SKA-121 is a potent, selective intermediate-conductance KCa3.1 positive-gating modulator with EC50 of 109 nM.
SKA-121 displays 41-fold selectivity over KCa2.3 (EC50=4.4 uM), and 200- to 400-fold selectivity over representative KV, NaV, as well as CaV1.2 channels.
SKA-121 significantly lowers mean arterial blood pressure in normotensive and hypertensive mice.
Physicochemical Properties
M.Wt
198.225
Formula
C12H10N2O
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
5-methylnaphtho[2,1-d]oxazol-2-amine
References
1. Coleman N, et al. Mol Pharmacol. 2014 Sep;86(3):342-57.
2. Christophersen P, et al. Channels (Austin). 2015;9(6):336-43.
3. Oliván-Viguera A, et al. Basic Clin Pharmacol Toxicol. 2016 Aug;119(2):184-92.
4. Brown BM, et al. Mol Pharmacol. 2017 Oct;92(4):469-480.
