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. ASK1 Inhibitor

    ASK1-IN-10 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 value of less than 200 nM. In addition to its primary mechanism, ASK1-IN-10 exhibits inhibitory activity against hERG potassium channels. This compound serves as a valuable tool for investigating the role of ASK1 in inflammation-related research and its potential therapeutic implications.
  6. Potassium Channel Opener

    Bimakalim is an ATP-sensitive potassium channel opener that induces vasodilation by enhancing potassium ion efflux. This compound has been shown to reduce transmural myeloperoxidase (MPO) activity and mimics ischemic preconditioning effects, leading to decreased infarct size and modulation of adenosine release and neutrophil function. Bimakalim is valuable for research applications focused on cardiovascular physiology and ischemia-reperfusion injury studies.
  7. 8,9-Z-isomer of Abamectin B1a

    8,9-Z-Abamectin B1a is the 8,9-Z isomer of Abamectin B1a, a key antiparasitic agent. It effectively paralyzes nematodes by interacting with glutamate-gated chloride channels, leading to increased permeability of cell membranes and subsequent paralysis. This compound is widely utilized in research related to parasitology and therapeutic development for nematode infections.
  8. Antiparasitic Agent

    Avermectin A1a is a potent antiparasitic agent that primarily targets nematodes and arthropods. It binds to glutamate-gated chloride channels, effectively blocking nerve signal transmission, which leads to paralysis of the parasites. Avermectin A1a is valuable for research on parasitic infections and contributes to the understanding of mechanisms involved in parasitic control.
  9. Insecticide

    Avermectin B2a is an insecticide that targets glutamate-gated chloride channels (GluCls). Its primary mechanism induces hyperpolarization in nematode and insect neurons, leading to paralysis and mortality. This compound is relevant for research into the control of agricultural pests and the exploration of neurotoxic mechanisms in pests.
  10. Antiparasitic Agent

    Δ2-Avermectin B1a is an antiparasitic agent that targets glutamate-gated chloride channels (GluCls) in the neuromuscular systems of invertebrates. By enhancing chloride ion influx, it induces hyperpolarization of the neuromuscular cell membrane, which inhibits neural signal transmission and ultimately results in paralysis and death of parasites. This compound is of significant interest for research applications aimed at controlling agricultural pests.
  11. Stable Isotope

    Flufenamic acid-d4 is a deuterium-labeled derivative of Flufenamic acid, a non-steroidal anti-inflammatory drug. It primarily functions as a cyclooxygenase (COX) inhibitor while also activating AMP-activated protein kinase (AMPK) and modulating various ion channels, including chloride channels and L-type Ca2+ channels. This compound inhibits TEAD2 YBD functionality, affecting YAP-dependent processes such as cell migration and proliferation. Flufenamic acid-d4 is thus a valuable tool for studies in inflammation, cell signaling, and cancer research.
  12. Parasite

    Doramectin monosaccharide, an acid degradation product of Doramectin, targets glutamate- and GABA-gated chloride channels in nematodes, enhancing their opening and resulting in effective anthelminthic activity. This compound is useful for studying the pharmacodynamics of anthelmintics and exploring mechanisms of resistance in parasitic infection research. Its significance lies in its role in understanding the biochemical pathways involved in nematode neuromuscular function and development.
  13. hERG Inhibitor

    GSK369796 is a selective inhibitor of the hERG potassium ion channel, demonstrating an IC50 value of 7.5 μM. This compound exhibits significant antimalarial activity, making it a valuable tool for research in both cardiac function and malaria therapeutics. Its potential implications in pharmacology and drug development provide a basis for further exploration in ion channel regulation and associated biological pathways.
  14. Parasiticide

    Sisapronil is a phenylpyrazole compound that functions as an ectoparasiticide by inhibiting the GABA-gated chloride channels in parasites, leading to paralysis and death. It exhibits potent activity against a variety of ectoparasites, making it valuable in veterinary medicine for controlling infestations. This compound is utilized in research to investigate mechanisms of action against parasitic infections.
  15. FRα Modulator

    Ricorfotide vedotin is a dual-ligand peptide-drug conjugate that primarily targets Folate receptor α (FRα) while also binding to TRPV6. It exhibits high-affinity binding to FRα and low-affinity interaction with TRPV6, demonstrating notable antitumor activity. This reagent is applicable in advanced solid tumor research, including studies focused on colorectal cancer, breast cancer, non-small cell lung cancer, ovarian cancer, adrenocortical carcinoma, and follicular dendritic cell sarcoma.
  16. 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.
  17. 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.
  18. 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.
  19. Antibiotic

    Milbemycin α10 is a macrolide antibiotic that targets glutamate-gated chloride channels in nematodes and arthropods. It exhibits potent insecticidal activity, effectively controlling a variety of agricultural pests, including larvae and other harmful insects. This compound is valuable for research in agricultural biotechnology and pest management.
  20. Parasite Inhibitor

    Milbemycin oxime is an orally active macrolide that serves as a potent inhibitor of parasite activity. This compound, a mixture of oxime derivatives related to milbemycin A4 and A3, selectively binds to glutamate-gated chloride channels, leading to paralysis and death of various intestinal nematodes and lung/heart worms. It is widely utilized in research focused on antiparasitic drug development and mechanisms of parasitic resistance.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. AMPAR Modulator

    Nooglutil is a positive modulator of AMPA-type glutamate receptors (AMPARs), enhancing synaptic transmission and plasticity. Additionally, it regulates dopamine D2 receptor function, contributing to its anxiolytic effects. This compound is of significant interest for research into neurodegenerative disorders, including Alzheimer's disease, and offers potential insights into therapeutic strategies targeting glutamatergic and dopaminergic systems.
  26. Dopamine Receptor Inhibitor

    Valbenazine dihydrochloride is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2) and primarily targets dopamine receptors. It is utilized in the treatment of tardive dyskinesia, offering therapeutic benefits for alleviating movement disorder symptoms linked to chronic dopamine receptor antagonism. Extensive preclinical studies support its efficacy, particularly in relation to the genetic factors contributing to tardive dyskinesia.
  27. Calcium Entry-Blocking

    YM-430 is a calcium entry-blocking and beta-adrenoceptor-blocking agent. It effectively inhibits Amifampridine-induced rhythmic contractions with an IC50 value of 59.2 nM and blocks arginine vasopressin-induced ST-segment depression with an IC50 of 36.6 mg/kg. This compound is valuable for research into angina pectoris and related cardiovascular conditions.
  28. CB1 and TRPV1 agonist

    N-Arachidonyldopamine is a selective agonist of the CB1 and TRPV1 receptors, exhibiting a Ki value of 250 nM for the CB1 receptor and an EC50 of approximately 50 nM for TRPV1. This compound plays a significant role in modulating pain and inflammatory responses, making it a valuable tool for research investigating endocannabinoid signaling pathways and their implications in various physiological processes.
  29. CB1 Agonist

    (R)-Methanandamide is a potent CB1 receptor agonist, exhibiting a Ki value of 20 nM. This compound serves as an analytical tool for studying cannabinoid signaling pathways and the endocannabinoid system. Additionally, (R)-Methanandamide can activate vanilloid (TRPV1) receptors, highlighting its potential applications in pain research and modulation of inflammatory processes in cellular assays.
  30. VR1/CB1 Agonist

    OMDM-6 is a hybrid agonist targeting vanilloid receptor type 1 (VR1, TRPV1) with an EC50 of 75 nM and cannabinoid receptor type 1 (CB1) with a Ki of 3.2 μM. This compound also inhibits the cellular uptake of anandamide, demonstrating a Ki of 7.0 μM. Due to its dual mechanism of action, OMDM-6 is valuable for research applications exploring pain modulation and the endocannabinoid system.
  31. Cannabinoid Receptor

    CB2 receptor antagonist 1 is a selective competitive antagonist of the cannabinoid receptor CB2, exhibiting strong potency. This hexyl resorcinol derivative not only effectively inhibits CB2 receptor activity but also demonstrates significant antinociceptive properties. Additionally, it has been observed to activate both cannabinoid and TRPV1 receptors, making it a valuable tool for research in pain modulation and cannabinoid signaling pathways.
  32. CB1 Agonist

    CB1/2 agonist 4 serves as a full agonist for the CB1 receptor and a partial agonist for the CB2 receptor, exhibiting EC50 values of 15.09 nM and 1.16 nM, respectively. It demonstrates high affinity for human CB1 and CB2 receptors, with Ki values of 1.1 nM and 4.2 nM. This compound displays notable antinociceptive activity and effectively activates both cannabinoid and TRPV1 receptors, featuring IC50 and EC50 values of 0.8 μM and 0.12 μM, respectively. CB1/2 agonist 4 is valuable for studies exploring cannabinoid receptor functions and their implications in pain modulation.
  33. CB1/2 Agonist

    AB-FUBICA is a potent agonist for CB1 and CB2 receptors, serving as a valuable tool in cannabinoid research. It functions by activating G-protein coupled inwardly rectifying potassium channels (GIRK) through its binding to these receptors, demonstrating significant cannabinoid-like activity. With EC50 values of 21 nM for CB1 and 15 nM for CB2, AB-FUBICA is ideal for investigating pain management, neurodegenerative diseases, and inflammation-related pathways.
  34. Multi-target modulator

    PQM-244 is a multi-target modulator that primarily interacts with TRPV1 and cannabinoid receptors CB1 and CB2. It exhibits noteworthy peripheral antinociceptive properties, effectively addressing both neurogenic and inflammatory pain. Additionally, PQM-244 demonstrates antioxidant activity with an IC50 of 14.15 µM for radical scavenging of DPPH. This compound is suitable for research applications related to chronic pain and inflammatory conditions, including diabetes, atherosclerosis, and Alzheimer's disease.
  35. Nucleoside Transport Blocker

    (S)-Draflazine is a selective nucleoside transport blocker that effectively inhibits nucleoside uptake. This compound demonstrates significant biological activity in modulating nucleoside transport mechanisms. (S)-Draflazine is utilized in research contexts to study nucleoside-related processes and their implications in various biological pathways and diseases.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. Anxiolytic Agent

    Succinic acid sodium functions as an effective anxiolytic agent. It has demonstrated inhibitory effects on colonic epithelial cell proliferation in vivo and can down-regulate the expression of key genes such as KCNMB1 and TET1. This compound is particularly useful for research involving gestational hypertension and related physiological studies.
  43. p97 ATPase Inhibitor

    p97-IN-2 is a selective inhibitor of the p97 ATPase, with an IC50 of 0.6 μM. This compound effectively inhibits the proliferation of cancer cell lines, including HCT15 (IC50 = 1.1 μM) and SW403 (IC50 = 0.8 μM). p97-IN-2 serves as a valuable tool for investigating the role of p97 in cancer biology and therapeutic applications.
  44. ERAD Inhibitor

    NCATS-SM0225 is an endoplasmic reticulum-associated degradation (ERAD) inhibitor that functions as a direct binder to VDAC1, VDAC2, and VDAC3. It demonstrates an IC50 of 1.02 μM for inhibiting ERAD and a Kd of 3.13 μM for binding human VDAC1. By disrupting cellular calcium homeostasis and enhancing VDAC1-IP3R coupling, NCATS-SM0225 activates the PERK pathway and selectively induces apoptosis in cancer cells. This reagent is valuable for investigating cancer biology, particularly in melanoma, as well as exploring the underlying mechanisms of ERAD and calcium homeostasis regulation.
  45. Serotonin And Norepinephrine Reuptake Inhibitor

    Milnacipran is an orally active serotonin and norepinephrine reuptake inhibitor that primarily targets the monoamine transporters responsible for neurotransmitter reuptake. It demonstrates high affinity for the norepinephrine transporter and serotonin transporter, with Ki values of 31 nM and 8.5 nM, respectively. Milnacipran exhibits antidepressant, anxiolytic, and analgesic properties, and has been shown to inhibit pERK1/2 activation. This compound is applicable in the study of major depressive disorder, anxiety disorders, and neuropathic pain conditions such as fibromyalgia.
  46. Stable Isotope

    Milnacipran-d5 hydrochloride is a deuterated form of Milnacipran hydrochloride, a potent serotonin and norepinephrine reuptake inhibitor. It targets monoamine transporters, exhibiting Ki values of 31 nM for the norepinephrine transporter and 8.5 nM for the serotonin transporter. With notable antidepressant, anxiolytic, and analgesic properties, Milnacipran-d5 hydrochloride is valuable for research on major depressive disorder, anxiety disorders, and neuropathic pain conditions such as fibromyalgia. Additionally, it has been shown to affect behavior in preclinical models, providing insights into its pharmacological mechanisms.
  47. Stable Isotope

    Milnacipran-d10 hydrochloride is a deuterium-labeled form of the serotonin and norepinephrine reuptake inhibitor, Milnacipran hydrochloride. It effectively inhibits monoamine transporters, targeting the norepinephrine and serotonin transporters with reported Ki values of 31 nM and 8.5 nM, respectively. This compound exhibits antidepressant, anxiolytic, and analgesic properties, and has demonstrated efficacy in reducing biting behavior in murine models. Milnacipran-d10 hydrochloride is valuable for research applications focused on major depressive disorder, anxiety disorders, and neuropathic pain syndromes, such as fibromyalgia.
  48. RAD51 Inhibitor

    DIDS is a RAD51 inhibitor that disrupts RAD51-mediated homologous pairing and strand exchange reactions, thereby impacting DNA repair processes. In addition to its primary function, DIDS also inhibits ABCA1 and VDAC1, affecting anion exchange and binding to red blood cell membranes. Furthermore, it has been shown to inhibit the activation of caspase-3 and -9, making it a valuable tool for cancer research applications.
  49. Proton Pump Inhibitor

    Ilaprazole sodium hydrate is a potent proton pump inhibitor that irreversibly targets H+/K+-ATPase, exhibiting an IC50 value of 6 μM in rabbit parietal cell preparations. This compound is primarily utilized in research related to gastric ulcers, providing insights into gastric acid secretion and its regulation. In addition, Ilaprazole sodium hydrate demonstrates inhibitory activity against TOPK (T-lymphokine-activated killer cell-originated protein kinase), making it a valuable tool for studies on cellular signaling pathways and cancer research.
  50. Adrenergic Receptor

    FFN270 hydrochloride is a fluorescent tracer that specifically targets adrenergic receptors, functioning as a substrate for norepinephrine and vesicular monoamine transporters. This compound displays distinct absorption and excitation maxima at either 320 nm or 365 nm depending on the solvent pH, with an emission wavelength of 475 nm. FFN270 hydrochloride is valuable in research applications that involve monitoring norepinephrine dynamics and can also serve as a ratiometric pH sensor for various biological studies.

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