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 (16)
Related Products (16)
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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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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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AA43279
0 ImagesAA43279 is an in gamma-aminobutyric acid (GABA) fast-firing interneurons located activator for Nav1.1 channel (SCN1A) with an EC50 of 9.5 μM. AA43279 enhances specific neuronal firing activity in vitro, and exhibits anticonvulsant activity in rat MEST model.
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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 ImagesCat. No.: HY-P1073CAS No.: 484598-35-8ProTx-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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Nav1.2-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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Huwentoxin-IV
0 ImagesCat. No.: HY-P1220CAS No.: 526224-73-7Huwentoxin-IV 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 preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain.
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Ceratotoxin-1
0 ImagesCat. No.: HY-P5811Synonyms: CcoTx1; β-TRTX-cm1aCeratotoxin-1 (CcoTx1), a peptide toxin, is an voltage-gated sodium channel subtypes inhibitor. Ceratotoxin-1 inhibits Nav1.1/β1, Nav1.2/β1, Nav1.4/β1, and Nav1.5/β1 with IC50 of 523 nM, 3 nM, 888 nM, and 323 nM, respectively. Ceratotoxin-1 also inhibits Nav1.8/β1.
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Nav1.2-IN-2
0 ImagesNav1.2-IN-2 is a Nav1.2 inhibitor with a human IC50 of 0.18 μM. Nav1.2-IN-2 preferentially binds to the inactivated state of Nav1.2, reduces window current, suppresses neuronal depolarization and action potential generation. Nav1.2-IN-2 suppresses Veratridine (HY-N6691)-induced Ca2+ influx. Nav1.2-IN-2 can be used for the research of epilepsy.
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