C 101248

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Description: Selective and potent inhibitor of both mouse and human THIK-1
Chemical Name: 4-[1-(4-Pyridinylmethyl)-1H-benzimidazol-2-yl]-1,2,5-oxadiazol-3-amine
Purity: ≥98% (HPLC)

Biological Activity for C 101248

C 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.

Technical Data for C 101248

M. Wt 292.3
Formula C15H12N6O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 361368-24-3
PubChem ID 723233
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.

Solubility Data for C 101248

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 29.23 100

Preparing Stock Solutions for C 101248

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.

Select a batch to recalculate based on the batch molecular weight:
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

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References for C 101248

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

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Citations for C 101248

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