| Identification | Back Directory | [Name]
Alicapistat (Synonyms: ABT-957) | [CAS]
1254698-46-8 | [Synonyms]
ABT-957
Alicapistat
Alicapistat (ABT-957)
Alicapistat (Synonyms: ABT-957)
2-Pyrrolidinecarboxamide, N-[3-(cyclopropylamino)-2,3-dioxo-1-(phenylmethyl)propyl]-5-oxo-1-(phenylmethyl)-, (2R)- | [Molecular Formula]
C25H27N3O4 | [MDL Number]
MFCD31813623 | [MOL File]
1254698-46-8.mol | [Molecular Weight]
433.5 |
| Chemical Properties | Back Directory | [density ]
1.29±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 8.33 mg/mL (19.22 mM) | [form ]
Solid | [pka]
11.83±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [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 (t1/2) 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%)[2]. | [storage]
Store at -20°C | [References]
[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. DOI:10.1002/cpdd.598
[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. DOI:10.1016/j.bmcl.2019.05.034
[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. DOI:10.1002/cmdc.202000385 |
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| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
| Company Name: |
ABBIOCHEM
|
| Tel: |
18964309092 18964309092 |
| Website: |
http://www.abbiochemical.com |
|