≥98% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Panoramica
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 IC 50 value of 395 nM .
In Vitro
Alicapistat exihibits inadequate CNS-penetration concentrations to obtain a pharmacodynamic effect. Calpain 1 (µ-calpain) and 2 (m-calpain) expression in a calcium-dependent manner with µ-molar or m-molar calcium concentrations required for their respective activation, respectively.\nAlicapistat (compound 22) (100 nM) prevents Aβ oligomer-induced deficits in synaptic transmission in rat. Alicapistat (compound 22) (385 nM) displays efficacy with respect to prevention of NMDA-induced neurodegeneration and A-induced synaptic dysfunction in rat hippocampal slice cultures. Alicapistat (9-21 nM) has the CSF concentrations without reaching the IC 50 for calpain inhibition and shows no dose-limiting toxicities (DLTs) in the broad populations studies. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Alicapistat (compound 22) (iv or po; 1-3 mg/kg) shows moderate mean plasma clearance values (CLp) in mouse, rat, and dog (0.13-1.04 L/hr.kg), while high in monkey (1.98 L/hr.kg). Mean steady-state volume of distribution values (Vss) were moderate in mouse, dog, and monkey (0.64-1.8 L/kg), but higher in rat (3.4 L/kg). The plasma elimination half-life (t 1/2 ) was shortest in dog (1.7 hours), followed by 2.3 hours in monkey and approximately 6.0 hours in mouse and rat. Oral bioavailability (F) values were high in mouse, rat, and dog (>80%), while moderate in monkey (14%). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 IC 5
Condizioni di conservazione di stoccaggio
Store at -20°C
Spedito in
Ice chest + Ice pads
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This compound belongs to the class of organic compounds known as proline and derivatives. These are compounds containing proline or a derivative thereof resulting from reaction of proline at the amino group or the carboxy group, or from the replacement of any hydrogen of glycine by a heteroatom.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
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