1. Metabolic Enzyme/Protease
  2. Proteasome
  3. (1S,2R)-Alicapistat

(1S,2R)-Alicapistat (Synonyms: (1S,2R)-ABT-957)

目录号: HY-109001A
产品使用指南

(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 12) 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 1IC50 为 395 nM。

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(1S,2R)-Alicapistat Chemical Structure

(1S,2R)-Alicapistat Chemical Structure

CAS No. : 2221010-57-5

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生物活性

(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for 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 IC50 value of 395 nM[2].

IC50 & Target

IC50: 395 nM (human calpain 1)[1]

体外研究
(In Vitro)

(1S,2R)-Alicapistat exihibits 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 IC50 for calpain inhibition and shows no dose-limiting toxicities (DLTs) in the broad populations studies[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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 (t1/2) 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Pharmacokinetics of (1S,2R)-Alicapistat in preclincial species following a single IV or PO dose[2]
Dosage:
Administration:
Result:
IV PO
species dose t1/2 AUC0-inf CLp Vss dose t1/2 AUC0-inf CLp F
mouse 2 6.0 15.45 0.13 1.0 分子量

433.50

Formula

C25H27N3O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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(1S,2R)-Alicapistat
目录号:
HY-109001A
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