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sodium-potassium pump inhibitor
Digoxin is a sodium-potassium pump inhibitor.- Ella Martin, .et al. , ACS Pharmacol Transl Sci, 2025, May 12;8(9):2996-3006 PMID: 40969890
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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Sodium Channel inhibitor
AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 uM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. Phase 3.- Giovanni Bocci, .et al. , ACS Pharmacol Transl Sci, 2020, Oct 14 PMID: 33330842
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HIF-1α inhibitor
Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
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SGLT2 inhibitor
PF-04971729 is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2. -
Sodium Channel Inhibitor
Lamotrigine-13C3 is a stable isotope-labeled derivative of Lamotrigine, a highly effective sodium channel inhibitor. This compound selectively targets voltage-gated Na+ channels, leading to stabilization of presynaptic neuronal membranes and a subsequent reduction in glutamate release. Lamotrigine-13C3 is suitable for research applications related to epilepsy, focal seizures, and other neurological disorders. -
glutamate release inhibitor
Sipatrigine, a neuroprotective agent, is a glutamate release inhibitor, voltage-dependent sodium channel and calcium channel inhibitor, penetrating the central nervous system. Has potential to treat focal cerebral ischemia and stroke. -
PDE1 inhibitor
Vinpocetine is a Ca2+-calmodulin-dependent phosphodiesterase I (PDE1) inhibitor. -
Nav inhibitor
Nav1.7-IN-2 is an inhibitor of voltage-gated sodium channels (Nav), in particular Nav 1.7, with IC50 of 80 nM. -
voltage-gated sodium channel Nav1.7 inhibitor
Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration. -
NaV1.3 and NaV1.1 channels inhibitor
ICA-121431 is a potent and selective inhibitor of human NaV1.3 and NaV1.1 channels (IC50 values are 13 and 23 nM respectively). -
sodium channel protein inhibitor
Oxcarbazepine is a sodium channel protein inhibitor. -
Sodium channel blocker/DNMT inhibitor
Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor. -
SChE inhibitor
Dibucaine (USAN) is an amide local anesthetic. Dibucaine reversibly binds to and inactivates sodium channels in the neuronal cell membrane. Inhibition of sodium channels prevents the depolarization of nerve cell membranes and inhibits subsequent propagation of impulses along the course of the nerve, thereby limiting the excitation of nerve endings. This results in loss of sensation. -
sodium channel inhibitor
Levobupivacaine is a local anaesthetic drug belonging to the amino amide group. -
Nav1.7 Inhibitor
PF-05089771 is a Selective Nav1.7 Inhibitor (IC50 = 11 nM) that interacts with the voltage-sensor domain (VSD) of domain IV. -
Nav1.7 sodium channel inhibitor
Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor. -
inhibitor of Kv2.1 and Kv2.2
RY785 (Kv2-IN-A1) is an inhibitor of Kv2.1 and Kv2.2. -
Nav1.7 inhibitor
PF-05241328 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (Nav1.7), with an IC50 of 31 nM. -
SLC13A5 inhibitor
BI01383298 is a potent inhibitor of SLC13A5, being selective over other family members and other transporters. -
Na+/H+ exchanger inhibitor
5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. -
NaV 1.7 inhibitor
NaV1.7 inhibitor-1 is an efficacious voltage-gated sodium channel (NaV) 1.7 inhibitor with an IC50 of 0.6 nM for hNaV1.7, exhibits 80-fold selectivity versus hNaV1.5. -
SLC34A1 inhibitor
PF-06869206 is an orally bioavailable selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC50 of 380 nM. -
Sodium Channel inhibitor
Sodium Channel inhibitor 1, one of 3-Oxoisoindoline-1-carboxamides, is a novel and selective voltage-gated sodium channel for pain treatment. -
Sodium Channel Inhibitor
Articaine is a selective inhibitor of voltage-gated sodium channels, including rNav1.4, hNav1.7, and rNav1.8, demonstrating an IC50 of 15.8 μM for open-state Na+ channels. It effectively blocks Na+ influx, leading to local anesthetic effects and interruption of nerve impulse conduction. Additionally, Articaine exhibits anti-inflammatory properties by inhibiting NF-κB activation and the NLRP3 inflammasome pathway. This compound is valuable for research in dental anesthesia and inflammatory-related conditions, such as acute kidney injury. -
Sodium Channel Inhibitor
Decarbamoylsaxitoxin is a potent sodium channel inhibitor that selectively blocks the influx of sodium ions in excitable tissues, such as nerve and skeletal muscle cells, thus preventing action potential generation. As a hydrolysis product of saxitoxin, Decarbamoylsaxitoxin exhibits similar neurotoxic effects, including the ability to inhibit veratridine- and ouabain-induced neuroblastoma cell swelling and lysis. This reagent is valuable for research involving mechanisms of paralytic shellfish poisoning and sodium channel pharmacology. -
NET Inhibitor
Nisoxetine is a potent and selective inhibitor of the norepinephrine transporter (NET) with a Kd of 0.76 nM. This compound exhibits antidepressant properties and functions as a local anesthetic, in addition to blocking voltage-gated sodium channels. Its mechanisms make it valuable for research in neuropharmacology and the investigation of depression and pain pathways. -
Sodium-Calcium Exchanger Inhibitor
KB-R7943 is a selective inhibitor of the sodium-calcium exchanger, exhibiting an IC50 value of 5.1 µM. This compound is utilized as a valuable tool in studies involving cardiac and renal failure models, facilitating research into calcium homeostasis and its implications in heart and kidney function. -
Sodium Channel Inhibitor
Benzamil is a sodium channel inhibitor, functioning as a non-selective blocker of epithelial sodium channels (ENaC) and a Na+/Ca2+ exchanger (NCX) inhibitor with an IC50 value of approximately 100 nM. Its pharmacological properties include the enhancement of myogenic vasoconstriction. Additionally, Benzamil inhibits TRPP3-mediated Ca2+-activated currents, exhibiting an IC50 of 1.1 μM. This compound is valuable for research applications focused on cardiovascular physiology and electrolyte transport mechanisms. -
NMDA Receptor Inhibitor
Bupivacaine is an NMDA receptor inhibitor that modulates neuronal excitability by blocking sodium, L-calcium, and potassium channels. It exhibits potent inhibition of SCN5A channels, with an IC50 of 69.5 μM. This compound is primarily utilized in research focused on chronic pain mechanisms and therapeutic interventions. -
NMDA Receptor Inhibitor
Bupivacaine-d9 is a deuterium-labeled analog of Bupivacaine, primarily targeting NMDA receptors. This compound exhibits inhibitory effects on sodium, L-calcium, and potassium channels, with a notable potency against SCN5A channels, characterized by an IC50 value of 69.5 μM. Bupivacaine-d9 is utilized in research related to chronic pain mechanisms and the modulation of excitatory neurotransmission, offering valuable insights into therapeutic applications in pain management. -
Potassium/Sodium Channel Inhibitor
Huwentoxin I is a peptide toxin that specifically inhibits voltage-gated sodium channels and N-type calcium channels. This compound has demonstrated significant inhibitory effects on sodium channels in both rat hippocampus and cockroach dorsal unpaired median (DUM) neurons, with IC50 values of 66.1 nM and 4.80 nM, respectively. Huwentoxin I is valuable for studies focused on neuronal excitability and channelopathy-related research applications. -
Sodium Channel Inhibitor
(-)-Sparteine sulfate pentahydrate is a sodium channel inhibitor that acts as a class 1a antiarrhythmic agent. It has demonstrated notable biological activity in modulating cardiac excitability and can be utilized in research focusing on arrhythmias and pharmacological studies related to ion channel function. This reagent is suitable for investigating the effects of sodium channel blockade in various biological models. -
Nav1.7 Inhibitor
Nav1.7-IN-6 is a selective inhibitor targeting the voltage-gated sodium channel Nav1.7, which is important in pain signaling pathways. This compound demonstrates significant biological activity in modulating neuronal excitability, making it a valuable tool for research on pain mechanisms and potential therapeutic interventions in pain disorders. Its specificity for Nav1.7 enhances its utility in elucidating the role of this channel in nociception and related studies. -
Sodium Channel Inhibitor
B-GYKI-38233 hydrochloride is a sodium channel inhibitor that exhibits potent antiarrhythmic properties. This compound is utilized in research focused on the modulation of sodium channels, which play a critical role in cardiac excitability and conductivity. Its mechanism of action makes it a valuable tool for the investigation of arrhythmias and related cardiovascular disorders. -
Nav1.8 channel Inhibitor
Nav1.8-IN-10 is a selective inhibitor of the Nav1.8 ion channel. At a concentration of 4 nM, it achieves an impressive blocking rate of 79.4%, demonstrating its potency. This compound is primarily utilized in the research of pain disorders, facilitating investigations into the modulation of pain pathways and potential therapeutic interventions. -
Nav1.8 Inhibitor
Nav1.8-IN-5 is a selective inhibitor of the voltage-gated sodium channel Nav1.8. It demonstrates potent biological activity against Nav1.8-mediated pain and pain-related disorders, making it a valuable tool for research in these areas. Additionally, Nav1.8-IN-5 can facilitate studies related to cardiovascular diseases, including conditions such as atrial fibrillation, by modulating sodium channel activity. -
Sodium Channel Inhibitor
R 59494 is a sodium channel inhibitor that effectively blocks Na+ and Ca2+ uptake triggered by veratridine exposure. This compound exhibits significant anti-ischemic properties, making it valuable for research in cardiovascular and neuroprotective studies. Its ability to modulate ion channel activity positions R 59494 as a useful tool for investigating the mechanisms of ischemia-related cellular damage. -
NaV1.8 Channel Inhibitor
Analgesic agent-2 is a selective NaV1.8 channel inhibitor, exhibiting a reported IC50 of 50.18 nM in HEK293 cells expressing the human NaV1.8 channel. It demonstrates significant analgesic activity, making it a valuable tool for pain research. This compound is ideal for studies investigating the role of NaV1.8 in nociception and the development of novel analgesic therapies. -
Nav1.8 Inhibitor
Nav1.8-IN-15 is a potent inhibitor of the voltage-gated sodium channel Nav1.8. It demonstrates significant analgesic effects and is relevant for research exploring pathways involved in chronic pain management. This compound can facilitate the study of Nav1.8's role in pain signaling and aid in the development of novel therapeutic strategies for pain relief.

