Nav1.8
NaV1.8, encoded by SCN10A, is a tetrodotoxin-resistant voltage-gated sodium channel expressed by dorsal root ganglion sensory neurons associated with C-fibres[1]. It supports nociceptor excitability because its sodium current contributes to action-potential generation in sensory neurons activated by tissue damage[1]. Mechanistically, inflammatory signaling can increase tetrodotoxin-resistant sodium current through the cyclic AMP-protein kinase A pathway, linking NaV1.8 function to peripheral sensitization[2]. In pain models, reducing NaV1.8 expression or blocking NaV1.8 attenuated neuropathic or inflammatory pain behaviors in rats[3][4]. Compared with NaV1.7, which strongly determines inflammatory pain thresholds, NaV1.8 is distinguished by sensory-neuron selectivity and tetrodotoxin resistance[1][5]. For experimental applications, A-803467 selectively blocked human NaV1.8 and reduced mechanical allodynia or thermal hyperalgesia in rat pain models[4]. Clinically, the oral selective NaV1.8 inhibitor VX-548 reduced acute postoperative pain at the highest tested dose in phase 2 trials[6].
References:
- [1]. Akopian AN, et al. A tetrodotoxin-resistant voltage-gated sodium channel expressed by sensory neurons. Nature. 1996 Jan 18;379(6562):257-62. [Content Brief]
- [2]. England S, et al. PGE2 modulates the tetrodotoxin-resistant sodium current in neonatal rat dorsal root ganglion neurones via the cyclic AMP-protein kinase A cascade. J Physiol. 1996 Sep 1;495 ( Pt 2)(Pt 2):429-40. [Content Brief]
- [3]. Mikami M, et al. Short hairpin RNA-mediated selective knockdown of NaV1.8 tetrodotoxin-resistant voltage-gated sodium channel in dorsal root ganglion neurons. Anesthesiology. 2005 Oct;103(4):828-36. [Content Brief]
- [4]. Jarvis MF, et al. A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8520-5. [Content Brief]
- [5]. Nassar MA, et al. Neuropathic pain develops normally in mice lacking both Na(v)1.7 and Na(v)1.8. Mol Pain. 2005 Aug 22;1:24. [Content Brief]
- [6]. Jones J, et al. Selective Inhibition of NaV 1.8 with VX-548 for Acute Pain. N Engl J Med. 2023 Aug 3;389(5):393-405. [Content Brief]
All Product Categories
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Nav1.8 Related Products (43)
Related Products (43)
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E0199
0 ImagesE0199 is a novel potent dual-target KV7/NaV modulator that activates the KV7 channel (KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), and KV7.5 (EC50 = 27.14 nM) channels) while simultaneously blocks the NaV1.7 (IC50 = 0.52 μM), NaV1.8 (IC50 = 0.24 μM), and NaV1.9 (IC50 = 0.16 μM) channels. E0199 shows a potent analgesic effect without affecting heart and skeletal muscle ion channels critically in a chronic constriction injury (CCI) mouse model. E0199 can be used for Neuropathic pain (NP) research.
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GpTx-1 TFA
0 ImagesCat. No.: HY-P1681APurity: 99.56%GpTx-1 TFA is a peptide-based NaV1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 TFA demonstrates potent inhibitory activity against the NaV1.7 channel with an IC50 value of 10 nM, while exhibiting excellent selectivity for NaV1.4 (IC50 = 0.301 μM) and NaV1.5 (IC50 = 4.20 μM), showing >20-fold and >950-fold selectivity respectively.
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Mambalgin 1 TFA
0 ImagesCat. No.: HY-P1441AMambalgin 1 TFA is a selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.
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PF-06305591 dihydrate
0 ImagesPF-06305591 dihydrate is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile.
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(R)-Funapide
0 ImagesSynonyms: (R)-TV 45070; (R)-XEN402(R)-Funapide ((R)-TV 45070) is the less active R-enantiomer of Funapide. Funapide is a potent inhibitor of the sodium channel Nav1.7, Nav1.8 and other Nav channels expressed in the peripheral nervous system. Fornabil is an orally effective analgesic agent.
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4',7-Di-O-methylnaringenin
0 ImagesSynonyms: (-)-Naringenin 4',7-dimethyl Ether; (-)-NRG-DM4',7-Di-O-methylnaringenin ((−)-NRG-DM) is a flavonoid found in Renealmia alpinia. (−)-NRG-DM inhibits Nav1.7, Nav1.8 and Kv2.1 channels and has analgesic activity. Intraperitoneal administration of (−)-NRG-DM dose-dependently attenuated pain in a formalin-induced mouse inflammatory pain model and mustard oil-induced mouse colorectal pain model[2].
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Nav1.8-IN-16
0 ImagesCat. No.: HY-172903Nav1.8-IN-16 (Compound (R)-40) is an orally active and selective hNaV 1.8 inhibitor (IC50: 5.9 nM). Nav1.8-IN-16 exerts analgesic effects by blocking NaV1.8 channels without significantly affecting other NaV subtypes or hERG channels. Nav1.8-IN-16 exhibits dose-dependent analgesic effects in postoperative pain and inflammatory pain models and can be used in pain-related research.
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Nav1.8-IN-21
0 ImagesCat. No.: HY-176911CAS No.: 3049923-99-8Nav1.8-IN-21 is a potent and selective Nav1.8 inhibitor with analgesic activity. Nav1.8-IN-21 can be used for analgesia Research.
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Nav1.8-IN-15
0 ImagesCat. No.: HY-159094CAS No.: 524061-69-6Nav1.8-IN-15 (compound 6) is a potent Nav1.8 inhibitor. Nav1.8-IN-15 shows analgesic effect. Nav1.8-IN-15 has the potential for the research of chronic pain.
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Pterinotoxin-1
0 ImagesCat. No.: HY-P5943Pterinotoxin-1 is a sodium channel inhibitor peptide toxin.
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Nav1.8-IN-23
0 ImagesCat. No.: HY-183646Nav1.8-IN-23 is a Nav1.8 voltage-gated sodium channel inhibitor with a pIC50 of 6.1. Nav1.8-IN-23 can be used for the research of pain-related diseases.
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Nav1.8-IN-25
0 ImagesCat. No.: HY-189273Nav1.8-IN-25 is a NaV1.8 inhibitor (IC50 of 3.43 μM for resting-state NaV1.8 and IC50 of 3.37 μM for half-inactivated NaV1.8). It exerts analgesic activity in inflammatory, neuropathic, and visceral pain models by blocking voltage-gated Sodium Channel currents in both resting and half-inactivated states. Nav1.8-IN-25 can be used for research on chronic pain.
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Nav1.8-IN-20
0 ImagesCat. No.: HY-174845CAS No.: 3024470-62-7Nav1.8-IN-20 (Compound I) is an orally active and potent voltage-gated sodium channel Nav1.8 inhibitor with an IC50 value of 14 nM. Nav1.8-IN-20 blocks the generation and conduction of action potentials in peripheral nociceptive neurons, exerting analgesic effects. Nav1.8-IN-20 is promising for research of various pain types such as acute pain, chronic pain, inflammatory pain, and neuropathic pain.
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Nav1.8-IN-11
0 ImagesCat. No.: HY-160592CAS No.: 2990578-70-4Nav1.8-IN-11 (Example 1) is a Nav1.8 channel inhibitor with a IC50 value of 0.1 nM. Nav1.8-IN-11 can be used in the study of pain disorders.
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Nav1.8-IN-13
0 ImagesCat. No.: HY-161572CAS No.: 2785391-79-7Nav1.8-IN-13 (compound 16) is a Nav1.8 inhibitor (pIC50=7.9).
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GpTx-1
0 ImagesCat. No.: HY-P1681CAS No.: 1661050-12-9GpTx-1 is a peptide-based NaV1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 demonstrates potent inhibitory activity against the NaV1.7 channel with an IC50 value of 10 nM, while exhibiting excellent selectivity for NaV1.4 (IC50 = 0.301 μM) and NaV1.5 (IC50 = 4.20 μM), showing >20-fold and >950-fold selectivity respectively.
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Nav1.7-IN-23
0 ImagesCat. No.: HY-189066CAS No.: 3138159-82-4Nav1.7-IN-23 is an orally active, selective NaV1.7 inhibitor. Nav1.7-IN-23 exhibits electrophysiological regulatory effects in mouse dorsal root ganglion neurons. Nav1.7-IN-23 can be used for the research of acute pain, chronic inflammatory pain and neuropathic pain.
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Onzotrigine
0 ImagesCat. No.: HY-186303CAS No.: 2834099-10-2Synonyms: LTG-001Onzotrigine (LTG-001) is a potent, selective, voltage-gated sodium channel Nav1.8 inhibitor. Onzotrigine may be used in pain-related research.
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Nav1.8-IN-24
0 ImagesCat. No.: HY-183709Nav1.8-IN-24 is a voltage-gated sodium channel Nav1.8 inhibitor with pIC50 values of 7.4 (resting state) and 7.5 (inactivated state), and it exhibits high selectivity for NaV1.1-1.7 subtypes. Nav1.8-IN-24 possesses in vitro safety and drug interaction profiles. Nav1.8-IN-24 can be used for the research of acute pain and chronic neuropathic pain.
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Nav1.8-IN-22
0 ImagesCat. No.: HY-181615CAS No.: 2966089-13-2Nav1.8-IN-22 (Formula I) is a Nav1.8 sodium channel inhibitor. Nav1.8-IN-22 regulates sodium channel activity by directly binding to Nav1.8. Nav1.8-IN-22 is applicable for pain-related research.
