Na_v1.7 Inhibitor

Veratridine (3-Veratroylveracevine) is a plant neurotoxin, a voltage-gated sodium channels (VGSCs) agonist. Veratridine inhibits the peak current of Nav1.7, with an IC₅₀ of 18.39 µM. Veratridine regulates sodium ion channels mainly by activating sodium ion channels, preventing channel inactivation and increasing sodium ion flow.

PF 05089771 is a potent, orally active and selective arylsulfonamide Na_v1.7 inhibitor, with IC₅₀ values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNa_v1.7, cynNa_v1.7, dogNa_v1.7, ratNa_v1.7, and musNa_v1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.

DSP-2230 is the orally active inhibitor for voltage-gated sodium channel that inhibits Nav1.7-, Nav1.8-, and Nav1.9-derived sodium currents with IC₅₀s of 7.1 μM, 11.4 μM and 6.7 μM, respectively. DSP-2230 can be used to improve neuropathic pain.

PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC₅₀s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect.

PF-06456384 trihydrochloride is an extremely potent and selective Na_v1.7 sodium channel blocker (IC₅₀: 0.01 nM for hNaV1.7; 75 nM for rNaV1.7; <0.1 nM for mNaV1.7). PF-06456384 trihydrochloride shows no significant analgesic efficacy in the mouse Formalin pain model.

GX-936 (PF-05196233) is a selective Nav1.7 inhibitor. GX-936 binds to the activated VSD4, forms a bidentate salt bridge with the R4 of the S4 helix, traps VSD4 in the activated state, and prevents the channel from recovering from the inactivated state. GX-936 can be used in studies related to pain.

Nav1.7-IN-22 (P58 13-2) is a selective inhibitor of voltage-gated sodium channel Nav1.7. Nav1.7-IN-22 inhibits abnormal electrical signal generation and conduction in sensory neurons by blocking Nav1.7 channel activity. Nav1.7-IN-22 can be used for the study of pain.

DA-0218 is a Nav1.7 inhibitor. DA-0218 exerts state-dependent inhibitory effects. DA-0218 alleviates formalin-induced inflammatory pain behavior and Paclitaxel-induced mechanical hyperalgesia in mice. DA-0218 inhibits Histamine-induced acute pruritus and lymphoma-induced chronic pruritus in mice. DA-0218 can be used in research related to inflammatory pain, neuropathic pain, acute pruritus and chronic pruritus.

ProTx II TFA is a selective blocker of Nav1.7 sodium channels, with an IC₅₀ value of 0.3 nM and a K_i of 0.389 nM against human NaV1.7. ProTx II TFA selectively blocks spinal cord NaV1.7 by reducing conductance and altering voltage dependence of activation, preferentially binds to the splice region of aNaV1.5, and can also block sodium channel subtypes such as Nav1.4 and Nav1.6. ProTx II TFA alleviates thermal hyperalgesia in diabetic mice and prevents the propagation of action potentials in nociceptors. ProTx II TFA can be used for research related to painful diabetic neuropathy and pain disorders.

TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC₅₀s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain.

GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC₅₀ value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects.

Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.

AM-2099 is a potent and selective inhibitor of voltage-gated sodium channel Nav1.7 with an IC₅₀ of 0.16 μM for human Nav1.7.

Raxatrigine (GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.

GDC-0310 is a selective acyl-sulfonamide Na_v1.7 inhibitor, with an IC₅₀ of 0.6 nM for hNa_v1.7.

Funapide (TV 45070; XEN402) is an orally active inhibitor of voltage-gated sodium channels (VGSC) in the peripheral nervous system with IC₅₀ values ??of 84 nM and 54 nM for Nav1.5 and Nav1.7, respectively. Funapide has analgesic effects.

XEN907 is a potent and spirooxindole blocker of Na_V1.7, with an IC₅₀ of 3 nM. XEN907 also inhibits CYP3A4 in a recombinant human enzyme assay. XEN907 can be used for the research of pain.

Nav1.7 inhibitor (compound II), a sulfonamide, is a potent Nav1.7 inhibitor. Nav1.7 inhibitor has the potential for a wide range of disorders, particularly pain, including acute pain, inflammatory pain and/or neuropathic pain.

DS-1971a is a potent, selective, and orally active NaV1.7 inhibitor, with IC₅₀s of 22.8 and 59.4 nM for hNaV1.7 and mNaV1.7, respectively. DS-1971a exerts analgesic effects.

GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC₅₀ of 3 nM.