nav1.7

Nav1.7-IN-6, a selective inhibitor of Nav1.7.

Nav1.7-IN-3 is a selective and orally bioavailable inhibitor of voltage-gated sodium channel Nav1.7(IC50 of 8 nM).

Nav1.7 inhibitor is a potent inhibitor of Nav1.7.

Nav1.7-IN-8 is a highly potent and selective inhibitor of NaV1.7, exhibiting greater selectivity for inhibiting NaV1.7 compared to the subtypes hNaV1.1 and hNaV1.5. Additionally, Nav1.7-IN-8 has inhibitory effects on CYP2C9 and CYP3A4, with IC50 values of 0.17 μM and 0.077 μM, respectively. Notably, Nav1.7-IN-8 demonstrates significant analgesic properties in rodent models of both acute and inflammatory pain.

NaV1.7 Blocker-801 is a potent NaV1.7 blocker.

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

Nav1.7-IN-2 is avoltage-gated sodium channels (Nav) inhibitor in particular Nav 1.7(IC50 of 80 nM).

(Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379 which is an orally active and selective sulfonamide NaV1.7 antagonist.

Raxatrigine (CNV 1014802) has been investigated for the treatment of Bipolar Disorder and Bipolar Depression.

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.

PF-05186462 (PF-05150122) is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 21 nM, no significant activity against Nav1.5.

GX 201 is a selective NaV1.7 inhibitor, IC50 of < 3.2 nM for hNaV1.7.

XEN907 is a novel spiro oxindole NaV1.7 blocker. XEN907 also inhibits hNaV1.7 (IC50: 3 nM).

Potent Nav1.7 blocker (IC50 = 2.5 nM). Also inhibits Nav1.1, Nav1.2, Nav1.3 and Nav1.6 in the nanomolar range. Exhibits no effects on Cav channels or nAChR at 5 μM. Demonstrates analgesic activity in vivo; antagonizes effects of scorpion-venom toxin OD1 a

3'-Methoxydaidzein is a dual isoflavone and Sodium Channel inhibitor. 3'-Methoxydaidzein inhibited NaV1.7, NaV1.8 and NaV1.3 with IC50 of 181 nM, 397 nM and 505 nM, respectively. 3'-Methoxydaidzein was specific for collagen-induced platelet aggregation with IC50 values of 12.3 and 61.5µM, respectively. 3'-Methoxydaidzein acts as an analgesic by inhibiting voltage-gated sodium channels. 3'-Methoxydaidzein showed antioxidant activity and antiplatelet aggregation activity.

LTGO-33 is a species-specific inhibitor of the voltage-gated sodium channel NaV1.8, inhibiting NaV1.8, NaV1.1-NaV1.7, and NaV1.9.LTGO-33 inhibits wild-type and multiple NaV1.8 variants associated with human pain disorders and can be used for the study of pain.hBChE-IN-2 is a low affinity Nurr1 agonist.

Cd1a, a β-toxin from the African spider Ceratogyrus darlingi, modulates calcium ion channels and inhibits human calcium ion channels (Ca v 2.2)(IC 50 2.6 μM) as well as mouse sodium ion channels (Na v 1.7). This compound has potential applications in creating drugs for the treatment of peripheral pain [1].

Selective NaV1.7 channel blocker. Shifts activation gating positively and decreases current magnitude. Displays 100-fold selectivity over other sodium channel subtypes.

DS-1971a is a highly potent and selective NaV1.7 inhibitor. DS-1971a exhibits a favorable toxicological profile and analgesic effects.

ProTx-II TFA is a potent and highly selective Nav1.7 sodium channel blocker, exhibiting an IC50 of 0.3 nM and demonstrating at least 100-fold selectivity over other sodium channel subtypes. It decreases channel conductance, shifts activation towards more positive potentials, and inhibits action potential propagation in nociceptors [1] [2].

Potent and reversible Kv3.4 potassium channel blocker (IC50 = 47 nM); also attenuates inactivation of sodium currents by acting on Nav1.7 and Nav1.3 channels. Enhances TTX-sensitive sodium currents in rat small dorsal root ganglion neurons. Neuroprotective.

Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective Nav1.1 channels positive modulator. Lu AE98134 also increases the activity of Nav1.2 and Nav1.5 channels but not of Nav1.4, Nav1.6 and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al[1].

Potent rat Nav1.7, human Nav1.4 and rat Nav1.6 channel activator (EC50 values are 7, 10 and 47 nM, respectively). Exhibits minimal activation at mammalian Nav1.2, Nav1.3 and Nav1.5 (EC50 values >3 μM). Inhibits fast inactivation on all channels. Increases

GNE-131 is a potent and specific inhibitor of human sodium channel NaV1.7 (IC50: 3 nM).

PF-05150122 is a novel potent and selective human Nav1.7 blocker.

ICA-121431 (2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl) is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, with little or no activity against human Nav1.5 or Nav1.7 channels.

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].

Phlotoxin-1 (PhlTx1), a 34-amino acid peptide featuring three disulfide bridges, is derived from the Phlogiellus genus spider and acts as an antinociceptive agent by inhibiting the NaV1.7 channel [1] [2].

δ-Theraphotoxin-Hm1b, a 42-amino acid peptide derived from the Togo starburst tarantula (Heteroscodra maculata) venom, selectively inhibits the inactivation of NaV1.1 channels without affecting NaV1.7 channels [1].

m3-Huwentoxin IV (m3-HwTx-IV) is a potent inhibitor of sodium channels (NaV), exhibiting half-maximal inhibitory concentrations (IC50s) of 3.3 nM for hNaV1.7, 6.8 nM for hNaV1.6, 7.2 nM for hNaV1.3, 8.4 nM for hNaV1.1, 11.9 nM for hNaV1.2, and 369 nM for hNaV1.4 in the QPatch assay. It also dose-dependently alleviates spontaneous pain in a rodent model when induced by the NaV1.7 activator OD1 [1].

Phlo1a (μ-TrTx-Phlo1a), a 35-amino acid peptide toxin, demonstrates a weak inhibitory effect on Nav1.2 and Nav1.5 channels [1]. Meanwhile, Phlo1b acts as a selective inhibitor of the Nav1.7 channel.

PF 05089771 is a Selective inhibitor of Nav1.7 (IC50 = 11 nM) that interacts with the voltage-sensor domain of domain IV. It shows a slow onset of the block that is depolarization and concentration-dependent.

CRMP2-Ubc9-NaV1.7 inhibitor 194, is a CRMP2-Ubc9-NaV1.7 inhibitor.

SUN49199, also known as NaV1.7 Blocker-13, is a novel selective blocker of NaV1.7 with little affinity for NaV 1.2, 1.3, or 1.6, being more potent at human vs guinea pig NaV1.7. SUN49199 was reported in Journal of Pharmacology and Experimental Therapeutics (2017), 361(1), 172-180. This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming).

GDC-0276, a potent, selective, reversible, and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM, offers potential for pain treatment while overcoming limitations associated with current pain medications, including addiction and off-target side effects. It is well tolerated and demonstrates a favorable pharmacokinetic profile.

AM-2099 is a voltage-gated sodium channel Nav1.7 inhibitor (IC50: 0.16 μM).

GNE-0439 is a novel Nav1.7-selective inhibitor (IC50: 0.34 uM) and inhibits Nav1.5 (IC50: 38.3 μM). GNE-0439 inhibits mutant N1742K channels (IC50: 0.37 uM) in membrane potential assays.

DSP-2230 is a selective blocker of Nav1.7/Nav1.8.

Selective NaV1.7 channel blocker. Preferentially inhibits neuronal NaV1.7, 1.2 and 1.3 (IC50 values are 26, 150 and 338 nM respectively), compared to muscle subtypes NaV1.4 and 1.5 (IC50 = >10 μM). Inhibits the channel by binding at the neurotoxin recepto

Veratridine is a benzoate-cevane found in Veratrum and Schoenocaulon. It activates sodium channels to stay open longer than normal.

Ancistrotecine B (Compound 2), a Nav1.7 channel inhibitor (IC50: 0.73 μM), has been shown to alleviate inflammatory pain in mice [1].

GrTx1, a peptide toxin derived from Grammostola rosea spider venom, selectively inhibits sodium channels Nav1.1, Nav1.2, Nav1.3, Nav1.4, Nav1.6, and Nav1.7, with IC50 values of 0.63 µM, 0.23 µM, 0.77 µM, 1.29 µM, 0.63 µM, and 0.37 µM, respectively [2]. This compound has applications in neurological disease research [1].

Theraphotoxin-Tap1a (Tap1a) is a spider venom-derived peptide that acts as an inhibitor of sodium channels, displaying IC50 values of 80 nM for Na v 1.7 and 301 nM for Na v 1.1. It demonstrates analgesic effects [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].

GsAF-I is a potent blocker of Na_v and hERG1 channels, exhibiting half-maximal inhibitory concentrations (IC50s) of 0.36 μM (Na_v 1.1), 0.6 μM (Na_v 1.2), 1.28 μM (Na_v 1.3), 0.33 μM (Na_v 1.4), 1.2 μM (Na_v 1.6), 0.04 μM (Na_v 1.7), and 4.8 μM (hERG1) [1].

GX-674 is a highly potent and selective voltage-gated sodium channel 1.7 (Nav1.7) antagonist with an IC50 value of 0.1 nM measured at -40 mV for the study of inflammatory and neuropathic pain.

Funapide (TV 45070) is a potent Sodium Channel Nav1.7 inhibitor with potential anti-inflammatory activity for the treatment of erythema gangrenosum, musculoskeletal pain, knee osteoarthritis, and postherpetic nerves.

Huwentoxin-IV TFA is a potent, selective blocker of sodium channels, specifically inhibiting neuronal Nav1.7, Nav1.2, Nav1.3, and Nav1.4 with IC50 values of 26, 150, 338, and 400 nM, respectively. It preferentially targets the peripheral nerve subtype Nav1.7 by interacting with neurotoxin receptor site 4, demonstrating analgesic effects in animal models of inflammatory and neuropathic pain [1] [2].

Piromelatine is an agonist of melatonin MT1/MT2 receptors, 5-HT1A and 5-HT1D, and an antagonist of 5-HT2B.Piromelatine has antinociceptive activity with inhibitory effects on P2X3, TRPV1, and Nav1.7 channels, and can be used in studies of sleep-promoting, pain-relieving, anti-neurodegenerative, and antidepressant diseases. diseases, and can be used to improve memory deficits associated with chronic mild stress-induced lack of pleasure in rats.

PF-05241328 is an effective and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (IC50: 31 nM).