1254698-46-8
Chemical Structure
Alicapistat
Synonym(s): ABT-957
- CAS No.: 1254698-46-8
- Formula:C25H27N3O4
- Molecular Weight:433.50
IUPAC Name: (2R)-1-benzyl-N-(4-(cyclopropylamino)-3,4-dioxo-1-phenylbutan-2-yl)-5-oxopyrrolidine-2-carboxamide
InChIKey: MMLDHJRGTZHNHV-BPGUCPLFSA-N
SMILES: O=C1N([C@H](CC1)C(NC(C(C(NC2CC2)=O)=O)CC3=CC=CC=C3)=O)CC4=CC=CC=C4
Biological Activity: 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].
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Alicapistat | 95.0% | 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. | ||||||||||||||||||||
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Alicapistat (Standard) | ≥98% | Alicapistat (Standard) is the analytical standard of Alicapistat (HY-109001). This product is intended for research and analytical applications. 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. | ||||||||||||||||||||
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- [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. 2018 Jul 27. [Content Brief]
- [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. [Content Brief]
Keywords
