SKA-121

SKA-121 is a positive-gating modulator of intermediate-conductance calcium-activated potassium channels (IKCa1/KCa3.1) with an EC50 value of 109 nM using whole-cell patch-clamp electrophysiology with calcium in the internal solution. It is selective for KCa3.1 over KCa2.1, KCa2.2 and KCa2.3 (EC50s = 8,700, 6,800, and 4,400 nM, respectively). It is also selective over KCa1.1 as well as voltage-gated potassium and sodium channels. SKA-121 (1 µM) potentiates calcium-evoked KCa currents by approximately 7-fold using whole-cell patch-clamp electrophysiology, an effect that can be blocked by the KCa3.1 inhibitor TRAM-34 (Cay-23385). It also potentiates calcium-evoked and basal KCa currents. In large porcine coronary arteries ex vivo, SKA-121 potentiates bradykinin-induced endothelium-dependent relaxation (EC50 = 7.9 nM). It also lowers mean arterial blood pressure (MAP) by approximately 20 and 25 mm Hg in normo- and hypertensive mice when used at a dose of 100 mg/kg but has no effect on MAP in KCa3.1 knockout mice.Formal Name: 5-methyl-naphth[2,1-d]oxazol-2-amine. CAS Number: 1820708-73-3. Molecular Formula: C12H10N2O. Formula Weight: 198.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 50 mg/ml, DMSO: 50 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 10 mg/ml. lambdamax: 253 nm. SMILES: CC1=CC2=C(OC(N)=N2)C3=CC=CC=C13. InChi Code: InChI=1S/C12H10N2O/c1-7-6-10-11(15-12(13)14-10)9-5-3-2-4-8(7)9/h2-6H,1H3,(H2,13,14). InChi Key: JEGUERWMMMQFJV-UHFFFAOYSA-N.