| Identification | Back Directory | [Name]
XPC-6444 | [CAS]
2230144-21-3 | [Synonyms]
XPC-6444
https://pubmed.ncbi.nlm.nih.gov/34355886/ | [Molecular Formula]
C22H25F3N4O2S2 | [MDL Number]
MFCD32263401 | [MOL File]
2230144-21-3.mol | [Molecular Weight]
498.58 |
| Chemical Properties | Back Directory | [Boiling point ]
574.8±60.0 °C(Predicted) | [density ]
1.384±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 125 mg/mL (250.71 mM; Need ultrasonic) | [form ]
Solid | [pka]
5.73±0.10(Predicted) | [color ]
Off-white to yellow |
| Hazard Information | Back Directory | [Uses]
XPC-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[1]. | [Biological Activity]
XPC-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[1].
XPC-6444 shows high selectivity over NaV1.1 and NaV1.5[1].
XPC-6444 exhibits good metabolic stability in human liver microsomes and hepatocytes, and low potential for MDR1 mediated efflux[1]. | [in vivo]
XPC-6444 exhibits good metabolic stability in human liver microsomes and hepatocytes, and low potential for MDR1 mediated efflux[1]. | [IC 50]
hNav1.6: 41 nM (IC50); Nav1.2: 125 nM (IC50) | [References]
[1]. Focken T, et al. Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective NaV1.6 Inhibitors with Efficacy in Mouse Models of Epilepsy. J Med Chem. 2019 Oct 3. |
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| Company Name: |
Biorbyt Ltd.
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| Tel: |
+44 (0)1223 859 353 |
| Website: |
http://www.biorbyt.com |
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