NS 8593 (hydrochloride)

NS 8593 is an inhibitory gating modifier of small-conductance calcium-activated potassium (KCa2/SK) channels (Kds = 0.42, 0.6, and 0.73 µM for KCa2.1/SK1, KCa2.2/SK2, and KCa2.3/SK3, respectively, in the presence of calcium) that decreases the calcium sensitivity of SK channels. It is selective for KCa2/SK channels over intermediate- (KCa3.1/IKCa1) and large-conductance (BK) potassium channels at 10 µM. NS 8593 induces relaxation of potassium- or acetylcholine chloride-precontracted isolated tracheal rings from wild-type mice (IC50s = 8.9 and 39.8 µM, respectively) or from mice in an ovalbumin-induced model of allergic asthma (IC50s = 16.4 and 32.2 µM, respectively). It inhibits aerosolized acetylcholine chloride-induced increases in respiratory system resistance in mice when administered as an aerosol at a dose of 500 µM. NS 8593 (5 mg/kg) decreases the duration of burst-pacing-induced atrial fibrillation in normotensive and spontaneously hypertensive rats.Formal Name: N-[(1R)-1,2,3,4-tetrahydro-1-naphthalenyl]-1H-benzimidazol-2-amine, monohydrochloride. CAS Number: 875755-24-1. Molecular Formula: C17H17N3 . HCl. Formula Weight: 299.8. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 100 mM, Ethanol: 20 mM. SMILES: C1(C=CC=C2)=C2CCC[C@H]1NC3=NC4=C(C=CC=C4)N3.Cl. InChi Code: InChI=1S/C17H17N3.ClH/c1-2-8-13-12(6-1)7-5-11-14(13)18-17-19-15-9-3-4-10-16(15)20-17,/h1-4,6,8-10,14H,5,7,11H2,(H2,18,19,20),1H/t14-,/m1./s1. InChi Key: VWEKCDTXUUPBNA-PFEQFJNWSA-N.