Catalog No.
Product Name
Application
Product Information
Citations
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Antiarrhythmic Agent
Encainide is an antiarrhythmic agent classified as a class IC antiarrhythmic. It functions by blocking voltage-dependent potassium channels, thus modulating cardiac excitability. This compound shows promise in research focused on life-threatening ventricular arrhythmias, symptomatic ventricular arrhythmias, and supraventricular arrhythmias. Its role in these conditions makes it valuable for studies aimed at understanding and treating various cardiac arrhythmias. -
Sodium Channel Inhibitor
XPC-6444 is a highly potent and isoform-selective sodium channel inhibitor, specifically targeting NaV1.6 with an IC50 of 41 nM. It also exhibits significant inhibition of NaV1.2 with an IC50 of 125 nM. This compound demonstrates anticonvulsant activity, making it a valuable tool for research in neuropharmacology and the study of epilepsy-related mechanisms. -
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. -
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. -
AQP2/CFTR Inhibitor
Steviol is a selective inhibitor of the aquaporin-2 (AQP2) and cystic fibrosis transmembrane conductance regulator (CFTR) proteins. This compound impedes renal cyst growth by inhibiting CFTR activity, which leads to decreased AQP2 expression and promotes the degradation of both AQP2 and CFTR. Steviol is relevant for research focused on polycystic kidney disease and mechanisms underlying renal cyst development. -
EHD4 ATPase Inhibitor
ATPase-IN-4 is a selective inhibitor of EHD4 ATPase activity, with an IC50 value of 0.92 μM. This compound also exhibits inhibitory effects on the ATPase activity of EHD2. ATPase-IN-4 is valuable for research applications focused on understanding the role of EHD proteins in cellular processes and membrane trafficking. -
ATPase Inhibitor
ATPase-IN-2 is a potent ATPase inhibitor with an IC50 value of 0.9 μM. It effectively inhibits the glycohydrolase activity of Clostridium difficile toxin B (TcdB) with an AC50 value of 30.91 μM. This compound serves as a valuable tool for studying ATP-related mechanisms and elucidating the role of ATPases in various biological processes. -
CF1 ATPase Inhibitor
Ovothiol A disulfide is a specific inhibitor of CF1 ATPase, targeting its light-activated function. This compound has been shown to effectively inhibit ATP synthesis in photophosphorylation processes, making it a valuable tool for studying energy transduction in photosynthetic organisms. Its role in modulating ATPase activity provides insights into the regulation of bioenergetics and enzyme kinetics in various biological systems. -
Mitochondrial F0F1-ATPase Inhibitor
Isoapoptolidin is an inhibitor of the mitochondrial F0F1-ATPase, exhibiting a Ki greater than 100 μM and selective action towards mitochondrial complex V. This compound is valuable for investigating mitochondrial energy metabolism-related disorders, including cancer and neurodegenerative diseases. Its inhibitory properties facilitate studies on the role of ATP synthase in cellular energy regulation. -
Dual MDR1/BCRP Inhibitor
CP-100356 hydrochloride is a potent dual inhibitor of MDR1 (P-glycoprotein) and BCRP, featuring IC50 values of 0.5 µM and 1.5 µM for the inhibition of MDR1-mediated transport of Calcein-AM and BCRP-mediated transport of Prazosin, respectively. It also exhibits off-target activity as a weak inhibitor of OATP1B1 with an IC50 of approximately 66 µM, while showing no significant inhibition against MRP2 or major human P450 enzymes (IC50 > 15 µM). This compound is useful in studying drug transport dynamics and enhancing the bioavailability of therapeutic agents in pharmacological research. -
BCRP Inhibitor
Ac32Az19 is a selective inhibitor of Breast Cancer Resistance Protein (BCRP), demonstrating a potent inhibitory effect with an EC50 value of 13 nM in BCRP-overexpressing HEK293/R2 cells. This high affinity and nontoxic profile make Ac32Az19 a valuable tool for research applications focused on drug transport mechanisms and multidrug resistance in cancer studies. Its specificity for BCRP allows for detailed investigations into therapeutic strategies and the modulation of drug pharmacokinetics. -
ABCG2/BCRP Inhibitor
Efflux inhibitor-1 is a pyrazolo[1,5-a]pyrimidine compound that selectively inhibits the ABCG2/BCRP transporter. With IC50 values of 0.45 μM for ABCG2/BCRP and 2.17 μM for ABCB1, this inhibitor is a valuable tool for studying drug efflux mechanisms and multidrug resistance. It is useful in research applications focused on cancer pharmacology and the modulation of drug absorption and resistance pathways. -
BCRP Inhibitor
ML753286 is a selective inhibitor of the Breast Cancer Resistance Protein (BCRP), exhibiting an IC50 of 0.6 μM. This compound demonstrates high permeability and moderate clearance in liver S9 fractions from both rodent and human sources. Additionally, ML753286 remains stable across species in plasma, making it a valuable tool for studies investigating drug resistance mechanisms and pharmacokinetics in cancer research. -
BCRP Inhibitor
Ac22(Az8)2 is a selective inhibitor of the Breast Cancer Resistance Protein (BCRP), exhibiting an EC50 value of 1-2 nM. This compound effectively restores drug sensitivity in BCRP-overexpressing cells by inhibiting BCRP-ATPase activity, thereby blocking drug efflux and enhancing intracellular drug accumulation. Ac22(Az8)2 is a valuable tool for investigating BCRP-mediated mechanisms in multidrug-resistant cancers. -
BCRP Inhibitor
Pentamethoxymorin is a selective inhibitor of the breast cancer resistance protein (BCRP/ABCG2), demonstrating significant potency with IC50 values of 5.98 μM and 5.94 μM in the Hoechst 33342 and Pheophorbide A assays, respectively. This compound showcases a preference for BCRP over other efflux transporters such as P-glycoprotein and MRP1. Pentamethoxymorin is valuable for research focusing on cancer resistance mechanisms and potential therapeutic interventions in breast cancer. -
MDR1/BCRP Inhibitor
CP-100356 is a dual inhibitor of MDR1 (P-glycoprotein) and BCRP, exhibiting IC50 values of 0.5 µM and 1.5 µM, respectively, for the inhibition of MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport. Additionally, CP-100356 shows weak inhibition of the OATP1B1 transporter, with an IC50 of approximately 66 µM, while demonstrating minimal inhibition against MRP2 and major human P450 enzymes (IC50 > 15 µM). This compound is valuable for research applications targeting drug resistance mechanisms and transport protein interactions in pharmacology and toxicology studies. -
BCRP/ABCG2 Inhibitor
Butein tetramethyl ether is a selective inhibitor of the breast cancer resistance protein (BCRP/ABCG2) that demonstrates potent biological activity. It has been shown to inhibit BCRP in MCF-7 MX and MDCK cell lines, with IC50 values of 2.2 μM and 1.03 μM, respectively. This compound is a valuable tool for research investigating the mechanisms of cancer resistance and could provide insights into therapeutic strategies for overcoming drug resistance in cancer treatments. -
ABCG2 (BCRP) Inhibitor
UR-MB108 is a selective inhibitor of ABCG2 (BCRP) with an IC50 value of 79 nM. This compound demonstrates high potency in inhibiting the efflux activity of the ABCG2 transporter. UR-MB108's stability in blood plasma enhances its potential for various biological applications, including studies on drug absorption and resistance in cancer research. -
P-gp/BCRP Inhibitor
P-gp/BCRP-IN-1 is a potent inhibitor targeting P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP). This compound is designed to reverse drug resistance by inhibiting the efflux activities of these pivotal transporters. P-gp/BCRP-IN-1 enhances the oral bioavailability of chemotherapeutic agents, such as Paclitaxel (PTX), making it a valuable tool in cancer research and therapeutic development. Its efficacy and oral activity suggest a promising utility in overcoming drug resistance in various cancer models. -
BCRP
2,4-Dibromoestradiol primarily targets the ABCG2 transporter, a member of the ATP-binding cassette (ABC) family. This compound exhibits significant influence on the function of the breast cancer resistance protein (BCRP), which is pivotal in drug efflux and resistance mechanisms. It is utilized in research focused on drug transport, pharmacokinetics, and cancer biology. -
Substrate for BCRP
INCB-056868 is a metabolite of Epacadostat (M11) that acts as a substrate for the Breast Cancer Resistance Protein (BCRP). This compound is valuable for investigating the mechanisms underlying metabolic diseases and the transport processes mediated by BCRP. Its role in examining drug metabolism and resistance mechanisms makes it a significant reagent for biochemical research. -
BCRP Inhibitor
BCRP-IN-2 is a potent inhibitor of Breast Cancer Resistance Protein (BCRP), demonstrating enhanced inhibitory activity upon ultraviolet light activation. This compound serves as an effective probe for investigating the interactions of quinazolinamine derivatives with BCRP, facilitating ATP hydrolysis of the transport protein. BCRP-IN-2 significantly increases the accumulation of mitoxantrone in H460/MX20 cells, which exhibit BCRP overexpression, making it valuable for studies on multidrug resistance mechanisms in cancer research.
