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Catalog No.
Product Name
Application
Product Information
Citations
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SGLT2 Inhibitor
Luseogliflozin hydrate is a selective and potent second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor, exhibiting an IC50 value of 2.26 nM. This compound is primarily utilized in research focused on type 2 diabetes mellitus (T2DM), where its ability to inhibit SGLT2 facilitates the reduction of glucose reabsorption in the kidneys, thereby lowering blood glucose levels. -
SGLT-2 Inhibitor
Rongliflozin is a selective and orally active inhibitor of sodium-glucose co-transporter-2 (SGLT-2), which plays a crucial role in glucose reabsorption in the kidneys. This compound exhibits significant biological activity in the regulation of glucose metabolism and has potential applications in the treatment of type 2 diabetes mellitus (T2DM). Research with Rongliflozin can further elucidate its therapeutic effects and mechanisms of action in managing glycemic control. -
SGLT Inhibitor
rel-Licogliflozin is a sodium glucose cotransporter (SGLT) inhibitor, specifically targeting SGLT1 and SGLT2. This compound demonstrates significant biological activity in glucose transport modulation, making it valuable for research into diabetes and other metabolic disorders. Its role in disrupting glucose reabsorption in the kidneys has potential applications in developing therapeutic strategies for hyperglycemia management. -
SGLT-2 Inhibitor
Atigliflozin is a selective sodium-glucose cotransporter 2 (SGLT-2) inhibitor, displaying IC50 values of 10 nM for hSGLT-2 and 8.2 μM for hSGLT-1. This compound is effective in lowering blood glucose levels and enhancing impaired oral glucose tolerance. Atigliflozin is utilized in research related to type II diabetes mellitus, contributing to the understanding of glucose regulation and potential therapeutic interventions. -
SGLT Inhibitor
Velagliflozin proline is an oral sodium-glucose cotransporter 2 (SGLT2) inhibitor that exhibits significant antidiabetic activity. This compound effectively reduces renal glucose reabsorption, leading to increased glycosuria, which in turn lowers blood glucose and insulin levels. Velagliflozin proline is primarily utilized in research focused on diabetes management and related metabolic disorders. -
SGLT Inhibitor
SGLT1/2-IN-2 is a potent dual inhibitor targeting sodium-glucose co-transporters 1 and 2 (SGLT1 and SGLT2), with IC50 values of 96 nM and 1.3 nM, respectively. This compound effectively regulates glucose absorption and reabsorption in the kidneys, making it a valuable tool in diabetes research. Its dual inhibitory action offers significant potential in studying glucose homeostasis and developing therapies for metabolic disorders. -
SGLT1/2 Inhibitor
SGLT1/2-IN-8 is a potent dual inhibitor of SGLT1 and SGLT2, exhibiting IC50 values of 4 nM and 1 nM, respectively. This compound demonstrates significant anti-hyperglycemic effects, making it a valuable tool for research in diabetes and glucose regulation. Its oral bioavailability supports its potential in in vivo studies aimed at exploring metabolic disorders. -
SGLT2 Inhibitor
BI-44847 is a selective and orally active inhibitor of the sodium-glucose cotransporter 2 (SGLT2), primarily targeting glucose reabsorption in the kidneys. This compound is known to enhance urinary glucose excretion (UGE) and reduce HbA1c levels, thus improving both fasting and postprandial glucose levels. BI-44847 is valuable for research applications focused on understanding and treating type 2 diabetes mellitus (T2DM). -
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. -
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. -
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. -
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 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. -
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. -
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. -
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. -
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. -
NaV1.6/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. -
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. -
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. -
NaV1.7 Inhibitor
GX-201 is a selective inhibitor of the voltage-gated sodium channel NaV1.7, exhibiting an IC50 of less than 3.2 nM for the human NaV1.7 isoform. This compound has demonstrated effectiveness in modulating pain pathways and is valuable for research into pain management, neuropathic pain disorders, and related therapeutic applications. Its high potency and specificity make it a suitable tool for investigating sodium channel-related biological processes. -
Nav1.8 Channel Inhibitor
Nav1.8-IN-4 is a potent inhibitor of the Nav1.8 ion channel, demonstrating an IC50 of 0.014 μM. This compound is valuable for studies investigating pain-related disorders, offering insights into the modulation of nociceptive pathways. Its application in research may contribute to the development of novel therapeutic strategies targeting chronic pain mechanisms. -
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. -
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. -
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. -
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. -
Nav1.8 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. -
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. -
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. -
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. -
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.
