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(1S,2R)-Alicapistat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(1S,2R)-Alicapistat图片
CAS NO:2221010-57-5
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议

产品介绍
(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。

产品描述

(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 with the potential application of Alzheimer's disease (AD) [1]. (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC 50 value of 395 nM [2].

体外活性

(1S,2R)-Alicapistat shows inadequate CNS-penetration concentrations to obtain a pharmacodynamic effect [1]. Calpain 1 (μ-calpain) and 2 (m-calpain) expression in a calcium-dependent manner with μ-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 [2]. (1S,2R)-Alicapistat (compound 22) (385 nM) diplays efficacy with respect to prevention of NMDA-induced neurodegeneration and A-induced synaptic dysfunction [2]. (1S,2R)-Alicapistat (9-21 nM) has the CSF concentrations without reaching the IC 50 for calpain inhibition and shows no dose-limiting toxicities (DLTs) in the broad populations studies [3].

体内活性

(1S,2R)-Alicapistat (compound 22) (iv or po; 1-3 mg/kg) exhibits moderate average 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%) [2].

Cas No.

2221010-57-5

分子式

C25H27N3O4

分子量

433.5

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years