Membrane Transporters-Ion Channels

Items 901-950 of 2532

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  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. ORL1 Receptor Antagonist

    MK-1925 is a selective ORL1 receptor antagonist, demonstrating human IC50 values of 8.2 nM and 4.6 nM. This compound exhibits oral bioavailability and the capability to penetrate the blood-brain barrier, making it a valuable tool for neuroscience research. MK-1925 specifically inhibits the ORL1 receptor without significant interaction with other opioid receptors or the hERG potassium channel, positioning it as a potential candidate for studies focused on pain modulation and opioid receptor mechanisms.
  12. ORL1 Antagonist

    ORL1 antagonist 2 is a selective antagonist of the opioid receptor-like 1 (ORL1). This compound has been primarily utilized in the study of P-glycoprotein (P-gp) interactions and transport mechanisms. Its ability to modulate ORL1 activity makes it a valuable tool in research aimed at understanding opioid signaling pathways and their implications in various physiological and pathological processes.
  13. Na+ Channel Blocker

    RSD-921 is a potent sodium (Na+) channel blocker exhibiting significant anti-arrhythmic properties. It acts with state- and voltage-dependent inhibition on the open states of cardiac, skeletal muscle, and neuronal Na+ channels. Additionally, RSD-921 has a low affinity for κ-opioid receptors and shows weak κ-agonistic activity in vitro. This reagent is valuable for research focusing on cardiac arrhythmias and the modulation of Na+ channels in various biological models.
  14. TRPV1 Antagonist/MOR Agonist

    TRPV1 Antagonist 11 is a potent antagonist of the TRPV1 receptor, exhibiting an IC50 of 29.3 nM. Additionally, it serves as a μ-opioid receptor (MOR) agonist with a Ki value of 60.3 nM. This compound demonstrates significant analgesic properties by antagonizing TRPV1, thereby reducing pain signaling, and activating MOR, which enhances the pain-relief effect. TRPV1 Antagonist 11 has been shown to provide a robust, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice, making it a valuable tool for pain research.
  15. δ2-opioid Receptor Antagonist/TRPM7 Activator

    Naltriben is a selective antagonist of the δ2-opioid receptor and an activator of TRPM7 channels. It has been shown to enhance migration and invasion of glioblastoma cells, making it a valuable tool for studying tumor biology. This compound is suited for research into neurological disorders and cancer mechanisms, providing insights into therapeutic approaches targeting these areas.
  16. OT Receptor Agonist

    (Thr4,Gly7)-Oxytocin is a specific agonist of the oxytocin receptor (OT receptor). This analogue enhances neuronal excitability in subicular neurons through the activation of TRPV1 channels and the inhibition of K+ channels. Its unique properties make it valuable for research applications involving neurobiology and the study of oxytocin-related pathways.
  17. TRPV1 Inhibitor

    (±)-Eriodictyol is a potent TRPV1 receptor antagonist, exhibiting an IC50 value of 44-47 nM in rTRPV1 assays. This compound demonstrates significant antioxidant and anti-inflammatory properties, effectively inhibiting lipid peroxidation and reducing the release of proinflammatory cytokines. By modulating the Nrf2 signaling pathway, (±)-Eriodictyol helps maintain the integrity of the blood-retinal barrier and can alleviate oxidative stress-induced apoptosis and hyperalgesia. It has potential applications in the research of diabetic retinopathy, acute lung injury, and various pain-related conditions, while also enhancing immune cell activity and promoting antioxidant enzyme levels.
  18. Endogenous Metabolite

    N-Oleoyl Taurine is an endogenous metabolite that acts as an amino-acyl endocannabinoid. It is known to activate transient receptor potential (TRP) channels, specifically TRPV1 and TRPV4, implicating its role in calcium signaling. This compound has been isolated from rat brain and presents potential applications in research studying the physiological effects of TRP channel modulation and its involvement in neurological functions.
  19. Antiarrhythmic Agent

    Droxicainide hydrochloride is an antiarrhythmic agent primarily targeting sodium channels. It is effective in the management of ventricular arrhythmias and is utilized in research to investigate cardiac electrophysiology. The compound is valuable for studying interactions in cardiac tissues and assessing the effects of sodium channel modulation on heart rhythm disorders.
  20. Endogenous Metabolite

    N-Stearoyl Taurine is an endogenous metabolite that exhibits activity as a fatty acyl amide. It demonstrates the ability to activate members of the transient receptor potential (TRP) family of calcium channels, linking it to various physiological processes. This compound is primarily used in research applications related to lipidomics and neurobiology, particularly in studies investigating the role of amino-acyl endocannabinoids in the central nervous system. Its discovery in rat brain lipid profiles underscores its significance in the exploration of neuronal signaling pathways.
  21. Endogenous Metabolite

    N-Lignoceroyl Taurine is an endogenous metabolite and taurine conjugate of lignoceric acid, identified through lipidomic analysis of bovine brain. This compound exhibits distinct biological activity as a substrate for fatty acid amide hydrolase (FAAH), with levels significantly elevated in FAAH knockout mice, indicating a potential role in lipid metabolism. Additionally, N-Lignoceroyl Taurine has been shown to activate transient receptor potential (TRP) calcium channels, including TRPV1 and TRPV4, highlighting its relevance in neurobiology and cellular signaling research.
  22. Natural Products

    Thevetin A is a cardiac glycoside derived from the plant Cascabela thevetioides. It exhibits potent biological activity by inhibiting Na+/K+ ATPase, leading to increased intracellular calcium levels and enhanced contractility of cardiac muscle. This compound is primarily utilized in cardiovascular research to study its effects on cardiac function and potential therapeutic applications in heart disease.
  23. 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.
  24. 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.
  25. 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.
  26. Endogenous Metabolite

    UCCF-029 free base is a potent activator of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel. This compound showcases enhanced activity due to the benzannulation of the flavone A-ring at the 7,8-position, serving as a critical structural reference for the development of more effective flavonoid analogues. UCCF-029 demonstrates superior potency compared to apigenin in activating wild-type CFTR and possesses potential for activating the mutant G551D-CFTR, though its efficacy in this regard is not as pronounced as that of apigenin. This reagent is valuable for research into cystic fibrosis and related therapeutic strategies.
  27. Endogenous Metabolite

    ISQ-1 hydrochloride is an isoquinolinone compound that functions as an inhibitor of the IKur potassium channel. It demonstrates potential to influence cardiac electrophysiology by modulating arrhythmic activity in atrial tissues. This reagent is primarily utilized in research focused on cardiac rhythm disorders and electrophysiological studies of heart functions.
  28. Furin Inhibitor

    BOS-318 is a highly selective and cell-permeable inhibitor of furin, exhibiting an IC50 value of 1.9 nM. This compound demonstrates the ability to protect epithelial sodium channels (ENaC) from activation by neutrophil elastase. BOS-318 is a valuable tool for research focused on cystic fibrosis and related pulmonary conditions.
  29. Stable Isotope

    Safinamide-d4-1 is a deuterium-labeled derivative of Safinamide, a selective and reversible inhibitor of monoamine oxidase B (MAO-B) with an IC50 of 0.098 μM, demonstrating significantly lower inhibition of MAO-A (IC50=580 μM). In addition to its MAO-B inhibitory activity, Safinamide also interacts with sodium channels and modulates glutamate release, exhibiting a greater affinity at depolarized potentials (IC50=8 μM) compared to resting potentials (IC50=262 μM). This reagent is valuable for research applications related to neurobiology, particularly in the investigation of Parkinson's disease and ischemic stroke mechanisms.
  30. Serotonin Transporter Inhibitor

    Lubazodone hydrochloride is a selective serotonin transporter inhibitor that primarily modulates serotonin levels in the central nervous system. Its biological activity is associated with antidepressant effects, making it a valuable compound for research into the treatment of depression and related mood disorders. This reagent can aid in the exploration of serotonin dynamics and its implications in various neurobiological studies.
  31. Serotonin Reuptake Inhibitor

    Citalopram is a selective serotonin reuptake inhibitor (SSRI) that primarily targets the serotonin transporter, resulting in increased serotonergic neurotransmission. This compound is utilized for its antidepressant properties and is effective in the treatment of major depressive disorder and anxiety-related conditions. Research applications include studies on mood regulation and neurotransmitter dynamics.
  32. Serotonin Transporter Inhibitor

    Fluvoxamine is a selective serotonin reuptake inhibitor (SSRI) that targets the serotonin transporter. It is primarily used in the treatment of obsessive-compulsive disorder and depression by increasing serotonin levels in the synaptic cleft. This compound is valuable in research applications exploring mood regulation, anxiety disorders, and the neural mechanisms underlying depression.
  33. SERT Inhibitor

    SERT-IN-2 is a potent serotonin transporter (SERT) inhibitor, demonstrating an IC50 of 0.58 nM. This compound exhibits significant anti-depressive activity and shows a high bioavailability of 83.28% in rat models. Additionally, SERT-IN-2 possesses the ability to cross the blood-brain barrier, making it a valuable tool for research into mood disorders and related pharmacological studies.
  34. Antidepressant Agent

    ZZL-7 is a fast-onset antidepressant agent that targets the interaction between the serotonin transporter (SERT) and neuronal nitric oxide synthase (nNOS) in the dorsal raphe nucleus (DRN). By disrupting this interaction, ZZL-7 demonstrates significant potential in alleviating symptoms associated with major depressive disorder (MDD). Its ability to effectively cross the blood-brain barrier makes it a valuable tool for neuroscience research focused on the mechanisms underlying depression and the development of novel therapeutic strategies.
  35. Serotonin Reuptake Inhibitor

    (S)-Fluoxetine hydrochloride is a selective serotonin reuptake inhibitor (SSRI) primarily utilized in the treatment of major depressive disorder and anxiety disorders. By increasing serotonin levels in the brain, it enhances mood and alleviates symptoms of depression. This compound is frequently employed in pharmacological studies related to depression, anxiety, and other mood disorders, making it valuable for researchers exploring therapeutic interventions in neuropsychology.
  36. NET/SERT Inhibitor

    Desmethyl Sibutramine hydrochloride is a potent norepinephrine transporter (NET) and serotonin transporter (SERT) inhibitor. As a secondary metabolite of Sibutramine, it plays a significant role in modulating neurotransmitter levels associated with appetite regulation. This compound is utilized in research focused on obesity and the development of appetite suppressant therapies.
  37. NET/SERT Inhibitor

    Ampreloxetine hydrochloride is an orally active inhibitor of the norepinephrine transporter (NET) and serotonin transporter (SERT), with no activity against the dopamine transporter (DAT). It shows binding affinities with EC50 values of 11.7 ng/mL for NET and 50.8 ng/mL for SERT in plasma. This compound is utilized in research related to mood disorders and anxiety, offering insights into the modulation of norepinephrine and serotonin levels within the central nervous system.
  38. Serotonin Reuptake Inhibitor

    (R)-Fluoxetine hydrochloride is a selective serotonin reuptake inhibitor (SSRI) primarily targeting the serotonin transporter. This compound demonstrates a modest affinity for the 5-HT2A and 5-HT2C receptors, contributing to its pharmacological profile. It is widely utilized in research related to depression, anxiety disorders, and other serotonin-related dysfunctions.
  39. Serotonin Transporter Inhibitor

    Dapoxetine-d7 hydrochloride is a deuterium-labeled derivative of Dapoxetine hydrochloride, specifically targeting the serotonin transporter. This compound acts as a selective serotonin reuptake inhibitor (SSRI) with a short duration of action. Dapoxetine-d7 hydrochloride is employed in pharmacokinetic studies, providing insights into the metabolism and distribution of SSRIs in biological systems.
  40. Methylphenidate Analogue

    rel-HDMP 28 hydrochloride is a methylphenidate analogue that selectively targets the serotonin transporter (SERT), exhibiting an inhibition constant (Ki) of 105 nM. This compound demonstrates potential in research applications focused on modulating serotonergic activity and understanding its implications in neuropsychiatric disorders. Its selective binding profile makes it a valuable tool for pharmacological studies related to serotonin reuptake inhibition.
  41. SERT Enhancer

    Adoxosidic acid acts as a serotonin transporter (SERT) enhancer, contributing to the modulation of serotonin levels in the brain. Derived from the plant N. jatamansi, it is utilized in antidepressant research to explore its potential therapeutic effects on mood disorders. This compound serves as a valuable tool for investigating the mechanisms underlying serotonin reuptake and its implications in depression treatment.
  42. NET/SERT Inhibitor

    Desmethyl Sibutramine is an orally active inhibitor of the norepinephrine transporter (NET) and serotonin transporter (SERT). This compound demonstrates significant biological activity in modulating neurotransmitter levels, making it a valuable tool in obesity research and the study of appetite suppression mechanisms. Its metabolic profile and pharmacological effects contribute to its utility in understanding weight management therapies.
  43. Serotonin Transporter Inhibitor

    Wy-45494 hydrochloride is a potent serotonin transporter inhibitor deriving from the selective norepinephrine and serotonin reuptake inhibitor venlafaxine, primarily formed via cytochrome P450 CYP3A4 metabolism. This compound demonstrates significant biological activity by inhibiting norepinephrine and serotonin reuptake, with IC50 values of 4.7 μM and 1.6 μM, respectively, in rat synaptosomal preparations. In animal studies, it effectively reverses reserpine-induced hypothermia in mice, establishing its potential utility in research related to mood disorders and neurotransmitter regulation.
  44. Serotonin-norepinephrine Reuptake Inhibitor

    Ansofaxine is a serotonin-norepinephrine reuptake inhibitor (SNRI) that plays a critical role in investigating the pathophysiology of depression and related mood disorders. By modulating the levels of serotonin and norepinephrine in the synaptic cleft, Ansofaxine enhancing neurotransmitter availability and activity. This compound is valuable for research applications focused on the mechanisms of action of SNRIs in the treatment of depression and for exploring new therapeutic strategies.
  45. SSRI Inhibitor

    Paroxetine maleate is a selective serotonin reuptake inhibitor (SSRI) that primarily targets the serotonin transporter (SERT). It exhibits significant efficacy in modulating serotonergic activity, making it valuable in the study of mood and anxiety disorders. Paroxetine maleate is commonly utilized in research related to generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, and chronic headache conditions.
  46. Antidepressant

    Oxaflozane is a non-tricyclic antidepressant that primarily targets serotonin receptors. It exhibits anti-cataleptic and anti-aggressive properties while also demonstrating a mild potentiation of amphetamine-induced stereotypic behaviors. This compound is useful for research on serotonin modulation and its implications in mood disorders.
  47. Antidepressant Agent

    (S)-Alaproclate hydrochloride is a selective serotonin reuptake inhibitor (SSRI) with significant antidepressant properties. It exhibits a potent blockade of N-methyl-D-aspartate (NMDA) receptor currents in hippocampal neurons, with an IC50 value of 1.1 μM, and effectively inhibits K+ currents. This compound is valuable for research exploring mechanisms of depression and neuronal signaling pathways.
  48. Serotonin Transporter Inhibitor

    (R)-Duloxetine hydrochloride is a selective serotonin transporter inhibitor primarily used in pharmacological studies. It demonstrates significant binding affinity and is of interest in investigations related to serotonin reuptake mechanisms. Unlike its enantiomer (S)-Duloxetine, (R)-Duloxetine has limited effectiveness as a dual reuptake inhibitor for serotonin and norepinephrine, making it a valuable compound for research on monoaminergic neurotransmission and related disorders.
  49. NE Reuptake Inhibitor

    Tampramine fumarate is a potent and selective noncompetitive inhibitor of norepinephrine (NE) reuptake. This compound exhibits significant antidepressant activity, making it a valuable tool for studying depression and its related mechanisms. Researchers can utilize Tampramine fumarate to investigate the role of NE reuptake inhibition in neuropharmacology and the development of antidepressant therapies.
  50. Serotonin Transporter Inhibitor

    Nitroxazepine hydrochloride is a potent serotonin transporter inhibitor functioning as a tricyclic antidepressant (TCA). It enhances serotonergic and noradrenergic neurotransmission by inhibiting the reuptake of serotonin and norepinephrine, making it a valuable compound for research into the mechanisms of depression and related mood disorders. Its role in modulating serotonin levels also provides insights into the pharmacological treatment options for various psychiatric conditions.

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