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Submit ReviewC 101248 is a selective and potent inhibitor of both mouse and human tandem pore domain halothane-inhibited K+ channel 1 (THIK-1, IC50 = 50 nM); it exhibits no activity against K2P family members, TREK-1 and TWIK-2, and Kv2.1. C 101248 blocks both tonic and ATP-evoked THIK-1 K+ currents in whole-cell patch-clamp recordings of mouse hippocampal microglia. C 101248 reduces neuroinflammation by preventing NLRP3-dependent release of IL-1β in isolated microglia.
M. Wt | 292.3 |
Formula | C15H12N6O |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 361368-24-3 |
PubChem ID | 723233 |
InChI Key | LXADAVBNVFYEBW-UHFFFAOYSA-N |
Smiles | NC1=NON=C1C2=NC3=CC=CC=C3N2CC4=CC=NC=C4 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 29.23 | 100 |
The following data is based on the product molecular weight 292.3. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.42 mL | 17.11 mL | 34.21 mL |
5 mM | 0.68 mL | 3.42 mL | 6.84 mL |
10 mM | 0.34 mL | 1.71 mL | 3.42 mL |
50 mM | 0.07 mL | 0.34 mL | 0.68 mL |
References are publications that support the biological activity of the product.
Ossola et al (2022) Characterisation of C101248: a novel selective THIK-1 channel inhibitor for the modulation of microglial NLRP3-inflammasome. Neuropharmacology 224 109330 PMID: 36375694
If you know of a relevant reference for C 101248, please let us know.
Keywords: C 101248, C 101248 supplier, C101248, tandem, pore, domain, halothane-inhibited, K+, channel, 1, inhibitor, inhibits, THIK-1, KCNK13, THIK1, potassium, potent, selective, NLRP3, IL1b, IL1beta, Two-P, Potassium, Channels, 8007, Tocris Bioscience
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