1. Metabolic Enzyme/Protease
  2. Proteasome
  3. Alicapistat

Alicapistat (Synonyms: ABT-957)

目录号: HY-109001 纯度: ≥98.0%
产品使用指南

Alicapistat (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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Alicapistat Chemical Structure

Alicapistat Chemical Structure

CAS No. : 1254698-46-8

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10 mg ¥12000
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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD)[1]. 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 calpains 1)[2].

体外研究
(In Vitro)

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. Alicapistat (compound 22) (100 nM) prevents Aβ oligomer-induced deficits in synaptic transmission in rat[2].
Alicapistat (compound 22) (385 nM) displays efficacy with respect to prevention of NMDA-induced neurodegeneration and A-induced synaptic dysfunction in rat hippocampal slice cultures[2].
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)

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 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 Clinical Trial
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
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (115.34 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3068 mL 11.5340 mL 23.0681 mL
5 mM 0.4614 mL 2.3068 mL 4.6136 mL
10 mM 0.2307 mL 1.1534 mL 2.3068 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 4.17 mg/mL (9.62 mM); Clear solution

    此方案可获得 ≥ 4.17 mg/mL (9.62 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 41.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.77 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

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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产品名称:
Alicapistat
目录号:
HY-109001
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