(1S,2R)-Alicapistat

(1S,2R)-Alicapistat

• CAS Number: 2221010-57-5
• UNSPSC Description: (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].
• Target Antigen: 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 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)
• Clinical Information: No Development Reported