ARN 23746 (ARN-23746) is a potent, selective inhibitor of Na+-K+-Cl- importer NKCC1, shows NKCC1 inhibition 31.8% at 10 uM, and 95.2% at 100 uM in the Cl− influx assay on NKCC1-transfected HEK293 cells.ARN23746 did not show significant NKCC2 inhibition and KCC2 inhibition at 10 uM.ARN23746 selectively blocks NKCC1 in a human cell line and restore the physiological [Cl−]i in murine DS neurons in culture, has excellent solubility and metabolic stability, and displays no issues with off-target activity in vitro.ARN23746 demonstrated in vivo efficacy in rescuing cognitive impairment in a DS mouse model and social deficits and repetitive behaviors in an autism mouse model.
Cat.No
DC70203
Name
ARN23746
Chemical Properties
CAS
2497525-96-7
Formula
C17H25F3N2O4S
MW
410.452
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
1. Savardi A, et al. Chem. 2020 Aug 6;6(8):2073-2096. 2. Borgogno M, et al. J Med Chem. 2021 Jul 22;64(14):10203-10229
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