Nav1.2
NaV1.2, encoded by SCN2A, is a neuronal voltage-gated sodium channel that supports action-potential initiation and propagation in developing excitatory cortical neurons[1]. Mechanistically, NaV1.2 contributes to axonal excitability during early development, while later studies show roles in dendritic excitability, synaptic strength, and synaptic plasticity in mature pyramidal neurons[2]. In disease models, SCN2A variants associate with autism spectrum disorder, developmental delay, intellectual disability, and epilepsy, with gain-of-function variants linked to infantile seizures and loss-of-function variants linked to autism-related phenotypes[1][3]. Compared with related isoforms, NaV1.2 differs from NaV1.6 because NaV1.6 replaces NaV1.2 in the distal axon initial segment during maturation and has a lower activation threshold[1][2]. NaV1.2 also differs from NaV1.1 because NaV1.2 is robustly expressed in glutamatergic neurons, whereas NaV1.1 is dominantly expressed in parvalbumin-positive GABAergic neurons[3]. For experimental applications, cannabidiol preferentially inhibited resurgent hNaV1.2 current, and GS967 preferentially inhibited persistent hNaV1.2 current in HEK cells expressing wild-type hNaV1.2[4].
References:
- [1]. Yarnell S, et al. Scanning for Justice With Functional Magnetic Resonance Imaging. Biol Psychiatry. 2017 Aug 15;82(4):e23-e24. [Content Brief]
- [2]. Huang L, et al. A visual circuit related to habenula underlies the antidepressive effects of light therapy. Neuron. 2019;102(1):128-142.e8.
- [3]. Ogiwara I, et al. Nav1.2 haplodeficiency in excitatory neurons causes absence-like seizures in mice. Commun Biol. 2018;1:96. [Content Brief]
- [4]. Mason ER, et al. Differential Inhibition of Human Nav1.2 Resurgent and Persistent Sodium Currents by Cannabidiol and GS967. Int J Mol Sci. 2020 Apr 1;21(7):2454. [Content Brief]
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Nav1.2 Related Products (25)
Related Products (25)
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PF-06456384 trihydrochloride
0 ImagesPF-06456384 trihydrochloride is an extremely potent and selective Nav1.7 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.
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XPC-5462
0 ImagesXPC-5462 is a selective NaV1.6/1.2 inhibitor, with an IC50 of 0.0103 μM against hNaV1.6, 0.0137 μM against mNaV1.6, and 0.0109 μM against hNaV1.2. XPC-5462 significantly reduces epileptiform discharges. XPC-5462 is applicable for epilepsy-related research.
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GDC-0310
0 ImagesGDC-0310 is a selective acyl-sulfonamide Nav1.7 inhibitor, with an IC50 of 0.6 nM for hNav1.7.
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Funapide
0 ImagesSynonyms: TV 45070; XEN402Funapide (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.
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AA43279
0 ImagesAA43279 is an orally effective, blood-brain barrier-penetrant Nav1.1 voltage-gated sodium channel activator with an EC50 of 9.5 μM in HEK-293 cells. AA43279 inhibits fast inactivation and enhances sodium conductance. AA43279 can be used in research on schizophrenia and Dravet syndrome.
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Nav1.2-IN-4
0 ImagesCat. No.: HY-189470Nav1.2-IN-4 is a blood-brain barrier-penetrant NaV1.2 inhibitor (IC50 = 31.21 μM). Nav1.2-IN-4 preferentially blocks the inactivated state of the neuronal voltage-gated sodium channel NaV1.2, inhibiting persistent and resurgent sodium currents associated with epileptogenesis. Nav1.2-IN-4 restores the GABA-glutamate balance by enhancing GABA and reducing glutamate. Nav1.2-IN-4 reduces oxidative stress in brain tissue by increasing GSH and decreasing MDA. Nav1.2-IN-4 protects mice against MES-induced tonic hindlimb extensor seizures and attenuates hippocampal neuronal degeneration in the PTZ kindling model. Nav1.2-IN-4 can be used for research on epilepsy.
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AMPAR/Nav1.2-IN-1
0 ImagesCat. No.: HY-189650AMPAR/Nav1.2-IN-1 is a blood-brain barrier-penetrant AMPAR inhibitor and Nav1.2 blocker with IC50 values of 12.7 and 7.01 μM, respectively. AMPAR/Nav1.2-IN-1 inhibits AMPA-mediated excitatory currents and neuronal Nav1.2 voltage-gated sodium channels. AMPAR/Nav1.2-IN-1 scavenges free radicals via HAT and SET, increases GSH and SOD while decreasing MDA, and restores GABA-glutamate homeostasis by attenuating glutamate elevation and increasing GABA. AMPAR/Nav1.2-IN-1 can be used for epilepsy research.
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NaV1.2/1.6 channel blocker-1
0 ImagesCat. No.: HY-152166CAS No.: 1199944-04-1NaV1.2/1.6 channel blocker-1 is a potent NaV1.2/1.6 channel blocker, with IC50s of 9.8 and 24.4 μM for rNaV1.6 and hNaV1.2, respectively. NaV1.2/1.6 channel blocker-1 can be used for the research of generalized epilepsy.
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XPC-6444
0 ImagesXPC-6444 is a highly potent, isoform-selective, and CNS-penetrant NaV1.6 inhibitor (IC50=41 nM for hNaV1.6). XPC-6444 also displays potent block of NaV1.2 (IC50=125 nM). XPC-6444 shows anticonvulsant activity.
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Huwentoxin-IV TFA
0 ImagesCat. No.: HY-P1220APurity: 99.18%Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain.
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ProTx-I
0 ImagesProTx-I is a toxin derived from Thrixopelma pruriens and a peptide inhibitor targeting TTX-resistant sodium channels. ProTx-I interacts with voltage sensors of multiple domains such as NaV1.7, reduces neuronal excitability through allosteric modulation of channel gating and alteration of voltage dependence. The IC50 values of ProTx-I against human NaV1.7, NaV1.2, NaV1.6, and NaV1.5 are 95 nM, 104 nM, 21 nM, and 358 nM, respectively; ProTx-I also potently inhibits Ba2+ currents of hCav3.1, while its inhibitory potency against hCav3.2 is approximately 160-fold lower. ProTx-I is applicable to the research of chronic pain.
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Phrixotoxin 3
0 ImagesCat. No.: HY-P1218CAS No.: 880886-00-0Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
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Anticonvulsant agent 9
0 ImagesCat. No.: HY-170930Anticonvulsant agent 9 (compound 4f) is an α1β2γ2 GABAA receptors activator. Anticonvulsant agent 9 activatesα1β2γ2 GABAA receptors with an EC50 of 1.24 μM. Anticonvulsant agent 9 inhibits the inactivation of Nav1.2 channels. Anticonvulsant agent 9 exhibits significant anticonvulsant activities.
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Hainantoxin-III
0 ImagesCat. No.: HY-P5180CAS No.: 1809149-40-3Jingzhaotoxin-V is a peptide that inhibits potassium currents in Xenopus laevis oocytes with an IC50 value of 604.2 nM. Jingzhaotoxin-V also inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC50 values of 27.6 and 30.2 nM, 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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Nav1.2-IN-1
0 ImagesCat. No.: HY-176065CAS No.: 3084825-09-9Nav1.2-IN-1 (compound 5i), a 3-(1,2,3,6-tetrahydropyridine)-4-azaindole derivative, is a potent and selective Nav1.2 inhibitor. Nav1.2-IN-1 induces a reduction in the peak amplitude of Nav1.2 currents with an IC50 value of 7.79 μM. Nav1.2-IN-1 exhibits antiepileptic activity. Nav1.2-IN-1 shows high anticonvulsant effect and low neurotoxicity in subcutaneous Pentetrazole (sc-PTZ)-induced epilepsy mode.
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Cy3 labled Elsunersen sodium
0 ImagesCat. No.: HY-177629DCy3 labled Elsunersen sodium refers to Elsunersen sodium (HY-177629A) tagged with the fluorescent dye Cy3 (HY-D0822). Elsunersen sodium (PRAX‑222 sodium) is a gapmer antisense oligonucleotide targeting SCN2A mRNA. Elsunersen sodium reduces the protein level of the voltage-gated sodium channel NaV1.2 by degrading SCN2A mRNA, alleviating neuronal network hyperexcitability. Elsunersen sodium combined with sodium channel blockers terminates refractory status epilepticus and reduces seizure frequency. Elsunersen sodium can be used in research related to epileptic encephalopathy.
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Elsunersen sodium
0 ImagesCat. No.: HY-177629ASynonyms: PRAX-222 sodiumElsunersen sodium (PRAX‑222 sodium) is a gapmer antisense oligonucleotide targeting SCN2A mRNA. Elsunersen sodium reduces the protein level of the voltage-gated sodium channel NaV1.2 by degrading SCN2A mRNA, alleviating neuronal network hyperexcitability. Elsunersen sodium combined with sodium channel blockers terminates refractory status epilepticus and reduces seizure frequency. Elsunersen sodium can be used in research related to epileptic encephalopathy.
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Elsunersen sodium scrambled negative control
0 ImagesCat. No.: HY-177629BElsunersen sodium scrambled negative control is a scrambled negative control for Elsunersen sodium (HY-177629A). Elsunersen sodium (PRAX‑222 sodium) is a gapmer antisense oligonucleotide targeting SCN2A mRNA. Elsunersen sodium reduces the protein level of the voltage-gated sodium channel NaV1.2 by degrading SCN2A mRNA, alleviating neuronal network hyperexcitability. Elsunersen sodium combined with sodium channel blockers terminates refractory status epilepticus and reduces seizure frequency. Elsunersen sodium can be used in research related to epileptic encephalopathy.
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Elsunersen
0 ImagesCat. No.: HY-177629CAS No.: 2756001-75-7Synonyms: PRAX-222Elsunersen (PRAX‑222) is a gapmer antisense oligonucleotide targeting SCN2A mRNA. Elsunersen reduces the protein level of the voltage-gated sodium channel NaV1.2 by degrading SCN2A mRNA, alleviating neuronal network hyperexcitability. Elsunersen combined with sodium channel blockers terminates refractory status epilepticus and reduces seizure frequency. Elsunersen can be used in research related to epileptic encephalopathy.
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