XPC-6444

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 555652

CAS#: Unknown

Description: XPC-6444 is a highly potent inhibitors of NaV1.6 with high selectivity over NaV1.1 and NaV1.5. XPC-6444 provided excellent anticonvulsant activity and reduced seizure activity in a dose-dependent manner in an induced seizure model, which utilized SCN8A GOF mice carrying the N1768D mutation identified in a human EIEE13 patient.


Price and Availability

Size
Price

Size
Price

Size
Price

XPC-6444 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

img

Theoretical Analysis

MedKoo Cat#: 555652
Name: XPC-6444
CAS#: Unknown
Chemical Formula: C22H25F3N4O2S2
Exact Mass: 498.1371
Molecular Weight: 498.5832
Elemental Analysis: C, 53.00; H, 5.05; F, 11.43; N, 11.24; O, 6.42; S, 12.86


Synonym: XPC-6444; XPC 6444; XPC6444;

IUPAC/Chemical Name: 4-((2-((tert-Butyl(methyl)amino)methyl)-6-fluorobenzyl)amino)-2,6-difluoro-N-(thiazol-4-yl)benzenesulfonamide

InChi Key: VOJFVKGTRNXOTJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H25F3N4O2S2/c1-22(2,3)29(4)11-14-6-5-7-17(23)16(14)10-26-15-8-18(24)21(19(25)9-15)33(30,31)28-20-12-32-13-27-20/h5-9,12-13,26,28H,10-11H2,1-4H3

SMILES Code: O=S(C1=C(F)C=C(NCC2=C(F)C=CC=C2CN(C(C)(C)C)C)C=C1F)(NC3=CSC=N3)=O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
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 Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>3 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
2934.99.90.01


Additional Information

Nonselective antagonists of voltage-gated sodium (NaV) channels have been long used for the treatment of epilepsies. The efficacy of these drugs is thought to be due to the block of sodium channels on excitatory neurons, primarily NaV1.6 and NaV1.2. However, these currently marketed drugs require high drug exposure and suffer from narrow therapeutic indices. Selective inhibition of NaV1.6, while sparing NaV1.1, is anticipated to provide a more effective and better tolerated treatment for epilepsies. In addition, block of NaV1.2 may complement the anticonvulsant activity of NaV1.6 inhibition.


References

Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective NaV1.6 Inhibitors with Efficacy in Mouse Models of Epilepsy
Thilo Focken*Kristen BurfordMichael E. GrimwoodAlla ZenovaJean-Christophe AndrezWei GongMichael WilsonMatt TaronShannon DeckerVerner LofstrandSultan ChowdhuryNoah ShuartSophia LinSamuel J. GoodchildClint YoungMaegan SorianoParisa K. TariMatthew WaldbrookKaren NelkenbrecherRainbow KwanAndrea LindgrenGina de BoerStephanie LeeLuis SojoRobert J. DeVitaCharles J. CohenSteven S. WesolowskiJ. P. Johnson Jr.Christoph M. DehnhardtJames R. Empfield
Journal of Medicinal Chemistry, Articles ASAP (As Soon As Publishable)Subscribed Access
Publication Date (Web):September 17, 2019