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(1S,2R)-Alicapistat

Catalog No. T60150 CAS 2221010-57-5

(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is a highly efficient, orally active compound that selectively inhibits human calpains 1 and 2, with promising implications for Alzheimer's disease (AD) therapy [1]. This compound effectively addresses the metabolic liability associated with carbonyl reduction, while demonstrating potent inhibition of calpain 1 with an IC50 value of 395 nM [2].

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(1S,2R)-Alicapistat, CAS 2221010-57-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 245.00
5 mg	In stock	$ 612.00
10 mg	In stock	$ 869.00
25 mg	In stock	$ 1,320.00
50 mg	In stock	$ 1,780.00
100 mg	In stock	$ 2,380.00
500 mg	In stock	$ 4,780.00
1 mL * 10 mM (in DMSO)	In stock	$ 713.00

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Purity: 98.05%

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Description	(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is a highly efficient, orally active compound that selectively inhibits human calpains 1 and 2, with promising implications for Alzheimer's disease (AD) therapy [1]. This compound effectively addresses the metabolic liability associated with carbonyl reduction, while demonstrating potent inhibition of calpain 1 with an IC50 value of 395 nM [2].
In vitro	(1S,2R)-Alicapistat fails to achieve sufficient concentrations in the central nervous system (CNS) for a pharmacodynamic effect [1]. It inhibits Calpain 1 (μ-calpain) and 2 (m-calpain) in a calcium-dependent manner, requiring μ-molar or m-molar calcium concentrations for activation. At 100 nM, (1S,2R)-Alicapistat (compound 22) prevents deficits in synaptic transmission caused by Aβ oligomer in rats [2]. Furthermore, at 385 nM, it effectively prevents NMDA-induced neurodegeneration and amyloid beta (Aβ)-induced synaptic dysfunction [2]. At concentrations ranging from 9-21 nM in cerebrospinal fluid (CSF), (1S,2R)-Alicapistat does not reach the IC 50 required for calpain inhibition, yet it exhibits no dose-limiting toxicities (DLTs) across broad population studies [3].
In vivo	(1S,2R)-Alicapistat (compound 22) administered intravenously (iv) or orally (po) at doses of 1-3 mg/kg shows moderate plasma clearance rates (CLp) across several species, being lowest in mouse, rat, and dog (0.13-1.04 L/hr.kg) and significantly higher in monkeys (1.98 L/hr.kg). Its average steady-state volume of distribution (Vss) is observed to be moderate in mouse, dog, and monkey (0.64-1.8 L/kg), with rats displaying a notably higher value (3.4 L/kg). The compound’s plasma elimination half-life (t 1/2 ) varies among species, being the shortest in dogs (1.7 hours), and extending to 2.3 hours in monkeys and approximately 6.0 hours in both mice and rats. Oral bioavailability (F) demonstrates high absorption in mice, rats, and dogs (>80%), contrasting with a moderate rate in monkeys (14%) [2].

Molecular Weight	433.5
Formula	C25H27N3O4
CAS No.	2221010-57-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (103.81 mM), Sonication is recommended.

References and Literature

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. 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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

(1S,2R)-Alicapistat 2221010-57-5 Proteases/Proteasome Cysteine Protease Alicapistat (1S,2R)Alicapistat inhibitor inhibit

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