TargetMol

(1S,2R)-Alicapistat

Product Code:
 
TAR-T60150
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20°C
1 / 1
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CodeSizePrice
TAR-T60150-1mg1mg£267.00
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TAR-T60150-5mg5mg£562.00
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TAR-T60150-1mL1 mL * 10 mM (in DMSO)£643.00
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TAR-T60150-10mg10mg£768.00
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TAR-T60150-25mg25mg£1,131.00
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TAR-T60150-50mg50mg£1,500.00
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TAR-T60150-100mg100mg£1,982.00
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TAR-T60150-500mg500mg£3,910.00
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Further Information

Bioactivity:
(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].
CAS:
2221010-57-5
Formula:
C25H27N3O4
Molecular Weight:
433.5
Pathway:
Proteases/Proteasome
Purity:
0.9805
SMILES:
C(N1[C@@H](C(N[C@@H](CC2=CC=CC=C2)C(C(NC3CC3)=O)=O)=O)CCC1=O)C4=CC=CC=C4
Target:
Cysteine Protease

References

Jastaniah A, Gaisina IN, Knopp RC, Thatcher GRJ. Synthesis of ?-Ketoamide-Based Stereoselective Calpain-1 Inhibitors as Neuroprotective Agents. ChemMedChem. 2020 Dec 3. 15(23):2280-2285. 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. 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.