Catalog No.
Product Name
Application
Product Information
Citations
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SGLT Inhibitor
YM-543 is a selective inhibitor of the sodium-glucose cotransporter 2 (SGLT2), designed to reduce hyperglycemia in type 2 diabetes models. It exhibits potent inhibition of both human and mouse SGLT2 activities at nanomolar concentrations, ultimately increasing urinary glucose excretion and improving glucose tolerance. When administered orally, YM-543 maintains its therapeutic effects for over 12 hours and enhances the action of other antidiabetic agents, such as rosiglitazone or metformin, without affecting blood glucose levels in non-diabetic models. This specificity underscores its potential utility in diabetic research and therapeutic strategies. -
SGLT1/2 Inhibitor
SAR-7226 is a dual inhibitor of sodium-glucose co-transporters SGLT1 and SGLT2. It demonstrates significant biological activity in reducing glucose reabsorption in the kidneys and intestines, making it a valuable tool for studying the mechanisms underlying type 2 diabetes. This compound is useful for research aimed at understanding the pharmacological modulation of glucose homeostasis and developing therapeutic strategies for managing diabetes and related metabolic disorders. -
SGLT1 Inhibitor
Mizagliflozin (sebacate) is a selective inhibitor of sodium-glucose cotransporter 1 (SGLT1), demonstrating significant potential in enhancing vascular cognitive impairment associated with small vessel disease. By inhibiting SGLT1 activity in neurons, Mizagliflozin (sebacate) effectively improves cerebral blood flow and cognitive functions such as spatial learning and memory in relevant mouse models. Additionally, Mizagliflozin (sebacate) has been shown to increase the survival rate of IL-1β-treated PC12HS cells, supporting its role in neuroprotection. This compound is valuable for research into therapeutic strategies for cognitive deficits linked to vascular health. -
Stable Isotope
Pragliflozin-13C6 is a stable isotope-labeled form of Ipragliflozin, a selective sodium-glucose cotransporter 2 (SGLT2) inhibitor. This compound demonstrates inhibitory activity with IC50 values of 7.38 nM for human SGLT2 and significantly higher values for SGLT1, making it a potent antidiabetic agent. Pragliflozin-13C6 is primarily utilized in pharmacokinetic studies and metabolic experiments to trace the pathways and mechanisms of Ipragliflozin in biological systems. -
SGLT2 Inhibitor
Velagliflozin proline hydrate is an oral sodium-glucose cotransporter 2 (SGLT2) inhibitor that exhibits significant antidiabetic activity. By diminishing renal glucose reabsorption, Velagliflozin promotes glycosuria, effectively lowering blood glucose levels and insulin concentrations. This compound is primarily utilized in research focused on diabetes management and metabolic disorders. -
SGLT1/2 Inhibitor
Janagliflozin is a selective inhibitor of sodium-glucose cotransporter 2 (SGLT2), exhibiting an IC50 of 0.0058 μM for SGLT2 and 4.802 μM for SGLT1. This compound functions primarily in the proximal renal tubules to inhibit glucose reabsorption, thereby enhancing urinary glucose excretion and lowering blood glucose levels. Janagliflozin holds potential for research applications targeting type 2 diabetes mellitus. -
SGLT2 Inhibitor
TA-1887 is a highly potent and selective SGLT2 inhibitor, exhibiting an IC50 of 1.4 nM. This compound demonstrates significant antihyperglycemic effects, making it valuable in the study of diabetes and glucose metabolism. Researchers can utilize TA-1887 to investigate the therapeutic potential and mechanisms of SGLT2 inhibition in metabolic disorders. -
SGLT2 Inhibitor
Dapagliflozin methyl acetate is a potent SGLT2 inhibitor, primarily targeting sodium-glucose co-transporter 2. It plays a crucial role in regulating glucose reabsorption in the kidneys, which is significant for managing blood glucose levels. This compound is commonly utilized in research related to type 2 diabetes and metabolic disorders, facilitating investigations into the pharmacological effects and potential therapeutic applications of SGLT2 inhibition. -
SGLT2 Inhibitor
YM543 free base is a potent, orally active inhibitor of the sodium-glucose cotransporter 2 (SGLT2). This compound effectively lowers blood glucose levels, making it a valuable tool in diabetes research. Its mechanism of action provides insights into glucose homeostasis and offers potential therapeutic strategies for managing diabetic conditions. -
Stable Isotope
Ertugliflozin-d5 is a deuterium-labeled form of Ertugliflozin, a selective and potent inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2). With an IC50 of 0.877 nM against human SGLT2, it effectively reduces glucose reabsorption in the kidneys, making it relevant in research aimed at understanding type 2 diabetes mellitus treatment mechanisms. This stable isotope-labeled reagent is valuable for pharmacokinetic studies and metabolic tracing in biological systems. -
Stable Isotope
Remogliflozin etabonate-d7 is the deuterium-labeled variant of Remogliflozin etabonate, a selective sodium glucose cotransporter 2 (SGLT2) inhibitor. With Ki values of 1.95 μM for hSGLT2 and 2.14 μM for rSGLT2, it demonstrates notable inhibition of glucose reabsorption in renal tissues. Remogliflozin etabonate is metabolized to its active form within the body, contributing to its antidiabetic effects observed in rodent models. This stable isotope-labeled compound is valuable for pharmacokinetic studies and metabolic research involving SGLT2 inhibition. -
SGLT1 Inhibitor
TP0438836 is a selective inhibitor of the sodium-glucose cotransporter 1 (SGLT1), demonstrating an IC50 value of 28 nM for human SGLT1 and 7 nM for human SGLT2. This compound is of significant interest in diabetes research, as it may help elucidate the role of glucose absorption in glucose homeostasis and insulin regulation. TP0438836 can be utilized in studies aimed at developing therapeutic strategies for managing diabetes and related metabolic disorders. -
SGLT Inhibitor
Sergliflozin-A is a selective inhibitor of sodium-glucose co-transporter proteins SGLT1 and SGLT2, which play key roles in glucose reabsorption in the kidney. By competitively inhibiting these transporters, Sergliflozin-A contributes to reduced glucose reabsorption, making it a valuable compound in the study and treatment of type 2 diabetes. Its efficacy may vary with different mutations in target sites, underscoring its potential for tailored therapeutic applications in metabolic disorders. -
SGLT2 Inhibitor
Galacto-Dapagliflozin is a selective inhibitor of the human sodium-glucose cotransporter 2 (hSGLT2), exhibiting a Ki value of 25 nM. This compound demonstrates significant potential in modulating glucose homeostasis and promoting renal glucose excretion. Its application extends to research in metabolic disorders, particularly in the study of type 2 diabetes and related glucose regulation mechanisms. -
SGLT2 Inhibitor
Fluoro-Dapagliflozin is a selective sodium-glucose cotransporter 2 (SGLT2) inhibitor, exhibiting a Ki value of 5.3 nM for SGLT2 and 330 nM for SGLT1. It functions by blocking glucose transport, thereby reducing glucose absorption in the kidneys. This compound is valuable for research applications aimed at understanding glucose homeostasis, diabetic metabolism, and the therapeutic potential in managing type 2 diabetes. -
Sodium Channel Blocker, NaV1.8 Inhibitor
Suzetrigine is a selective inhibitor of the sodium channel NaV1.8, functioning as a sodium channel blocker. This compound exhibits significant analgesic properties, making it a valuable tool for pain research. It is particularly promising for studying acute pain management following surgical procedures such as abdominoplasty and bunionectomy. -
SCN8A Blocker
Zandatrigine is a selective inhibitor of the voltage-gated sodium channel NaV1.6 (SCN8A), exhibiting potent activity at the blood-brain barrier. By non-covalently binding to the VSD4 region of NaV1.6, Zandatrigine effectively blocks sodium influx, thereby mitigating persistent currents associated with pathological conditions. This compound has demonstrated a significant ability to reduce neuronal hyperexcitability and decrease the frequency of epileptic seizures. With 134-756-fold selectivity over other sodium channel isoforms such as NaV1.1 and NaV1.2, Zandatrigine serves as a valuable tool in research focused on SCN8A-related developmental epileptic encephalopathy (SCN8A-DEE) and adult focal epilepsy. -
Nav1.7 Inhibitor
PF-04856264 is a selective inhibitor of the Nav1.7 sodium channel, exhibiting IC50 values of 28 nM for human, 131 nM for mouse, 19 nM for cynomolgus monkey, and 42 nM for dog Nav1.7. It displays limited activity against rat Nav1.7, highlighting its specificity. PF-04856264 is primarily utilized in research focused on pain pathways and has demonstrated notable analgesic effects, making it a valuable tool for investigating pain-related mechanisms and potential therapeutic applications. -
Sodium Channel Blocker
QX-314 bromide is a membrane-impermeable sodium channel blocker that exerts its effects by binding to the intracellular side of sodium channels, effectively inhibiting neuronal activation. Its permanent positive charge prevents diffusion across cellular membranes, making it useful for investigating the role of sodium channels in physiological and pathological states. QX-314 bromide is commonly utilized in pain research, neurobiology, and studies of excitability in various cell types. -
NaV1.7 Blocker
PF-06456384 trihydrochloride is a highly potent and selective blocker of the NaV1.7 sodium channel, exhibiting an IC50 value of 0.01 nM for human NaV1.7, 75 nM for rat NaV1.7, and less than 0.1 nM for mouse NaV1.7. This compound is instrumental in researching pain pathways and the physiological role of NaV1.7 in nociception. Notably, PF-06456384 trihydrochloride has shown minimal analgesic efficacy in animal models such as the mouse Formalin pain model, highlighting its specificity in sodium channel modulation. -
Sodium Channel Inhibitor
Dibucaine hydrochloride is a sodium channel inhibitor that effectively blocks the influx of sodium ions, thereby preventing the propagation of action potentials in excitable tissues. This compound exhibits potent activity as an anesthetic and is utilized in various research applications, including studies of nerve conduction and muscle excitability. Additionally, it serves as a significant inhibitor of serum cholinesterase, contributing to its utility in pharmacological investigations and the development of anesthetic protocols. -
NaV1.8 Inhibitor
LTGO-33 is a potent and selective inhibitor of the voltage-gated sodium channel NaV1.8. With nanomolar potency and over 600-fold selectivity against human NaV1.1-NaV1.7 and NaV1.9 channels, LTGO-33 demonstrates state-independent inhibition across closed and inactivated conformations. It effectively reduces TTX-resistant NaV1.8 currents in non-human primate and human dorsal root ganglion neurons, leading to decreased action potential firing. LTGO-33 is a valuable tool for research into pain disorders and related mechanisms. -
Sodium Channel Modulator
Suzetrigine phenol is a sodium channel modulator that acts by selectively altering the gating of sodium channels. This compound exhibits significant biological activity related to the modulation of neuronal excitability and has potential applications in the study of pain pathways and neuroprotection. Research utilizing Suzetrigine phenol can aid in understanding sodium channel function and developing therapeutic strategies for neurological disorders. -
ENaC Activator
S3969 is a potent and reversible activator of the human epithelial sodium channel (hENaC). With an apparent EC50 of 1.2 μM, S3969 enhances sodium transport across epithelial tissues. This compound serves as a valuable tool for investigating cellular mechanisms related to sodium homeostasis and may be applied in studies of conditions such as hypertension and edema. -
Nav1.7 Inhibitor
TC-N 1752 is a selective inhibitor of the voltage-gated sodium channel Nav1.7, exhibiting potent activity with an IC50 of 0.17 μM. It also demonstrates inhibitory effects on other sodium channels, including hNav1.3, hNav1.4, hNav1.5, and rNav1.8. This compound has been shown to provide analgesic effects in the Formalin model of pain, making it a valuable tool for research in pain mechanisms and related therapies. -
Nav1.1 Activator
Nav1.1 activator 1 is a potent activator of the Nav1.1 sodium channel, effectively enhancing the decay time constant (tau) of Nav1.1 currents at a concentration of 0.03 μM. This compound demonstrates significant selectivity for Nav1.1 over other sodium channels, including Nav1.2, Nav1.5, and Nav1.6, facilitating targeted research. Its ability to penetrate the blood-brain barrier makes it a valuable tool for studying neurological function and related therapeutic applications. -
Sodium Current Inhibitor
Relutrigine is an orally active sodium current inhibitor that specifically targets persistent sodium channels. It demonstrates potent inhibition of persistent INa induced by both ATX-II (Nav 1.5 activator) and the SCN8A mutation N1768D, with IC50 values of 141 nM and 75 nM, respectively. In addition to exhibiting a strong use-dependent block, Relutrigine effectively reduces intrinsic neuronal excitability and possesses significant anticonvulsant properties, making it valuable for research in neuropharmacology and epilepsy studies. -
Sodium Channel Activator
Bifenthrin is a synthetic pyrethroid insecticide that acts as a sodium channel activator, specifically targeting Nav1.8 sodium channels. By prolonging the opening time of these channels, Bifenthrin induces membrane depolarization and disrupts neural function in insects. It exhibits potent insecticidal activity with reported lethal doses (LD50) of 0.15 ng/mg against Aedes gambiae and 0.16 ng/mg against Culex quinquefasciatus, making it an effective agent for control of both susceptible and resistant mosquito populations. Its efficacy in inhibiting blood-sucking behavior presents potential applications in developing mosquito-repellent materials. -
NaV1.7 Inhibitor
GDC-0276 is a selective and reversible inhibitor of the NaV1.7 ion channel with an IC50 value of 0.4 nM. This orally active compound demonstrates favorable pharmacokinetic properties and is well tolerated, making it a promising candidate for pain management. GDC-0276 may offer an alternative to existing analgesics, addressing issues such as addiction and off-target side effects in the treatment of various pain disorders. -
Potassium Channel Inhibitor
RY785 is a potent and selective inhibitor of voltage-gated potassium channels, specifically targeting KV2.2 with an IC50 of 0.05 μM. This compound exhibits notable analgesic activity, making it valuable for research into pain management and related therapeutic applications. Its specificity towards KV2 channels allows for exploration of their role in various physiological and pathological processes. -
Sodium Channel Blocker
A-887826 is a selective voltage-dependent sodium channel blocker targeting Na(v)1.8, exhibiting a potent IC50 of 11 nM. This compound has demonstrated efficacy in attenuating neuropathic tactile allodynia in vivo, making it a valuable tool for researching pain mechanisms and potential therapeutic interventions for neuropathic pain conditions. Its oral bioavailability further supports its utility in preclinical studies. -
Nav1.7 Inhibitor
GDC-0310 is a selective inhibitor of the Voltage-gated sodium channel Nav1.7, demonstrating a potent inhibitory activity with an IC50 of 0.6 nM against hNav1.7. This compound is primarily utilized in research exploring pain mechanisms, particularly in the context of chronic pain and neuropathic pain models. Its specificity makes it a valuable tool for investigating Nav1.7's role in various physiological and pathophysiological processes. -
NaV1.8 Inhibitor
VX-150 is a highly selective inhibitor of the sodium channel NaV1.8. This compound demonstrates significant analgesic properties and shows potential for research in various pain-related indications. Its oral bioavailability makes it a valuable tool for studies investigating pain mechanisms and the development of novel pain therapies. -
Nav1.1 Activator
Lu AE98134 is a selective activator of voltage-gated sodium channel Nav1.1, functioning as a positive modulator. It also enhances the activity of Nav1.2 and Nav1.5 channels, while exhibiting no effect on Nav1.4, Nav1.6, or Nav1.7 channels. This compound serves as a valuable tool for investigating the pathophysiological roles of Nav1.1 in various central nervous system disorders, including potential applications in cognitive improvement in schizophrenia. -
NaV1.6/NaV1.2 Inhibitor
XPC-5462 is a selective inhibitor of the voltage-gated sodium channels NaV1.6 and NaV1.2, exhibiting IC50 values of 10.9 nM and 10.3 nM, respectively. It effectively suppresses epileptiform activity in ex vivo brain slice seizure models, making it a valuable tool for research in epilepsy and related neurological disorders. Its ability to modulate excitability in neuronal populations highlights its potential for studying sodium channel dynamics and their role in neuronal excitability. -
Sodium Channel Inhibitor
RY796 is a selective sodium channel inhibitor targeting voltage-gated sodium channels. Its potent activity has demonstrated analgesic effects, making it relevant for pain research. This compound can be utilized in studies investigating the modulation of sodium channels in various physiological and pathological conditions. -
Nav1.8 Inhibitor
Sodium Channel Inhibitor 6 is a selective Nav1.8 inhibitor primarily targeting voltage-gated sodium channels associated with neuronal excitability. It demonstrates significant biological activity in modulating pain pathways, making it a valuable tool for research on neuropathic pain mechanisms. This compound is suitable for in vitro and in vivo studies aimed at understanding the role of Nav1.8 in pain signaling and potential therapeutic interventions. -
ENaC Inhibitor
Phenamil methanesulfonate is a potent inhibitor of the epithelial sodium channel (ENaC), exhibiting an IC50 of 400 nM. In addition, it competitively inhibits TRPP3, with an IC50 of 140 nM, thereby blocking TRPP3-mediated calcium transport. This compound has potential applications in promoting bone repair by strongly activating the BMP signaling pathway and is valuable in research related to cystic fibrosis lung disease. -
Nerve Conduction Blocker
Butacaine is a reversible nerve conduction blocker that primarily targets voltage-gated sodium channels to inhibit nerve impulses, resulting in sensory and motor paralysis. This compound is commonly utilized in research as a negative control for local anesthetics. Butacaine is known to form inclusion complexes with α-cyclodextrin and β-cyclodextrin, enhancing its solubility and stability in biological applications. Its properties make it valuable for studying mechanisms of local anesthesia and nerve conduction. -
NaV1.8 Inhibitor
PF-04885614 is a potent inhibitor of the sodium channel NaV1.8, primarily involved in pain signaling pathways. Its inhibition may provide therapeutic benefits for managing neurological and neurodevelopmental disorders. This compound is valuable for research applications focused on pain mechanisms and the development of analgesic therapies. -
Pyrethroid Insecticide
S-Bioallethrin, a pyrethroid insecticide, primarily targets voltage-gated sodium channels, disrupting nerve function by altering the gating kinetics between conducting and nonconducting states. This compound exhibits significant biological activities, including the inhibition of lymphocyte proliferation and the induction of histamine release from human basophils. S-Bioallethrin is commonly utilized in studies investigating insecticidal mechanisms and the effects of neurotoxic compounds on immune responses. -
Insecticide
(±)-Indoxacarb is a broad-spectrum oxadiazine insecticide that exerts its effects by blocking sodium channels in insect nerve preparations and isolated neurons. This mechanism results in significant insecticidal activity while maintaining low toxicity to mammals. It is primarily utilized in research applications focusing on pest control and insect physiology. -
Antiarrhythmic Agent
Mexiletine is an orally active antiarrhythmic agent that primarily targets sodium channels to exert its effects, with IC50 values of 75±8 μM for tonic block and 23.6±2.8 μM for use-dependent block. In addition to its antiarrhythmic properties, Mexiletine has demonstrated efficacy in treating myotonia and neuropathic pain. This compound is valuable for research applications in both cardiovascular and neurological studies, providing insights into channelopathies and pain mechanisms. -
Sodium Channel Blocker
Licarbazepine is a voltage-gated sodium channel blocker that demonstrates anticonvulsant and mood-stabilizing properties. Its mechanism of action involves inhibiting sodium influx, which leads to a reduction in neuronal excitability. This compound is primarily utilized in research related to epilepsy and mood disorders, providing a valuable tool for investigating potential therapeutic interventions. -
Pyrethroid
Cyfluthrin is a type II pyrethroid that primarily targets Nav1.8 sodium channels, leading to prolonged stimulation of neuronal activity in insects. This compound exhibits potent insecticidal activity against a variety of pest species, making it suitable for applications in agriculture and veterinary practices, as well as in stored product protection. Its efficacy as an insecticide is attributed to its ability to disrupt normal neural function in target organisms. -
CRMP2-Ubc9 Interaction/NaV1.7 Inhibitor
AZ194 is a novel, orally active inhibitor that targets the interaction between CRMP2 and Ubc9, functioning as a specific inhibitor of NaV1.7 with an IC50 of 1.2 μM. By blocking the SUMOylation process of CRMP2, AZ194 effectively reduces the surface expression of NaV1.7, demonstrating significant antinociceptive properties. This agent is useful for research in pain modulation and associated neurological studies. -
Sodium Channel Inhibitor
3'-Methoxydaidzein is an isoflavone acting as a sodium channel inhibitor. It selectively inhibits sodium channel subtypes NaV1.7, NaV1.8, and NaV1.3 with IC50 values of 181 nM, 397 nM, and 505 nM, respectively. This compound exhibits significant analgesic activity through its modulation of voltage-gated sodium channels, making it a valuable tool for research in pain pathways and related therapeutic applications. -
Sodium Channels Inhibitor
Vormatrigine is an orally active inhibitor of sodium channels, demonstrating anti-epileptic properties. This compound is utilized in research to investigate human focal and generalized epilepsy, providing insights into its mechanisms and potential therapeutic applications. Its effectiveness in modulating sodium channel activity makes it a valuable tool for studying epilepsy-related pathophysiology. -
NaV1.7 Inhibitor
DS-1971a is a selective and orally bioavailable inhibitor of the voltage-gated sodium channel NaV1.7, with IC50 values of 22.8 nM and 59.4 nM for human and murine NaV1.7, respectively. This compound demonstrates significant analgesic properties, making it a valuable tool for research in pain management and neurological studies. Its specificity for NaV1.7 positions DS-1971a as an important reagent for exploring the mechanisms of pain signaling and potential therapeutic interventions. -
Sodium Channel Blocker
Evenamide is an orally available voltage-gated sodium channel blocker (Ki = 0.4 µM) primarily targeted for research in schizophrenia. It demonstrates efficacy across a variety of rodent models representing psychosis, mania, depression, and aggressive behavior. This compound serves as a valuable tool for investigating the underlying mechanisms of these psychiatric conditions and evaluating potential therapeutic interventions.
