regulator (CFTR) protein, facilitating its proper folding and trafficking. This compound is predominantly utilized in research on cystic fibrosis (CF), aiming to enhance CFTR function and investigate potential therapeutic approaches for this genetic disorder. Its role in correcting defects in CFTR provides valuable insights into the disease mechanism and efficacy of treatment strategies. -
CFTR Activator
CFTR activator 1 is a potent and selective modulator of the cystic fibrosis transmembrane conductance regulator (CFTR) channel, exhibiting an EC50 of 23 nM. This compound effectively enhances CFTR function and is applicable in research related to dry eye disease treatment. Its ability to promote chloride ion transport makes it a valuable tool for investigating therapeutic strategies in CFTR-related pathologies. -
CFTR Corrector
Bamocaftor is a CFTR corrector that specifically targets the cystic fibrosis transmembrane conductance regulator (CFTR) protein, aiming to restore function to the F508del-CFTR variant. This compound is instrumental in cystic fibrosis research, particularly when used in conjunction with Tezacaftor and Ivacaftor, to enhance CFTR functionality and evaluate therapeutic strategies for cystic fibrosis management. -
CFTR Activator
CFTR Corrector 6 is a potent activator of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR). It is specifically designed for research into cystic fibrosis and other disorders associated with CFTR dysfunction. This compound enhances CFTR protein function, making it a valuable tool for investigating therapeutic strategies and understanding the underlying mechanisms of CFTR-related diseases. -
CFTR Modulator
(R)-Elexacaftor is an enantiomeric modulator of the cystic fibrosis transmembrane conductance regulator (CFTR), specifically targeting the F508del mutation. With an EC50 value of 0.29 µM, it exhibits potent biological activity in restoring CFTR function. This compound is essential for research focused on cystic fibrosis therapies and drug discovery aimed at improving CFTR activity in affected individuals. -
CFTR
VRT-325 is a small molecule designed to target the cystic fibrosis transmembrane conductance regulator (CFTR), specifically addressing the ΔF508 mutation associated with cystic fibrosis. This compound promotes the efflux of ΔF508-CFTR from the endoplasmic reticulum, thereby restoring chloride transport in epithelial cells derived from CF patients. VRT-325 is valuable for research into therapeutic strategies aimed at correcting CFTR function and enhancing epithelial ion transport in cystic fibrosis. -
CFTR Corrector
CFTR Corrector 4 is an (R,R)-form enantiomer that acts as a potent corrector of the cystic fibrosis transmembrane conductance regulator (CFTR). This compound enhances the expression of CFTR at the cellular surface, making it a promising candidate for therapeutic applications in cystic fibrosis research. Its ability to modulate CFTR levels may contribute to correcting defective chloride ion transport associated with the disease. -
CFTR Corrector
CFTR Corrector 12 (compound 17C) is a bithiazole derivative that acts as a CFTR corrector by promoting the proper folding of defective CFTR mutants. This compound enhances chloride transport across the plasma membrane, making it beneficial for studies involving cystic fibrosis and related disorders. Additionally, CFTR Corrector 12 has been shown to recover α-sarcoglycan (α-SG) levels in mutant cells, indicating its potential in therapeutic approaches targeting CFTR-related pathologies.
