XPC-6444
Based on 1 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 98.93
- CAS No.: 2230144-21-3
- Formula: C22H25F3N4O2S2
- Molecular Weight:498.58
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) XPC-6444
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Biological Activity
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hNav1.6 41 nM (IC50) |
Nav1.2 125 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10 μM
Compound: 31
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Inhibition of recombinant human full length Nav1.1 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential by whole cell patch clamp assay
Inhibition of recombinant human full length Nav1.1 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential by whole cell patch clamp assay
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[PMID: 31525968] |
| HEK293 | IC50 |
>10 μM
Compound: 31
|
Inhibition of recombinant human full length Nav1.5 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -60 mV holding potential by whole cell patch clamp assay
Inhibition of recombinant human full length Nav1.5 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -60 mV holding potential by whole cell patch clamp assay
|
[PMID: 31525968] |
| HEK293 | IC50 |
0.04 μM
Compound: 31
|
Inhibition of recombinant human full length Nav1.6 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential by whole cell patch clamp assay
Inhibition of recombinant human full length Nav1.6 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential by whole cell patch clamp assay
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[PMID: 31525968] |
| HEK293 | IC50 |
0.122 μM
Compound: 31
|
Inhibition of recombinant human full length SCN1B/Nav1.6 N1768D mutant co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -60 mV holding potential by whole cell patch clamp assay
Inhibition of recombinant human full length SCN1B/Nav1.6 N1768D mutant co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -60 mV holding potential by whole cell patch clamp assay
|
[PMID: 31525968] |
| HEK293 | IC50 |
0.125 μM
Compound: 31
|
Inhibition of recombinant human full length Nav1.2 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential by whole cell patch clamp assay
Inhibition of recombinant human full length Nav1.2 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential by whole cell patch clamp assay
|
[PMID: 31525968] |
| HEK293 | IC50 |
0.625 μM
Compound: 31
|
Inhibition of recombinant human full length Nav1.7 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -60 mV holding potential by whole cell patch clamp assay
Inhibition of recombinant human full length Nav1.7 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -60 mV holding potential by whole cell patch clamp assay
|
[PMID: 31525968] |
| HEK293 | IC50 |
26.3 μM
Compound: 31
|
Inhibition of human ERG expressed in HEK293 cells by IonWorks barracuda patch clamp method
Inhibition of human ERG expressed in HEK293 cells by IonWorks barracuda patch clamp method
|
[PMID: 31525968] |
XPC-6444 shows high selectivity over NaV1.1 and NaV1.5[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2230144-21-3
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Appearance Solid
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Molecular Weight 498.58
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Formula C22H25F3N4O2S2
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Color Off-white to yellow
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SMILES
O=S(C1=C(F)C=C(NCC2=C(F)C=CC=C2CN(C(C)(C)C)C)C=C1F)(NC3=CSC=N3)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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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bioRxiv
Automated high-throughput patch clamp electrophysiology of hiPSC-derived neuronal models. [Abstract]2025 May 15:2025.05.12.653142. PMID: 40462992
Solvent & Solubility
DMSO : 125 mg/mL (250.71 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (275 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
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 | 2.0057 mL | 10.0285 mL | 20.0570 mL | 50.1424 mL |
| 5 mM | 0.4011 mL | 2.0057 mL | 4.0114 mL | 10.0285 mL | |
| 10 mM | 0.2006 mL | 1.0028 mL | 2.0057 mL | 5.0142 mL | |
| 15 mM | 0.1337 mL | 0.6686 mL | 1.3371 mL | 3.3428 mL | |
| 20 mM | 0.1003 mL | 0.5014 mL | 1.0028 mL | 2.5071 mL | |
| 25 mM | 0.0802 mL | 0.4011 mL | 0.8023 mL | 2.0057 mL | |
| 30 mM | 0.0669 mL | 0.3343 mL | 0.6686 mL | 1.6714 mL | |
| 40 mM | 0.0501 mL | 0.2507 mL | 0.5014 mL | 1.2536 mL | |
| 50 mM | 0.0401 mL | 0.2006 mL | 0.4011 mL | 1.0028 mL | |
| 60 mM | 0.0334 mL | 0.1671 mL | 0.3343 mL | 0.8357 mL | |
| 80 mM | 0.0251 mL | 0.1254 mL | 0.2507 mL | 0.6268 mL | |
| 100 mM | 0.0201 mL | 0.1003 mL | 0.2006 mL | 0.5014 mL |