Membrane Transporters-Ion Channels

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  1. Anti-malarial Agent

    Quinine dihydrochloride is an orally active alkaloid extracted from cinchona bark, primarily used as an anti-malarial agent. It functions as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel, with an IC50 of 169 μM. This compound is utilized in various research applications aimed at understanding malaria pathophysiology and exploring therapeutic strategies for its treatment.
  2. Stable Isotope

    Quinine-d3 is a deuterium-labeled derivative of quinine, primarily used as a stable isotope in chemical research. Quinine is an alkaloid isolated from the cinchona tree, known for its efficacy as an antimalarial agent and its role as a potassium channel inhibitor. It specifically inhibits wild-type mouse Slo3 (KCa5.1) channel currents induced by voltage pulses, exhibiting an IC50 of 169 μM. This reagent facilitates studies in pharmacology and biochemistry, enabling precise tracking and quantification in various applications.
  3. CV-B3 2C ATPase Inhibitor

    ATPase-IN-8 is a selective inhibitor of CV-B3 2C ATPase, exhibiting an IC50 of 1.4 μM. This compound demonstrates significant anti-enteroviral activity, particularly against coxsackievirus B3 (CV-B3) and enterovirus D68 (EV-D68). ATPase-IN-8 is suitable for research applications focusing on enteroviral infections and their molecular mechanisms.
  4. Adenosine Receptor Antagonist

    Swertisin is an adenosine A1 receptor antagonist with additional SGLT2 inhibitory activity. This compound exhibits various biological functions, including anti-diabetic and antioxidant properties, as well as the ability to inhibit hepatitis B virus (HBV). Research has demonstrated that Swertisin can enhance cognitive function and alleviate memory impairments in murine models, making it a valuable tool for studies in diabetes, neuroprotection, and viral infections.
  5. H+, K+-ATPase Inhibitor

    Esomeprazole magnesium salt is a selective inhibitor of the H+, K+-ATPase enzyme in gastric parietal cells, functioning as an effective proton pump inhibitor. This compound demonstrates significant biological activity by reducing gastric acid secretion. It is primarily utilized in research related to gastroesophageal reflux disease, exploring its therapeutic potential and mechanisms of action in acid-related disorders.
  6. Proton Pump Inhibitor

    S-Pantoprazole sodium trihydrate is a potent proton pump inhibitor that effectively reduces gastric acid secretion. It is primarily utilized in the treatment of conditions associated with excessive gastric acid production, such as gastroesophageal reflux disease (GERD) and peptic ulcers. Its mechanism of action involves the irreversible inhibition of the H+/K+ ATPase enzyme in gastric parietal cells, providing therapeutic benefits in managing acid-related disorders.
  7. Na+-V-ATPase Inhibitor

    V-161 is an orally active inhibitor of Na+-V-ATPase, exhibiting an IC50 of 144 nM. This compound effectively inhibits the growth of Enterococcus hirae and Vancomycin-resistant Enterococcus faecium (VRE) under alkaline conditions, with a minimum inhibitory concentration (MIC) of 4 µg/mL for both bacterial strains. In vivo studies demonstrate that V-161 significantly reduces VRE colonization in the mouse small intestine, making it a valuable tool for research into antimicrobial resistance and gut microbiota interactions.
  8. 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.
  9. Active Metabolite

    Desacetyl bisacodyl is the active metabolite of the laxative bisacodyl, primarily targeting epithelial chloride channels. This compound is known to stimulate chloride secretion in the colon and rectum of rat models, leading to increased mucus and electrolyte secretion. It is utilized in research applications focused on gastrointestinal physiology and the mechanisms underlying laxative action.
  10. Tricyclic Antidepressant Trimipramine Active Metabolite

    Trimipramine N-oxide is the active metabolite of the tricyclic antidepressant trimipramine, primarily targeting human monoamine transporters. It effectively inhibits noradrenaline (hNAT), serotonin (hSERT), and dopamine (hDAT) transporters, along with human organic cation transporters (hOCT1 and hOCT2), with IC50 values of 11.7, 3.59, 9.4, 9.35, and 27.4 nM, respectively. This compound is valuable for research focused on depression and anxiety, contributing to the understanding of mood disorders and the pharmacological mechanisms of antidepressants.
  11. Calcium Antagonist

    F-0401 is a calcium antagonist that exerts its effects through antagonism of the platelet-activating factor receptor (PAFR). This compound demonstrates significant potential in neurological research, particularly in studies related to stroke and related pathologies. Its ability to modulate calcium signaling pathways makes F-0401 a valuable tool for investigating therapeutic strategies in the context of neuroprotection and cerebrovascular disorders.
  12. δ2-opioid Receptor Antagonist/TRPM7 Activator

    Naltriben mesylate is a potent antagonist of the δ2-opioid receptor and an activator of TRPM7 channels. It demonstrates high affinity, with Ki values of 0.013 nM for the δ receptor, alongside 19 nM and 152 nM for μ and κ receptors, respectively. Research indicates that Naltriben mesylate enhances glioblastoma cell migration and invasion, making it a valuable tool for studies related to neurological diseases and cancer biology.
  13. μ-opioid Receptor Activator, hERG (Kv11.1) Potassium Channel Inhibitor

    ERG-IN-6 is a potent μ-opioid receptor activator, exhibiting an EC50 of 0.12 nM, which makes it an effective tool for studies related to pain modulation. Additionally, ERG-IN-6 functions as a hERG (Kv11.1) potassium channel inhibitor with an IC50 of 0.681 μM. This compound is valuable for research applications investigating the interplay between opioid signaling and ion channel regulation.
  14. Calcium Channel

    C18 LPA (PA(18:0e/0:0)) targets calcium channels and serves as a bioactive phospholipid involved in signal transduction via G protein-coupled receptors (GPCRs). This compound promotes smooth muscle contraction, chemotaxis, cytoskeletal rearrangement, and is implicated in neurotransmitter release and cell proliferation. Increased levels of C18 LPA in human plasma are correlated with ovarian cancer and atherosclerosis, indicating its potential utility as a biomarker in oncological and cardiovascular research.
  15. HCN Channel Blocker

    Ivabradine impurity 1 is a derivative of Ivabradine, a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker. This compound has been utilized in research to investigate the modulation of cardiac rhythms and treatment of conditions such as angina and heart failure. Its biological activity contributes to the understanding of ion channel interactions and cardiac electrophysiology.
  16. Overoxidized By-product of Lansoprazole

    Lansoprazole N-oxide is the overoxidized by-product derived from the synthesis of the proton pump inhibitor Lansoprazole. This compound is of interest for studies related to gastrointestinal disorders, including duodenal and gastric ulcers, reflux esophagitis, and Zollinger–Ellison syndrome. Researchers may utilize Lansoprazole N-oxide to deepen the understanding of proton pump inhibition and its implications in these conditions.
  17. Drug Metabolite

    15-Hydroxy Lubiprostone is an active metabolite of the laxative drug Lubiprostone, primarily targeting chloride channels. This compound exhibits biological activity by promoting fluid secretion in the intestinal lumen, thereby facilitating bowel movements. It is mainly utilized in research applications focused on gastrointestinal pharmacology and the mechanisms of action related to chloride channel activation.
  18. Overoxidized By-product of Lansoprazole

    Lansoprazole sulfone N-Oxide is an overoxidized by-product generated during the synthesis of the proton pump inhibitor Lansoprazole. This compound is relevant for research into gastrointestinal conditions, such as duodenal and gastric ulcers, reflux esophagitis, and Zollinger–Ellison syndrome. Its study may provide insights into the metabolic pathways and potential therapeutic implications related to proton pump inhibition.
  19. Bupivacaine metabolite

    Bupivacaine N-oxide hydrochloride is a metabolite of the local anesthetic Bupivacaine, which primarily acts as an NMDA receptor inhibitor. It also exhibits significant activity by blocking sodium, L-calcium, and potassium channels, particularly SCN5A channels with an IC50 of 69.5 μM. This compound is relevant for research into chronic pain mechanisms and provides insight into the pharmacological action of Bupivacaine and its derivatives.
  20. Active Metabolite of T-1095

    T-1095A is the active metabolite of T-1095, functioning as a sodium-glucose cotransporter (SGLT) inhibitor. This compound demonstrates significant biological activity in the regulation of glucose reabsorption in the renal system and is primarily utilized in research related to diabetes and metabolic disorders. Its mechanism of action aids in the investigation of glucose homeostasis and associated therapeutic strategies.
  21. Sodium Channel Inhibitor

    Decarbamoylsaxitoxin is a potent sodium channel inhibitor that selectively blocks the influx of sodium ions in excitable tissues, such as nerve and skeletal muscle cells, thus preventing action potential generation. As a hydrolysis product of saxitoxin, Decarbamoylsaxitoxin exhibits similar neurotoxic effects, including the ability to inhibit veratridine- and ouabain-induced neuroblastoma cell swelling and lysis. This reagent is valuable for research involving mechanisms of paralytic shellfish poisoning and sodium channel pharmacology.
  22. Drug Metabolite Control

    Nicorandil pyridine oxide is a metabolite of Nicorandil, which acts as an activator of the sulfonylurea receptor 2B (SUR2B) and the ATP-sensitive potassium channel Kir6.2. This compound serves as a crucial tool for drug metabolite control, offering insights into the pharmacokinetics and therapeutic mechanisms of Nicorandil. Its biological activity is important for researchers studying cardiovascular effects and the modulation of ion channels in various biological systems.
  23. EBP Inhibitor

    EBP-IN-1 is a selective inhibitor of emopamil binding protein (EBP) that effectively crosses the blood-brain barrier. This compound demonstrates an IC50 of 8.2 μM against human ERG potassium channels in CHO cells, leading to the inhibition of EBP's sterol isomerase activity and subsequent accumulation of Zymostenol. EBP-IN-1 has been shown to promote oligodendrocyte differentiation in human cortical organoids, making it a valuable tool for research into multiple sclerosis and related neurological disorders.
  24. Calcium Influx/NO Modulator

    Palmitoylglycine (N-palmitoyl glycine) is an endogenous lipid that functions as a modulator of calcium influx and nitric oxide production in sensory neurons. This compound is associated with an increased risk of Brugada syndrome (BrS) and interacts with various BrS-related proteins, displaying moderate binding affinities for DCC, CR1, CTSB, NAAA, DEFB1, EPHA1, IGF1/IGFBP3/ALS, and LTA. Palmitoylglycine is valuable in research investigating its roles in neuronal signaling and cardiovascular conditions linked to BrS.
  25. Calcium Channel Inhibitor

    Ethacrynic acid sodium is an effective calcium channel inhibitor that primarily targets L-type voltage-dependent and store-operated calcium channels. This compound exhibits diuretic properties and significantly modulates glutathione S-transferases (GSTs) while inhibiting the NF-kB signaling pathway. Ethacrynic acid sodium demonstrates anti-inflammatory activity, evidenced by its ability to reduce retinoid-induced ear edema in murine models, making it a valuable tool in research focused on inflammation and airway smooth muscle relaxation.
  26. Calcium Channel Blockers

    Levamlodipine hydrochloride is a dihydropyridine calcium channel blocker that primarily targets L-type calcium channels on vascular smooth muscle cells. By inhibiting calcium ion influx, it promotes vasodilation, effectively lowering blood pressure and alleviating angina. Additionally, its binding affinity to human serum albumin (HSA) enhances research into drug transport and release mechanisms within the body. This compound is beneficial for studies focused on cardiovascular therapies and mechanisms of action related to hypertension and coronary artery disease.
  27. Calcium Channel Inhibitor

    Levamlodipine hydrobromide is a calcium channel inhibitor with notable antioxidant and vasodilatory properties. This compound has been shown to reduce serum malondialdehyde (MDA) levels while increasing superoxide dismutase (SOD) activity, thus improving oxidative stress responses. It is appropriate for research applications related to vascular dementia, hypertension, and cerebrovascular diseases.
  28. Calcium Channel Blocker

    Levamlodipine besylate hemipentahydrate is a calcium channel blocker that exhibits significant antioxidant and vasodilatory effects. This compound has been shown to lower serum malondialdehyde (MDA) levels while enhancing superoxide dismutase (SOD) activity, thereby mitigating oxidative stress. Levamlodipine besylate hemipentahydrate is suitable for research applications focused on vascular dementia, hypertension, and cerebrovascular diseases.
  29. TLR4/HCN Inhibitor

    HCN-IN-1 is a TLR4 inhibitor and modulator of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels, specifically targeting HCN2 and HCN4. It effectively inhibits TLR4-mediated signaling, evidenced by reduced alkaline phosphatase activity. HCN-IN-1 modulates HCN2 currents by shifting the voltage-dependent activation to hyperpolarized potentials and slowing activation kinetics, while also blocking currents through HCN4 channels. This compound demonstrates significant analgesic, anti-inflammatory, and anti-anginal properties, making it valuable for research into inflammatory pain, neuropathic pain, heart failure, and related inflammatory conditions.
  30. ATPase

    Creatine phosphokinase, Rabbit muscle (CPK) is an enzyme that catalyzes the reversible conversion of creatine and ATP into phosphocreatine and ADP. By facilitating the maintenance of an optimal ATP/ADP ratio, CPK plays a critical role in energy metabolism, particularly during periods of high energy demand. This enzyme is widely used in biochemical research to study cellular energy dynamics and various metabolic disorders.
  31. BCRP Inhibitor

    5,7-Dimethoxyflavone is a potent inhibitor of the Breast Cancer Resistance Protein (BCRP). It exhibits significant biological activities, including anti-obesity, anti-inflammatory, and antineoplastic effects. Additionally, this compound has been shown to inhibit cytochrome P450 (CYP) 3A enzymes, making it valuable for research applications focused on drug resistance and metabolic pathways in cancer therapy.
  32. Sodium Channel Blocker

    CAY10568 is a sodium channel blocker that modulates neuronal excitability. This compound, a derivative of QX-314, exhibits a smaller and less hydrophobic profile, making it suitable for exploring its effects on inflammation and pain perception. CAY10568 is valuable for research applications aimed at understanding pain mechanisms and developing analgesic therapies.
  33. Sodium Channel Inhibitor

    (-)-Sparteine sulfate pentahydrate is a sodium channel inhibitor that acts as a class 1a antiarrhythmic agent. It has demonstrated notable biological activity in modulating cardiac excitability and can be utilized in research focusing on arrhythmias and pharmacological studies related to ion channel function. This reagent is suitable for investigating the effects of sodium channel blockade in various biological models.
  34. Nav1.7 Inhibitor

    Nav1.7-IN-6 is a selective inhibitor targeting the voltage-gated sodium channel Nav1.7, which is important in pain signaling pathways. This compound demonstrates significant biological activity in modulating neuronal excitability, making it a valuable tool for research on pain mechanisms and potential therapeutic interventions in pain disorders. Its specificity for Nav1.7 enhances its utility in elucidating the role of this channel in nociception and related studies.
  35. NaV1.7 Antagonist

    AMG8379 is a selective sulfonamide antagonist targeting the voltage-gated sodium channel NaV1.7. It demonstrates potent inhibition with IC50 values of 8.5 nM for human NaV1.7 and 18.6 nM for mouse NaV1.7, effectively blocking TTX-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM. This compound is useful for research applications related to pain pathways and sodium channel modulation.
  36. Sodium Channel Inhibitor

    B-GYKI-38233 hydrochloride is a sodium channel inhibitor that exhibits potent antiarrhythmic properties. This compound is utilized in research focused on the modulation of sodium channels, which play a critical role in cardiac excitability and conductivity. Its mechanism of action makes it a valuable tool for the investigation of arrhythmias and related cardiovascular disorders.
  37. Nav1.8 channel Inhibitor

    Nav1.8-IN-10 is a selective inhibitor of the Nav1.8 ion channel. At a concentration of 4 nM, it achieves an impressive blocking rate of 79.4%, demonstrating its potency. This compound is primarily utilized in the research of pain disorders, facilitating investigations into the modulation of pain pathways and potential therapeutic interventions.
  38. Nav1.8 Inhibitor

    Nav1.8-IN-5 is a selective inhibitor of the voltage-gated sodium channel Nav1.8. It demonstrates potent biological activity against Nav1.8-mediated pain and pain-related disorders, making it a valuable tool for research in these areas. Additionally, Nav1.8-IN-5 can facilitate studies related to cardiovascular diseases, including conditions such as atrial fibrillation, by modulating sodium channel activity.
  39. Sodium Channel Inhibitor

    R 59494 is a sodium channel inhibitor that effectively blocks Na+ and Ca2+ uptake triggered by veratridine exposure. This compound exhibits significant anti-ischemic properties, making it valuable for research in cardiovascular and neuroprotective studies. Its ability to modulate ion channel activity positions R 59494 as a useful tool for investigating the mechanisms of ischemia-related cellular damage.
  40. Nav1.7 Blocker

    NAV 26 is a selective blocker of the voltage-gated sodium channel Nav1.7, exhibiting an IC50 of 0.37 μM. This compound is valuable for investigating pain mechanisms and developing novel analgesics. Its specificity for Nav1.7 makes it a crucial tool in researching pain pathways and potential therapeutic interventions.
  41. NaV1.8 Channel Inhibitor

    Analgesic agent-2 is a selective NaV1.8 channel inhibitor, exhibiting a reported IC50 of 50.18 nM in HEK293 cells expressing the human NaV1.8 channel. It demonstrates significant analgesic activity, making it a valuable tool for pain research. This compound is ideal for studies investigating the role of NaV1.8 in nociception and the development of novel analgesic therapies.
  42. Nav1.8 Inhibitor

    Nav1.8-IN-15 is a potent inhibitor of the voltage-gated sodium channel Nav1.8. It demonstrates significant analgesic effects and is relevant for research exploring pathways involved in chronic pain management. This compound can facilitate the study of Nav1.8's role in pain signaling and aid in the development of novel therapeutic strategies for pain relief.
  43. NaV1.7 Antagonist

    AMG8380 is a selective antagonist of the voltage-gated sodium channel NaV1.7, exhibiting IC50 values of 0.907 µM and 0.387 µM in human and mouse tissues, respectively. This compound effectively inhibits Tetrodotoxin (TTX)-sensitive native channels with an IC50 of 2560 nM, making it a valuable tool for research on pain pathways and sodium channel function. Its properties allow for exploration of NaV1.7's role in nociception and related applications in pharmacological studies.
  44. NaV1.7 Inhibitor

    Sodium Channel-IN-7 is a selective inhibitor of the NaV1.7 voltage-gated sodium channel. It interacts with the voltage-sensor domain 4 (VSD4) binding pocket of NaV1.7, demonstrating limited interaction with residue Try1537. This compound is primarily utilized in research focused on pain mechanisms and pain-related disorders.
  45. Sodium Channel Inhibitor

    Cofirasersen is a sodium channel inhibitor that targets the epithelial sodium channel (ENaC). It is specifically developed to downregulate ENaC expression in the lungs, where hyperactivity of ENaC is implicated in cystic fibrosis, a disorder linked to mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) gene. This compound has potential applications in research related to cystic fibrosis and the modulation of sodium transport in pulmonary tissues.
  46. Nav1.7 Antagonist

    Nav1.7-IN-15 is a potent state-dependent antagonist of the sodium channel Nav1.7, exhibiting an IC50 of 0.42 μM for human Nav1.7 PX. This compound is valuable for studying pain mechanisms and is useful in research focusing on neuropathic pain and other conditions associated with Nav1.7 activity. Its ability to selectively inhibit Nav1.7 makes it an important tool for investigating the therapeutic potential of sodium channel modulation.
  47. NaV1.7 Inhibitor

    PF-06456384 is a potent and selective inhibitor of NaV1.7, exhibiting an IC50 of 0.01 nM. This compound is primarily utilized in research involving pain mechanisms, particularly in formalin pain model studies, to elucidate the role of NaV1.7 in nociceptive signaling. Its high selectivity makes it an important reagent for exploring therapeutic strategies targeting chronic pain conditions.
  48. Sodium Channel Inhibitor

    Nav1.8-IN-1 is a selective inhibitor of the Na(v)1.8 sodium channel, demonstrating significant potency in blocking its activity. This compound is particularly relevant for research focused on inflammatory and neuropathic pain pathways, providing valuable insights into pain mechanisms and potential therapeutic strategies. Its ability to modulate sodium channel function makes it a promising tool for understanding pain-related conditions.
  49. Sodium Channel Blocker

    BW-4030W92 is a selective sodium channel blocker that inhibits sodium ion influx. This compound is utilized in research to study the role of sodium channels in neuronal excitability and can induce ataxia, providing insights into neurological disorders. Its application is significant in pharmacological studies aiming to investigate the mechanisms of action of sodium channel modulation.
  50. NaV Modulator

    Clathrodin is a marine alkaloid derived from Agelas sponges that functions as a modulator of voltage-gated sodium (NaV) channels. As a sodium channel neurotoxin, Clathrodin impacts sodium channel ionic conductance, making it a valuable tool for studying excitability in neurons and muscle cells. This reagent is useful in research applications involving neuropathic pain, neurotoxicity assessments, and the physiological characterization of sodium channel function.

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