ns13001

NS13001 is a potent, selective, orally active allosteric positive modulator of small conductance calcium‐activated potassium channels (SK channels), specifically targeting the SK2 (KCa2.2) and SK3 (KCa2.3) subtypes with high selectivity and efficacy. It has EC50 values of approximately 1.6–1.8 μM for SK2 and 0.14 μM for SK3, showing much less activity on SK1 or intermediate-conductance K+ channels even at higher concentrations[1][4][7]. NS13001 enhances channel activity by binding allosterically to these targets, thereby increasing their open probability in response to intracellular calcium without affecting voltage dependence[4]. This mechanism is relevant for regulating neuronal excitability and firing patterns in the central nervous system[8]. NS13001 has been investigated as a potential therapeutic agent for spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias due to its neuroprotective effects on Purkinje cell function[3][4].

Other names

N-(4-chlorophenyl)-2-(3,5-dimethyl-1H-pyrazol-1-yl)-9-methyl-9H-purin-6-amine