nav1.7

Nav1.7-IN-6, a selective 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).

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

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 Nav1.7 inhibitor for research in the field of pain and anesthesia.

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

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

Nav1.7-IN-18 (Compound 31) is a Nav1.7 inhibitor with a Ki value of 4.9 nM and an IC50 of 13 nM, demonstrating analgesic effects in transgenic mice with inherited erythromelalgia (IEM).

Nav1.7-IN-13 (compound 3g) is a sodium channel inhibitor that notably suppresses Veratridine-induced neuronal activity. It inhibits the total Na+ current in DRG neurons in a concentration-dependent manner and delays the activation of Navs. Nav1.7-IN-13 significantly alleviates mechanical pain behavior in a rat model of nerve injury (SNI), exhibiting analgesic properties.

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

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

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 1 (example 41), an effective Na+ channel (Na v) blocker, exhibits a potent IC50 value of 0.037 μM. This compound is utilized in pain research, encompassing neuropathic, postoperative, and inflammatory pain among others [1].

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.

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

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

GX-585 is a sulfonamide analog that is a Nav 1.7 channel inhibitor with analgesic activity for the study of neuropathic pain and inflammation.

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

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

GDC-0276 is an orally active, selective, and potent NaV1.7 inhibitor that can be used for the study of pain-related diseases.

GNE-0439 is a novel, Nav1.7-selective inhibitor with an IC50 of 0.34 uM that also inhibits Nav1.5 (IC50=38.3 uM) and mutant N1742K channels (IC50=0.37 uM), possessing a carboxylic acid group that binds outside the channel pore, distinguishing it from known selective VSD4 binders and making it a valuable tool for ion channel research.

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.

AM-2099 is a selective voltage-gated sodium channel Nav1.7 inhibitor used in pain research.

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