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C101248

Chemical Structure : C101248

CAS No.: 361368-24-3

C101248 (C 101248)

Catalog No.: PC-49461Not For Human Use, Lab Use Only.

C101248 is the first selective small-molecule inhibitor of tandem pore domain halothane-inhibited K+ channel 1 (THIK-1) with IC50 of 50 nM for both mouse and human THIK-1.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

C101248 is the first selective small-molecule inhibitor of tandem pore domain halothane-inhibited K+ channel 1 (THIK-1) with IC50 of 50 nM for both mouse and human THIK-1.
C101248 is selective for THIK-1 and is inactive against K2P family members TREK-1 and TWIK-2, and Kv2.1.
C101248 potently blocked both tonic and ATP-evoked THIK-1 K+ currents in whole-cell patch-clamp recordings of microglia from mouse hippocampal slices.
C101248 had no effect on other constitutively active resting conductance in slices from THIK-1-depleted mice.
C101248 attenuated the NLRP3-dependent release of IL-1β from microglia.

Physicochemical Properties

M.Wt 292.302
Formula C15H12N6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(1-(pyridin-4-ylmethyl)-1H-benzo[d]imidazol-2-yl)-1,2,5-oxadiazol-3-amine

References

1. Bernardino Ossola, et al. Neuropharmacology. 2022 Nov 11;109330

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