Rimtuzalcap 是首创的,选择性的小电导钙激活钾通道 (SK通道) 正变构调节剂。Rimtuzalcap 可用于运动障碍的研究,包括脊髓小脑性共济失调 (SCA)和特发性震颤 (ET)。
产品描述
Rimtuzalcap (CAD-1883) is a first-in-class selective positive allosteric modulator of small-conductance calcium-activated potassium channels (SK channels). Rimtuzalcap can be used for the research of movement disorders including spinocerebellar ataxia (SCA) and essential tremor (ET).
体外活性
Rimtuzalcap (Compound 1) is a small molecule modulator of potassium ion channels. It shows great therapeutic potential for treating a variety of diseases characterized by dysfunction of potassium ion channels and dysfunction from other causes which influence these potassium channels[1].
体内活性
Rimtuzalcap (CAD-1883) reduces the firing rate of Purkinje cells by approximately 40% which is consistent with the anticipated therapeutic mechanism of positive allosteric modulation of SK channels. Sequential bath application of 1 or 3 μM CAD-1883 results in a partial reversal of the increased coefficient of variation of the interspike interval which is seen in cerebellar slices from 11-month-old spinocerebellar ataxia-2 58Q mice[1].
Cas No.
2167246-24-2
分子式
C18H24F2N6O
分子量
378.428
别名
CAD-1883
储存和溶解度
DMSO:250mg/mL (660.64mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years