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Alicapistat

$750$6,200

Products Details

Product 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].

Web ID

– HY-109001

Storage Temperature

– -20°C, 3 years; 4°C, 2 years (Powder)

Shipping

– Room Temperature

Applications

– Neuroscience-Neurodegeneration

Molecular Formula

– C25H27N3O4

References

– [1]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. |[2]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. |[3]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.

CAS Number

– 1254698-46-8

Molecular Weight

– 433.50

Compound Purity

– 98.0

SMILES

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

Clinical Information

– Phase 1

Research Area

– Neurological Disease

Solubility

– DMSO : 50 mg/mL (ultrasonic;warming;heat to 60°C)

Target

– Proteasome

Pathway

– Metabolic Enzyme/Protease

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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