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

Alicapistat  (Synonyms: ABT-957)

Cat. No.: HY-109001 Purity: ≥98.0%
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Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD). Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM.

For research use only. We do not sell to patients.

Alicapistat Chemical Structure

Alicapistat Chemical Structure

CAS No. : 1254698-46-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 825 In-stock
Solution
10 mM * 1 mL in DMSO USD 825 In-stock
Solid
5 mg USD 750 In-stock
10 mg USD 1200 In-stock
25 mg USD 2400 In-stock
50 mg USD 3850 In-stock
100 mg USD 6200 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Alicapistat:

Alicapistat Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Alicapistat

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].
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].

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

Alicapistat Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

433.50

Formula

C25H27N3O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N([C@H](CC1)C(NC(C(C(NC2CC2)=O)=O)CC3=CC=CC=C3)=O)CC4=CC=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (115.34 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a clear solution of ≥ 4.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (41.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: ≥98.0%

COA (252 KB) HNMR (219 KB) MS (80 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3068 mL 11.5340 mL 23.0681 mL 57.6701 mL
5 mM 0.4614 mL 2.3068 mL 4.6136 mL 11.5340 mL
10 mM 0.2307 mL 1.1534 mL 2.3068 mL 5.7670 mL
15 mM 0.1538 mL 0.7689 mL 1.5379 mL 3.8447 mL
20 mM 0.1153 mL 0.5767 mL 1.1534 mL 2.8835 mL
25 mM 0.0923 mL 0.4614 mL 0.9227 mL 2.3068 mL
30 mM 0.0769 mL 0.3845 mL 0.7689 mL 1.9223 mL
40 mM 0.0577 mL 0.2884 mL 0.5767 mL 1.4418 mL
50 mM 0.0461 mL 0.2307 mL 0.4614 mL 1.1534 mL
60 mM 0.0384 mL 0.1922 mL 0.3845 mL 0.9612 mL
80 mM 0.0288 mL 0.1442 mL 0.2884 mL 0.7209 mL
100 mM 0.0231 mL 0.1153 mL 0.2307 mL 0.5767 mL
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Alicapistat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Alicapistat1254698-46-8ABT-957ABT957ABT 957ProteasomeA-1212805aberrant activationcalpainneurodegenerative diseasesAlzheimer′s Diseasecalpain 1CNS-penetrationInhibitorinhibitorinhibit

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