nav1.8 channel

Suzetrigine (VX-548) is a small molecule inhibitor and a highly selective inhibitor of the NaV1.8 target, with oral activity and good peripheral nerve selectivity. Suzetrigine is used for the treatment of moderate to severe acute pain following abdominoplasty or bunionectomy.

PF 04531083 is a selective blocker of the NaV1.8 channel. PF 04531083 can be used for neuropathic and inflammatory pain studies.

Cyfluthrin binds to voltage-sensitive sodium channel such as Nav 1.8 sodium channel and modify their gating kinetics, thereby disrupting nerve function of pests.

PF-04885614 is a potent inhibitor of NaV1.8, has potential for neurological and neurodevelopmental diseases treatment.

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

ABBV-318 can be used as small molecule Nav1.7/Nav1.8 blockers for the treatment of pain, with IC50 values of 2.8 μM for hNav1.7 and 3.8 μM for hNav1.8. ABBV-318 can be used to study pain-related disorders.

Nav1.8-IN-4 is a potent Nav1.8 channel inhibitor with potential analgesic activity.Nav1.8-IN-4 can be used for pain and neurological related disorders.

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

VX-150 is a highly selective NaV1.8 inhibitor relative to the other sodium channel subtypes (>400-fold).

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.

PF-06305591 is an effective and selective blocker of voltage-gated sodium channel NaV1.8 (IC50 = 15 nM).

PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker [IC50: 196 nM].

QX-314 bromide is a membrane-impermeable sodium channel blocker that inhibits TRPV1 and NaV1.8 expression, causing sensory-selective blockade of TRPV1 channels. It exhibits anti-inflammatory effects and may be used in studies of gastroesophageal reflux disease (GERD).

A-803467 is a selective NaV1.8 channel blocker.

Nav1.8-IN-16 (Compound (R)-40) is an orally bioavailable and selective hNaV 1.8 inhibitor with an IC50 of 5.9 nM. It provides analgesic effects by blocking the NaV1.8 channel without significantly affecting other NaV subtypes or the hERG channel. Nav1.8-IN-16 demonstrates dose-dependent pain relief in postoperative and inflammatory pain models and is suitable for pain-related research.

Nav1.8-IN-6 (Compound 2j) is a novel pyridinone amide Nav1.8 channel inhibitor with IC50 values of 513.33 nM in the resting state and 471.81 nM in the partially activated state. Nav1.8-IN-6 also exhibits analgesic activity.

(S)-LTGO-33 is a small molecule inhibitor of the voltage-gated sodium channel NaV1.8, and it can be utilized in research for the treatment of pain disorders.

Nav1.8-IN-20 (Compound I) is an orally active inhibitor of the voltage-gated sodium channel Nav1.8, with an IC50 value of 14 nM. It effectively blocks the generation and propagation of action potentials in peripheral nociceptive neurons, providing analgesic effects. Nav1.8-IN-20 shows potential for research in several pain types, including acute, chronic, inflammatory, and neuropathic pain.

PF-06305591 dihydrate is a potent and highly selective voltage-gated sodium channel NaV1.8 blocker (IC50 = 15 nM) with excellent preclinical in vitro ADME and safety profiles [1].

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.

Mambalgin 1 TFA, a selective inhibitor of ASIC1a (with IC50 values of 192 nM for human ASIC1a and 72 nM for the ASIC1a/1b dimer), preferentially binds to the channel in its closed/inactive state. It demonstrates selectivity for ASIC1a over a range of other channels, including ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2, and Kv1.2. In vivo, Mambalgin 1 TFA effectively prolongs the latency of the withdrawal response in mouse tail-flick and paw-flick tests.

Analgesic Agent-2, a selective orally active inhibitor of the NaV1.8 channel, demonstrates an IC50 of 50.18 nM in HEK293 cells that stably express the human NaV1.8 channel, indicating its potential for analgesic activity [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].

VSTx-3 is a potassium voltage-gated channel (K_V) blocker, which has also been shown to be a potent tetrodotoxin-sensitive (TTX-sensitive) sodium channel inhibitor, with particular efficacy against NaV1.8 channels, as evidenced by its half-maximal inhibitory concentration (IC_50) values of 0.19 μM for hNaV1.3, 0.43 μM for hNaV1.7, and 0.77 μM for hNaV1.8 channels.