Catalog No.
Product Name
Application
Product Information
Citations
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Sodium Channel Blocker
Taplucainium chloride is a sodium channel blocker that demonstrates 70-95% inhibition at a concentration of 10 μM. It exhibits significant analgesic properties, making it a valuable tool for pain research. This reagent can be utilized to investigate sodium channel function and its role in pain signaling pathways. -
Nav1.7 Inhibitor
PF-05186462 is a selective inhibitor of the human Nav1.7 voltage-dependent sodium channel, exhibiting an IC50 value of 21 nM. This compound demonstrates a high degree of selectivity for Nav1.7 over other sodium channels, including Nav 1.1, 1.2, 1.3, 1.4, 1.5, 1.6, and 1.8. PF-05186462 is ideally suited for research applications focused on acute and chronic pain mechanisms. -
Antitussive Agent
Benzonatate is a non-narcotic peripheral antitussive agent that acts primarily by inhibiting reversible voltage-gated sodium channels. This compound effectively reduces the activity of cough stretch receptors, leading to a suppression of the cough reflex. Benzonatate is commonly utilized in research focusing on respiratory pathways and the modulation of cough response. -
Nav1.1 Inhibitor
AA43279 is a selective inhibitor of the Nav1.1 sodium channel (SCN1A), with an EC50 of 9.5 μM. This compound modulates the activity of gamma-aminobutyric acid (GABA) fast-firing interneurons, enhancing neuronal firing in vitro. AA43279 demonstrates anticonvulsant properties in the rat MEST model, making it a valuable tool for research involving epilepsy and related neurological disorders. -
Sodium Channel Modulator
ATX-II is a selective sodium channel modulator toxin that enhances late sodium current by preventing complete sodium channel inactivation, leading to persistent current fractions. This compound exhibits pro-arrhythmic effects, characterized by a slowed intrinsic heart rate, prolonged QT interval, and extended sinus node recovery time, potentially resulting in sinus pauses and arrests. ATX-II is valuable for research related to atrial fibrillation, long QT syndrome, and long QT3 syndrome. -
Aconitum Alkaloid
6-Benzoylheteratisine acts as an antagonist of tetrodotoxin and targets sodium channels, demonstrating potential neuroprotective activity. It effectively inhibits the influx of sodium ([Na+]i) and calcium ([Ca2+]i) ions, as well as the release of glutamate, making it relevant for the study of excitatory neurotransmission. Additionally, 6-Benzoylheteratisine has shown inhibitory effects on neuronal activity associated with epileptiform burst discharge, suggesting its utility in neurological research and potential therapeutic applications in epilepsy. -
Nav1.7 Antagonist
GX-674 is a potent antagonist of the voltage-gated sodium channel Nav1.7, exhibiting state-dependent and isoform-selective inhibition with an IC50 of 0.1 nM at -40 mV. This compound is valuable for research focused on pain pathways and neuropathic pain mechanisms, providing insights into the role of Nav1.7 in nociception and related disorders. Its high specificity and potency make it an essential tool for studying the therapeutic potential in pain management. -
Noradrenaline Reuptake Inhibitor
Atomoxetine is a selective noradrenaline reuptake inhibitor primarily targeting norepinephrine transporters with Ki values of 5 nM. It is known to increase dopamine and norepinephrine extracellular levels in the prefrontal cortex, thereby enhancing catecholaminergic neurotransmission. Additionally, Atomoxetine acts as a sodium channel blocker (VGSCs). This compound is widely utilized in research focusing on attention-deficit hyperactivity disorder (ADHD) and related neuropharmacological studies. -
Nav1.7/ Nav1.8 Blocker
ABBV-318 is a potent blocker of the voltage-gated sodium channels Nav1.7 and Nav1.8, demonstrating IC50 values of 2.8 μM and 3.8 μM for hNav1.7 and hNav1.8, respectively. This compound is of significant interest in pain research, providing insights into mechanisms of pain signaling and potential therapeutic avenues for pain management. Its specificity for Nav1.7 and Nav1.8 makes it a valuable tool for elucidating neuronal function and designing targeted analgesic strategies. -
Sodium Channel Blocker
Bliretrigine is a potent sodium channel blocker, primarily targeting voltage-gated sodium channels to modulate neuronal excitability. It has demonstrated significant analgesic properties, making it effective in alleviating pain associated with various neurological conditions. This compound is valuable for research into pain mechanisms and the development of novel analgesic therapies. -
Antiarrhythmic Agent
Ethacizine hydrochloride is a Class Ic antiarrhythmic agent that primarily targets sodium channels to modulate cardiac conduction. This compound is recognized for its long-lasting effects compared to other agents in its class, making it valuable for the management of arrhythmias. Ethacizine hydrochloride is utilized in research applications focused on cardiac electrophysiology and the mechanism of arrhythmias, providing insights into therapeutic interventions for cardiac disorders. -
Nav1.8 Inhibitor
Nav1.8-IN-2 is a selective inhibitor of the voltage-gated sodium channel Nav1.8, exhibiting a potent IC50 value of 0.4 nM. This compound is utilized in research related to various pain disorders, cough disorders, and both acute and chronic itch conditions. Its high affinity for Nav1.8 makes it a valuable tool for elucidating pain signaling pathways and developing therapeutic strategies for sensory nerve modulation. -
Sodium Channel Blocker
Co 102862 is a potent, broad-spectrum sodium channel blocker with state-dependent activity. This compound exhibits significant anticonvulsant properties, making it valuable for research in epilepsy and other neurological disorders. Its oral bioactivity supports its use in in vivo studies aimed at exploring sodium channel modulation in various therapeutic contexts. -
Anesthetic Agent
Etidocaine hydrochloride is a long-acting aminoamide local anesthetic that primarily targets sodium channels to inhibit neuronal excitability. It is effective in suppressing or relieving pain during surgical procedures and other medical applications requiring localized anesthesia. Its prolonged duration of action makes it suitable for various clinical settings. -
Sodium Channel Blocker
Aneratrigine is a selective blocker of the sodium channel protein type 9 subunit alpha, primarily inhibiting its activity. This compound exhibits significant potential in the study of neuropathic pain disorders, making it a valuable tool for research into pain management and associated neurological conditions. Researchers can utilize Aneratrigine to explore mechanisms of sodium channel modulation and its effects on neuronal excitability. -
ENaC Inhibitor
ETD001 is a potent ENaC (epithelial sodium channel) inhibitor, demonstrating an IC50 of 57.5 nM in cultured human bronchial epithelial (HBE) cells. This compound is particularly valuable for research applications related to cystic fibrosis, as it modulates sodium transport and influences fluid secretion in airway epithelium. Its long-acting properties make it an important tool for investigating ENaC's role in pulmonary pathophysiology and potential therapeutic interventions. -
Voltage-gated Sodium Channel Blocker
Mexiletine-d6 hydrochloride is a deuterated analog of Mexiletine hydrochloride, acting primarily as a voltage-gated sodium channel blocker. This compound is classified as a Class IB antiarrhythmic agent and exhibits non-selective inhibition of sodium channels. It is valuable in research applications focused on cardiac rhythm management and the modulation of neuronal excitability. -
NaV1.8 Blocker
PF-06305591 dihydrate is a selective blocker of the voltage-gated sodium channel NaV1.8, exhibiting an IC50 of 15 nM. This compound demonstrates significant potential for neurophatic pain research due to its ability to modulate sodium ion flux and reduce excitability in sensory neurons. Its favorable preclinical in vitro ADME and safety profile make it a valuable tool for studying pain mechanisms and developing analgesic therapies. -
Nav1.7 Inhibitor
PF-05198007 is a selective inhibitor of the Nav1.7 sodium channel, demonstrating potent and orally active properties. This compound is utilized in research focused on pain signaling pathways, specifically in the exploration of pain relief mechanisms and the development of analgesic therapies. Its pharmacodynamic profile aligns closely with that of PF-05089771, making it a valuable tool for studying Nav1.7-related biological processes. -
NaV1.7 Antagonist
(Rac)-AMG8379 is a potent antagonist of the NaV1.7 sodium channel, demonstrating selective inhibition with IC50 values of 8.5 nM for human NaV1.7 and 18.6 nM for mouse NaV1.7. This compound is known for its oral bioavailability and serves as a valuable tool in research focused on pain pathways and sodium channel modulation. Investigations utilizing (Rac)-AMG8379 can advance understanding of the role of NaV1.7 in nociception and related disorders. -
R-enantiomer of Funapide
(R)-Funapide is the R-enantiomer of Funapide, targeting the sodium channels Nav1.7 and Nav1.8, among others, in the peripheral nervous system. This compound exhibits biological activity as a sodium channel inhibitor, which may have implications in pain modulation. Research applications for (R)-Funapide include studies on analgesic mechanisms and the exploration of peripheral nerve functions. -
Glucokinase Activator
Glucokinase activator 3 is a potent activator of glucokinase (GK) with an AC50 of 38 nM. This compound has demonstrated significant efficacy in reducing blood glucose levels in diet-induced obese (DIO) mice, highlighting its potential in type 2 diabetes research. Additionally, glucokinase activator 3 has been shown to inhibit the hERG channel and sodium channels in patch clamp assays, providing insight into its pharmacological profile. -
Analgesic Agent
(+)-Mepivacaine is an amide-type local anesthetic that exhibits potent analgesic and vasoconstrictive properties. By selectively binding to voltage-gated sodium channels on neuronal cell membranes, it effectively inhibits sodium influx, leading to a temporary loss of sensation in targeted areas. This compound is widely utilized in various research applications, particularly in studies focused on pain management and anesthesia. -
Antiarrhythmic Agent
(S)-Propafenone is an antiarrhythmic agent that functions primarily as a sodium channel blocker. This compound exhibits beta-blocking properties and demonstrates class 1 antiarrhythmic activity, making it valuable in the study of cardiac arrhythmias. Its efficacy in modulating myocardial excitability and conduction makes it an important tool for research applications aimed at understanding arrhythmic disorders and developing therapeutic strategies. -
Sodium Channel Blocker
Zilvetrigine is a sodium channel blocker that selectively inhibits voltage-gated sodium channels. This compound exhibits analgesic properties, making it valuable for pain management research. Its mechanism of action can be explored in studies related to neuropathic pain and other conditions mediated by sodium channel activity. -
Cardioactive Agent
DPI 201-106 is a cardiotonic agent that exerts its effects through a synergistic mechanism involving both sarcolemmal and intracellular pathways. It selectively modulates voltage-gated sodium channels (VGSCs), leading to a significant positive inotropic effect. This compound is useful for research applications focused on cardiac function and the modulation of ion channel activity in cardiac tissues. -
Sodium Channel Blocker
Tocainide hydrochloride is a sodium channel blocker that inhibits the activity of voltage-gated sodium channels, effectively reducing neuronal excitability in pain pathways. This compound is primarily used in research related to pain mechanisms and the treatment of conditions such as tinnitus. Tocainide hydrochloride functions as a primary amine analog of lidocaine, providing insights into sodium channel modulation and its therapeutic potential. -
Sodium Channel Inhibitor
Licarbazepine-d4 is a deuterated derivative of Licarbazepine, functioning as a sodium channel inhibitor. This compound exhibits anticonvulsant and mood-stabilizing properties, making it a valuable tool in the study of neurological disorders. It is particularly useful for researchers investigating the mechanisms of epilepsy and mood regulation. -
VGSC Blocker
KC 12291 hydrochloride is a potent blocker of voltage-gated sodium channels (VGSC). It effectively reduces sustained Na+ current amplitude, demonstrating notable anti-ischemic properties. This compound exhibits significant cardioprotective effects in both in vitro and in vivo studies, making it a valuable tool for cardiac research and the investigation of sodium channel-related pathophysiology. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
Histamine H1 Receptor Antagonist
Terfenadine N-oxide is a histamine H1 receptor antagonist with an IC50 value of 2.73 μM, also exhibiting inhibition of the hERG potassium channel with an IC50 of 0.698 μM. This compound is valuable for investigating histamine-related allergic diseases and the role of hERG channels in arrhythmias. Its dual activity makes it a useful tool for research in pharmacology and toxicology related to allergic responses and cardiac rhythm disturbances. -
Antispasmodic Agent
Terodiline is an antispasmodic agent that primarily targets the hERG potassium channel, exhibiting an IC50 of 375 nM. It possesses both anticholinergic and calcium antagonist properties, making it effective in reducing abnormal bladder contractions associated with detrusor instability. Terodiline is suitable for research applications focused on urinary incontinence. -
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. -
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. -
Biochemical Assay Reagent
Phlorizin dihydrate is a biochemical reagent that acts as a specific inhibitor of glucose transporters, primarily SGLT1 and SGLT2. Its key biological activity includes the inhibition of glucose reabsorption in the kidneys, making it valuable for studies in diabetes and renal physiology. Phlorizin dihydrate is commonly used in research applications involving glucose transport mechanisms and metabolic profiling. -
Proton Acceptor
2,6-Diphenylpyridine serves as a proton acceptor and a tridentate [C^N^C] dianionic ligand. This compound facilitates efficient proton transfer at the interface of two immiscible electrolyte solutions. Its ability to form mononuclear and binuclear complexes with gold(III) enhances its utility in studies of electrochemical ion transfer kinetics and organometallic chemistry. 2,6-Diphenylpyridine is valuable for research applications involving coordination chemistry and catalytic processes. -
Ca2+ Inducer
D-myo-Inositol-1,3,4,5-tetrakisphosphate potassium acts as a Ca2+ inducer by enhancing extracellular calcium entry via the upregulation of voltage-gated calcium channels. This compound is instrumental in studies related to calcium signaling pathways and is often utilized in investigations of cellular processes influenced by calcium ions. It serves as a valuable reagent for researchers exploring the roles of calcium in various physiological and pathological contexts. -
Active Small Molecule
17α-Hydroxydigitoxigenin is an active small molecule primarily known for its ability to inhibit Na+/K+-ATPase activity. This inhibition plays a crucial role in various physiological processes and has been linked to cardiac and neuroprotective effects. It is relevant for research applications involving ion transport, cellular signaling, and the study of cardiovascular diseases. -
Biochemical Assay Reagent
Digitoxigenin is a biochemical assay reagent primarily used for the study of cardiac glycosides. This compound exhibits significant biological activity, particularly in inhibiting Na+/K+ ATPase, which is crucial for cell membrane potential and ion transport. It is applied in research focusing on cardiac function, cellular signaling, and related pathways in various biological systems. -
Starting CompoundsFor The Synthesis of KV7.2/3 Openers
2,6-Dichloro-3-nitropyridine is a key starting compound in the synthesis of sulfide analogs of Flupirtine, which function as KV7.2/3 channel openers. This compound exhibits potential biological activity relevant to pain research, making it a valuable reagent for studies focused on the modulation of neuronal excitability and analgesic mechanisms. Its utility in the development of KV7.2/3 activators positions it as an important tool in therapeutic research. -
Oct4 Activator
Oct4 inducer-1 is a potent activator of the Oct4 transcription factor, significantly enhancing the expression of Oct4 and Nanog promoters. This compound promotes the formation of induced pluripotent stem cells (iPSCs) and improves the efficiency of cell reprogramming while reducing the overall reprogramming time. It is a valuable tool for research applications in stem cell biology and regenerative medicine. -
OCT4 Inducer
Oct4 inducer-2 is a compound that promotes the expression of endogenous OCT4, facilitating the maintenance and proliferation of human induced pluripotent stem cells (hiPSCs). This inducer is valuable for research applications focused on stem cell biology, regenerative medicine, and anti-aging studies. By enhancing OCT4 levels, Oct4 inducer-2 supports the maintenance of pluripotency, making it an essential tool for scientists investigating cellular reprogramming and differentiation. -
Stable Isotope
Digitoxigenin-21,23,23-d3 is a deuterium-labeled derivative of Digitoxigenin, serving as a stable isotope for research applications. This compound is primarily important for the synthesis of cardiac glycosides used in the treatment of heart failure and arrhythmias. By inhibiting the sodium-potassium ATPase pump, Digitoxigenin enhances cardiac contraction efficiency and force, making it a critical component in cardiovascular research and drug development. -
Stable Isotope
rac Felodipine-(Methoxy-d3) is a deuterium-labeled analog of rac Felodipine, a potent calcium channel blocker that primarily targets L-type calcium channels. This stable isotope variant is useful for pharmacokinetic studies, metabolic tracing, and isotopic labeling in drug development research. Its deuterium labeling enhances the analytical sensitivity and specificity in mass spectrometry applications, facilitating the investigation of drug absorption, distribution, metabolism, and excretion (ADME) profiles.
