sodium channel inhibitor 1

Sodium Channel inhibitor1 is a novel and selective voltage-gated sodium channel for pain treatment. (IC50 Value of 0.16 uM and 0.41 uM for Na v1.7, V hold-90mV and Na v1.7, V hold-90mV)

Procainamide Hydrochloride (Procapan) is the hydrochloride salt form of procainamide, an amide derivative exhibiting class 1A antiarrhythmic property and analog of procaine. Procainamide hydrochloride reversibly binds to and blocks activated (open) voltage-gated sodium channels, thereby blocks the influx of sodium ions into the cell, which leads to an increase in threshold for excitation and inhibit depolarization during phase 0 of the action potential.

Ropivacaine (LEA-103 HCl) is a local anaesthetic drug belonging to the amino amide group.

Triamterene is a barosensitive epithelial sodium channel (ENaC) blocker with a diuretic effect. It can also act as an inhibitor of the TGR5 receptor, reducing GLP-1 secretion and cAMP level increases induced by TGR5 activation in a dose-dependent manner.

Benzocaine is a surface anesthetic that acts by preventing transmission of impulses along nerve fibers and at nerve endings.

Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.

AZD7507 is a CSF-1R inhibitor with an IC50 of 32 nM. AZD7507 has antitumor activity.

1-(2,4-difluorophenyl)guanidine hydrochloride is a compound that is a potent and selective inhibitor of the voltage-gated sodium channel Nav1.7, a key player in pain signaling. It is therefore able to reduce pain signaling, resulting in an analgesic effect.

Nav1.8-IN-1 (CHEMBL1270208) is an inhibitor of human NaV1.8

Ropivacaine hydrochloride (Ropivacaine monohydrochloride) is the hydrochloride salt of ropivacaine, a local anesthetic of the amide type with analgesic activity.

NaV1.7 inhibitor-1, an efficacious inhibitor of voltage-gated sodium channel (NaV) 1.7 (IC50 of 0.6 nM for hNaV1.7).

SLC13A5-IN-1 is a selective inhibitor of the sodium-citrate co-transporter (SLC13A5) that completely blocks the uptake of 14C-citrate, with an IC50 of 0.022 μM in HepG2 cells.

Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide inhibits H. pylori recombinant carbonic anhydrase (CA) and the human CA isoforms I, II, and V with Ki values of 218, 56, 35, and 21 nM, respectively.4,5 In mice, it has anticonvulsant activity against maximal electroshock seizure (MES) and pentylenetetrazole-induced maximal, but not minimal, seizures (ED50s = 19.6, 9.3, and >500 mg/kg, respectively). Zonisamide (40 mg/kg, p.o.) prevents MPTP-induced decreases in the levels of dopamine , but not homovanillic acid or dihydroxyphenyl acetic acid , and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy. |1. Masuda, Y., Ishizaki, M., and Shimizu, M. Zonisamide: Pharmacology and clinical efficacy in epilepsy. CNS Drug Rev. 4(4), 341-360 (1998).|2. Rock, D.M., Macdonald, R.L., and Taylor, C.P. Blockade of sustained repetitive action potentials in cultured spinal cord neurons by zonisamide (AD 810, CI 912), a novel anticonvulsant. Epilepsy Res. 3(2), 138-143 (1989).|3. Suzuki, S., Kawakami, K., Nishimura, S., et al. Zonisamide blocks T-type calcium channel in cultured neurons of rat cerebral cortex. Epilepsy Res. 12(1), 21-27 (1992).|4. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).|5. De Simone, G., Di Fiore, A., Menchise, V., et al. Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: Solution and X-ray crystallographic studies. Bioorg. Med. Chem. Lett. 15(9), 2315-2320 (2005).|6. Yabe, H., Choudhury, M.E., Kubo, M., et al. Zonisamide increases dopamine turnover in the striatum of mice and common marmosets treated with MPTP. J. Pharmacol. Sci. 110(1), 64-68 (2009).

Ropivacaine mesylate, a long-acting amide local anaesthetic, is used for spinal block and effectively mitigates neuropathic pain. It achieves analgesia by reversibly inhibiting sodium ion influx in nerve fibers, thus blocking impulse conduction. Additionally, Ropivacaine acts as an inhibitor of the K2P (two-pore domain potassium channel) TREK-1, exhibiting an IC50 of 402.7 μM in COS-7 cell membranes.

Nav1.3 Channel Inhibitor 1 (Compound 15b) is a state-dependent inhibitor of the voltage-gated sodium channel Na v 1.3, with an IC50 value of 20 nM. It has the ability to cross the blood-brain barrier, making it applicable for research into nervous system disorders [1].

ProTx-III, a spider venom peptide derived from the Peruvian green velvet tarantula, functions as a selective and potent inhibitor of the voltage-gated sodium channel Na v 1.7, exhibiting an IC 50 of 2.1 nM. Characterized by its inhibitor cystine knot motif (ICK), ProTx-III can attenuate the pain response and is applicable in research on chronic pain, epilepsy, and arrhythmia [1].

GTx1-15, an inhibitor cystine knot (ICK) peptide, antagonizes the voltage-dependent calcium channel Cav3.1, as well as voltage-dependent sodium channels Nav1.3 and Nav1.7 [1].

Ceratotoxin-2 (CcoTx2) is a voltage-gated sodium channel inhibitor with half maximal inhibitory concentrations (IC50) of 8 nM for Na v 1.2 β 1 and 88 nM for Na v 1.3 β 1 [1].

Ceratotoxin-1 (CcoTx1) is a peptide toxin that functions as an inhibitor of various voltage-gated sodium channel subtypes. It selectively inhibits Nav1.1 β1, Nav1.2 β1, Nav1.4 β1, and Nav1.5 β1 with IC50 values of 523 nM, 3 nM, 888 nM, and 323 nM, respectively. Additionally, Ceratotoxin-1 is known to inhibit Nav1.8 β1 [1].

Pterinotoxin-2 is a peptide toxin that acts as a sodium channel inhibitor [1].

Pterinotoxin-1 is a peptide toxin that functions as an inhibitor of sodium channels [1].

Sodium Channel Inhibitor 4 is a compound that functions as a sodium channel inhibitor [1].

Nav1.8-IN-5 (Example 1), a voltage-gated sodium channel Nav1.8 inhibitor, is applicable in the research of Nav1.8-mediated diseases including pain, pain-related disorders, and cardiovascular diseases (such as atrial fibrillation) [1].

Nav1.8-IN-8 (Compound A11), a Nav1.8 channel inhibitor, potentially mitigates diseases mediated by sodium ion channels (NaV) [1].