nav1.7 inhibitor

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

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

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.

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

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.

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

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

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.

PF-04856264 is a potent and selective human Nav1.7 voltage-gated sodium channel inhibitor (IC50 = 28 nM).

PF-05198007 is a compound with a similar pharmacodynamic profile to PF-05089771. PF-05198007 is an effective and selective arylsulfonamide Nav1.7 inhibitor.

TC-N 1752 is an orally active inhibitor of Nav1.7 channel with IC50 of 0.17 μM. TC-N 1752 shows analgesic activities.

GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype-selective Nav1.7 inhibitor (Ki: 0.79 nM, Kd: 0.38 nM for hNav1.7) for the treatment of chronic pain.

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].

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].

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.

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.

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

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].

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.

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

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.

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.

Heteropodatoxin-1 (HpTx1), a spider peptide toxin, acts as an inhibitor of the Kv4.2 current, while concurrently inhibiting Nav1.7 and activating Nav1.9 channels. However, it has no effect on Nav1.8 channels [1].

Pe1b (μ-TrTx-Pe1b) is a selective inhibitor of the NaV1.7 channel, exhibiting an inhibitory concentration 50 (IC50) value of 167 nanomolar (nM) [1].

PF-06456384 is a highly potent and selective NaV1.7 inhibitor with IC50 value of 0.01 nM.

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

GX-936, a Nav1.7 inhibitor, inhibits Nav1.7 through a voltage-sensor trapping mechanism, likely by stabilizing inactivated states of the channel.

GX-395 is a novel Nav1.7 inhibitor.

Raxatrigine hydrochloride is a state-dependent sodium channel blocker and a Nav1.7 sodium channel inhibitor.