SKA-121 是一种选择性的 K_Ca3.1 激活剂。SKA-121 作用于 K_Ca3.1 和 K_Ca2.3，EC₅₀ 分别为 109 nM 和 4.4 μM。

SKA-121 is a selective K Ca 3.1 activator. SKA-121 exhibits EC 50 s of 109 nM and 4.4 μM for K Ca 3.1 and K Ca 2.3, respectively.

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EC50: 109 nM (KCa3.1), 4.4 μM (KCa2.3)

SKA-121, a compound generated through an isosteric replacement approach. SKA-121 is a typical positive-gating modulator and shifts the calcium-concentration response curve of KCa3.1 to the left. SKA-121 displays 41-fold selectivity for KCa3.1 (EC50 109 nM±14 nM) over KCa2.3 (EC50 4.4 ± 1.6 μM). SKA-121 is 200- to 400-fold selective over representative KV (KV1.3, KV2.1, KV3.1, and KV11.1), NaV (NaV1.2, NaV1.4, NaV1.5, and NaV1.7), as well as CaV1.2 channels. has not independently confirmed the accuracy of these methods. They are for reference only.

In blood pressure telemetry experiments, SKA-121 (100 mg/kg i.p.) significantly lowers mean arterial blood pressure in normotensive and hypertensive wild-type but not in K Ca 3.1 mice. SKA-121 can be used as a new K Ca 3.1 selective pharmacological tool compound despite its relatively short half-life in mice. A lower dose of 30 mg/kg of SKA-121 does not produce significant alterations in MAP. The vehicle, peanut oil/DMSO (9:1 v/v, for SKA-121), does not cause significant alterations in MAP or HR. SKA-121 has a short half-life (~20 minutes), and plasma decay is extremely rapid (21.3±2.4 μM at 5 minutes; 483±231 nM at 1 hour and 53±44 nM at 4 hours). Since SKA-121 is relatively well soluble (logP=1.79) and can potentially be added to drinking water in animal experiments, it orally is also administered, and find that it has an oral availability of roughly 25%.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Coleman N, et al. New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1. Mol Pharmacol. 2014 Sep;86(3):342-57.

In Vitro: DMSO : ≥ 42.86 mg/mL (216.22 mM)配制储备液