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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
HCN1 Inhibitor
RO-275 is a potent and selective HCN1 inhibitor, demonstrating IC50 values of 0.046 µM for HCN1, while showing significantly lower activity against HCN2 (14.3 µM), HCN3 (4.6 µM), and HCN4 (13.9 µM). This compound has been shown to effectively rescue impaired working memory, highlighting its potential utility in researching cognitive dysfunction associated with various brain disorders. RO-275 serves as a valuable tool for investigations into HCN1-related pathways and their implications in neurobiology. -
HCN2 Inhibitor
HCN2-IN-3 is an orally active inhibitor of HCN2 ion channels. It effectively reduces the activity of HCN2, making it valuable for research into pain mechanisms, tinnitus, and various central nervous system disorders. Additionally, HCN2-IN-3 has potential applications in studies focusing on mental illnesses and mood-related conditions. -
HCN2 Inhibitor
HCN2-IN-6 is a selective inhibitor of the HCN2 ion channel, demonstrating an IC50 value of 7 nM. It exhibits minimal inhibition of HCN4, making it a valuable tool for studying HCN2-specific pathways. This reagent is suitable for research into inflammatory diseases and neurological disorders, facilitating the exploration of potential therapeutic strategies targeting these conditions. -
HCN Inhibitor
pan-HCN-IN-1 is a potent inhibitor of the hyperpolarization-activated and cyclic-nucleotide-gated 1 (HCN1) ion channel, exhibiting an IC50 value of 58 nM. This compound effectively attenuates the voltage sag response and enhances excitatory postsynaptic potential (EPSP) summation in ex vivo rat brain slices. It serves as a valuable tool for investigating the role of HCN1 channels in neuronal excitability and synaptic integration in various research applications. -
HCN Channel Inhibitor
MS7710 is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels. It effectively reduces HCN channel-mediated Ih current, leading to decreased firing frequency and burst activity in dopaminergic neurons within the ventral tegmental area. Research has demonstrated that MS7710 ameliorates deficits in social interaction and cognitive flexibility related to reward processing in mice subjected to chronic social defeat stress. This compound is valuable for studies focusing on major depressive disorder and its underlying mechanisms. -
HCN2 Inhibitor
HCN2-IN-4 is an orally active inhibitor of the HCN2 ion channel, which plays a crucial role in neuronal excitability and rhythmic activity. This compound effectively inhibits HCN2 channel activity, making it a valuable tool for investigating its involvement in pain mechanisms, tinnitus, and various central nervous system disorders. Researchers may utilize HCN2-IN-4 to explore therapeutic strategies targeting these conditions. -
HCN2 Inhibitor
HCN2-IN-2 is a selective inhibitor of the HCN2 ion channel, characterized by an IC50 of 145 nM. This azaindazole derivative effectively blocks HCN2 channel activity, preventing abnormal firing in peripheral nociceptive neurons. HCN2-IN-2 is suited for research applications focused on pain modulation and the underlying mechanisms of nociceptive signaling. -
HCN2 Inhibitor
HCN2-IN-1 is a potent HCN2 inhibitor with an IC50 of 98 nM. This compound selectively targets hyperpolarization-activated cyclic nucleotide-gated channels, making it a valuable tool for investigating central nervous system (CNS) and psychiatric disorders. HCN2-IN-1 can facilitate research into the mechanisms underlying neuronal excitability and potential therapeutic strategies for related conditions. -
HCN2 Inhibitor
HCN2 modulator-6 is a potent inhibitor of the HCN2 ion channel, exhibiting an IC50 of 7 nM. This compound effectively suppresses HCN2 channel activity, making it a valuable tool for investigating mechanisms underlying pain, including inflammatory and neuropathic pain. Additionally, HCN2 modulator-6 is applicable in research focused on tinnitus, central nervous system disorders, psychiatric conditions, and mood disorders. -
HCN2 Inhibitor
HCN2-IN-5 is a potent HCN2 ion channel inhibitor with an IC50 of 9 nM, exhibiting minimal inhibitory activity on HCN4. This compound is valuable in the study of inflammatory diseases and neurological disorders, providing insights into the modulation of ion channel activity. Its specificity and potency make it a useful tool for elucidating the role of HCN2 in various physiological and pathological processes. -
AMPAR Inhibitor
TAT-GluA2 3Y is an AMPAR inhibitor that interferes with the endocytosis of AMPA receptors, thereby blocking long-term depression (LTD) at glutamatergic synapses. This peptide has been shown to mitigate pentobarbital-induced spatial memory deficits, highlighting its potential in studying synaptic plasticity and memory-related research applications. TAT-GluA2 3Y serves as a valuable tool for exploring the mechanisms underlying synaptic transmission and cognitive function. -
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.
