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NBI-921352 free base · Synonyms: Zandatrigine | XEN901

Zandatrigine is a sodium channel protein type 8 subunit alpha blocker.

For research use only. Not for human or veterinary use.

Research area Neurological Disease
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NBI-921352 structure

CAS No.: 2154406-04-7

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
250 mg USD 580.00 BP-01976-250mg In stock Get quote
500 mg USD 928.00 BP-01976-500mg In stock Get quote
1 g USD 1,485.00 BP-01976-1g In stock Get quote

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Description

Zandatrigine (NBI-921352) is a sodium channel protein type 8 subunit alpha (Scn8α) blocker.

Biological activity

In Vitro 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. In Vivo Zandatrigine (15 mg/kg; oral; single dose, 2 hours before electrical epilepsy induction) significantly reduces the incidence of electric shock-induced generalized tonic-clonic seizures (GTCs) in the Scn8aN1768D/+ gene mutant mouse model, with an ED50 of 15 mg/kg, with a positively correlated concentration in the brain with the therapeutic effect.

Identifiers

SMILES
CN([C@@H]1CN(CC1)CC2=CC=CC=C2)C3=C(C=C(C(F)=C3)S(NC4=CSC=N4)(=O)=O)C
InChIKey
UCSHINHOAVARGQ-SFHVURJKSA-N

Specifications

MW (average)
460.5880
Formula
C22H25FN4O2S2
CAS No.
2154406-04-7
Physical state
Solid
Color
White to light yellow
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO : 125 mg/mL

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.
[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.

Same target

Search Sodium Channel

Same research area

Search Neurological Disease