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(1S,2R)-Alicapistat

CAS No. : 2221010-57-5

MCE 站：(1S,2R)-Alicapistat

产品活性：(1S,2R)-Alicapistat ((1S,2R)-ABT-957) 是一种具有口服活性的人钙激活中性蛋白酶 (calpains 1 和 2) 的选择性抑制剂，可能用于阿尔茨海默病 (AD) 的研究。 Alicapistat 可减轻羰基还原的代谢倾向，对 calpain 1 的 IC₅₀ 为 395 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Proteasome

In Vitro: (1S,2R)-Alicapistat exihibits inadequate CNS-penetration concentrations to obtain a pharmacodynamic effect.
Calpain 1 (-calpain) ａnd 2 (m-calpain) expression in a calcium-dependent manner with -molar or m-molar calcium concentrations required for their respective activation, respectively. (1S,2R)-Alicapistat (compound 22) (100 nM) prevents Aβ oligomer-induced deficits in synaptic transmission in rat.
(1S,2R)-Alicapistat (compound 22) (385 nM) diplays efficacy with respect to prevention of NMDA-induced neurodegeneration ａnd A-induced synaptic dysfunction.
(1S,2R)-Alicapistat (9-21 nM) has the CSF concentrations without reaching the IC₅₀ for calpain inhibition ａnd shows no dose-limiting toxicities (DLTs) in the broad populations studies.

In Vivo: (1S,2R)-Alicapistat (compound 22) (iv or po; 1-3 mg/kg) shows moderate mean plasma clearance values (CLp) in mouse, rat, ａnd dog (0.13-1.04 L/hr.kg), while high in monkey (1.98 L/hr.kg). Mean steady-state volume of distribution values (Vss) were moderate in mouse, dog, ａnd monkey (0.64-1.8 L/kg), but higher in rat (3.4 L/kg). The plasma elimination half-life (t_1/2) was shortest in dog (1.7 hours), followed by 2.3 hours in monkey ａnd approximately 6.0 hours in mouse ａnd rat. Oral bioavailability (F) values were high in mouse, rat, ａnd dog (>80%), while moderate in monkey (14%).

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