Zandatrigine
Based on 1 publication(s) in Google Scholar
Zandatrigine (NBI-921352; XEN901) is a selective, orally active, voltage-gated sodium channel NaV1.6/SCN8A inhibitor that can penetrate the blood-brain barrier. Zandatrigine inhibits sodium influx by non-covalently binding to the VSD4 structure of NaV1.6, blocking the persistent and resuscitative currents under pathological conditions. Zandatrigine can reduce neuronal hyperexcitability and reduce epileptic seizures. Zandatrigine is 134-756-fold selective for other isoforms such as NaV1.1 and NaV1.2, and has minimal effect on NaV1.1 expressed by inhibitory interneurons. Zandatrigine can be used to study NaV1.6-mediated neuroexcitability diseases such as SCN8A-related developmental epileptic encephalopathy (SCN8A-DEE) and adult focal epilepsy.
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- Purity: 99.28%
- CAS No.: 2154406-04-7
- 화학식: C22H25FN4O2S2
- 분자량:460.59
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Zandatrigine
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Biological Activity
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NaV1.6/SCN8A |
Zandatrigine significantly inhibits persistent sodium current (INaP) in HEK293 cells expressing NaV1.6, with IC50 of 0.051 μM and 0.058 μM for hNaV1.6 and mNaV1.6, respectively; while the IC50 for hNaV1.1, hNaV1.2, mNaV1.1, and NaV1.2 are 39 μM, 6.9 μM, 709 μM, and 191 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells stably expressing human Nav1.6
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Concentration:0.01, 0.1, 1 μM
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Incubation Time:24 h
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Result:Whole-cell patch-clamp recordings showed a concentration-dependent inhibition of INaP.
The IC50 value was determined to be 0.051 μM. Western blot analysis indicated no significant change in Nav1.6 protein expression levels.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Scn8aN1768D/+ mice (C57BL/6 background, F7 spring, 35-42 days old) with genetic epilepsy[1]
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Dosage:15 mg/kg, 10 mL/kg
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Administration:Oral gavage, daily for 3 weeks
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Result:Significantly reduced GTC seizures induced by electrical stimulation.
Showed the brain EC50 of 0.064 μM.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2154406-04-7
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Appearance Solid
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분자량 460.59
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화학식 C22H25FN4O2S2
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Color White to light yellow
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SMILES
CN([C@@H]1CN(CC1)CC2=CC=CC=C2)C3=C(C=C(C(F)=C3)S(NC4=CSC=N4)(=O)=O)C
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Synonyms
NBI-921352; XEN901
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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J Biol Chem
TET1 participates in oxaliplatin-induced neuropathic pain by regulating microRNA-30b/Nav1.6. [Abstract]2025 Mar;301(3):108228. PMID: 39864621
용액&용해도
DMSO : 125 mg/mL (271.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Bialer M, et al. Progress report on new antiepileptic drugs: A summary of the Fourteenth Eilat Conference on New Antiepileptic Drugs and Devices (EILAT XIV). I. Drugs in preclinical and early clinical development. Epilepsia. 2018 Oct;59(10):1811-1841. [Content Brief]
[2]. Johnson JP, et al. Epileptogenic Channelopathies Guide Design of NBI-921352, a Highly Isoform-Selective Inhibitor of NaV1.6. In: Noebels JL, Avoli M, Rogawski MA, Vezzani A, Delgado-Escueta AV, editors. Jasper's Basic Mechanisms of the Epilepsies. 5th ed. New York: Oxford University Press; 2024. Chapter 72. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1711 mL | 10.8556 mL | 21.7113 mL | 54.2782 mL |
| 5 mM | 0.4342 mL | 2.1711 mL | 4.3423 mL | 10.8556 mL | |
| 10 mM | 0.2171 mL | 1.0856 mL | 2.1711 mL | 5.4278 mL | |
| 15 mM | 0.1447 mL | 0.7237 mL | 1.4474 mL | 3.6185 mL | |
| 20 mM | 0.1086 mL | 0.5428 mL | 1.0856 mL | 2.7139 mL | |
| 25 mM | 0.0868 mL | 0.4342 mL | 0.8685 mL | 2.1711 mL | |
| 30 mM | 0.0724 mL | 0.3619 mL | 0.7237 mL | 1.8093 mL | |
| 40 mM | 0.0543 mL | 0.2714 mL | 0.5428 mL | 1.3570 mL | |
| 50 mM | 0.0434 mL | 0.2171 mL | 0.4342 mL | 1.0856 mL | |
| 60 mM | 0.0362 mL | 0.1809 mL | 0.3619 mL | 0.9046 mL | |
| 80 mM | 0.0271 mL | 0.1357 mL | 0.2714 mL | 0.6785 mL | |
| 100 mM | 0.0217 mL | 0.1086 mL | 0.2171 mL | 0.5428 mL |
Zandatrigine Related Classifications
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