(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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
Frequently Asked Questions
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