(1S,2R) -Alicapistat

(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].

Product Specifications

CAS Number

[2221010-57-5]

Product Name Alternative

(1S,2R) -ABT-957

UNSPSC

12352005

Target

Proteasome

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/1s-2r-alicapistat.html

Purity

98.0

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C25H27N3O4

Molecular Weight

433.50

References & Citations

[1]Lon HK, et al. Pharmacokinetics, Safety, Tolerability, and Pharmacodynamics of Alicapistat, a Selective Inhibitor of Human Calpains 1 and 2 for the Treatment of Alzheimer Disease: An Overview of Phase 1 Studies. Clin Pharmacol Drug Dev. 2019 Apr. 8 (3) :290-303.|[2]Jantos K, et al. Discovery of ABT-957: 1-Benzyl-5-oxopyrrolidine-2-carboxamides as selective calpain inhibitors with enhanced metabolic stability. Bioorg Med Chem Lett. 2019 Aug 1. 29 (15) :1968-1973. |[3]Jastaniah A, Gaisina IN, Knopp RC, Thatcher GRJ. Synthesis of α-Ketoamide-Based Stereoselective Calpain-1 Inhibitors as Neuroprotective Agents. ChemMedChem. 2020 Dec 3. 15 (23) :2280-2285.