BChE-IN-56
BChE-IN-56 is a blood-brain barrier-penetrant BChE inhibitor. BChE-IN-56 covalently carbamoylates the catalytic serine Ser198, producing pseudo-irreversible inhibition, with an IC50 of 18.2 nM and a Ki of 416 nM against hBChE. BChE-IN-56 improves cognitive performance in mouse models of cognitive impairment without inducing motor deficits. BChE-IN-56 can be used for research on Alzheimer's disease.
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- CAS. Nr.: 3137514-33-8
- Formel: C20H24N2O2
- Molecular Weight:324.42
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
hBCHE 18.2 nM (IC50) |
hAChE 71330 nM (IC50) |
hBCHE 416 nM (Ki) |
In Vitro
BChE-IN-56 has a protein binding rate of 85.92% in human plasma; it is stable in human plasma with a half-life of 278.00 min[1].
BChE-IN-56 has a half-life of 38.72 min in human liver microsomes, with an intrinsic clearance of 35.84 μL/min/mg protein; it has a half-life of 68.2 min in human hepatocytes, with an intrinsic clearance of 14.7 μL/min/million cells[1].
BChE-IN-56 is metabolized in human hepatocytes through pathways including deamination, deformylation, dealkylation, desaturation, oxidation, methylation, acetylation, and glucoside conjugation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Cmax | Cmax (Brain) | Tmax (Plasma) | Tmax (Brain) |
|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 1270.58 nM | 779.50 nM | 5.00 min | 10.00 min |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Albino Swiss (CD-1) (adult male, 18-22 g, induced by Scopolamine hydrobromide (HY-N0296A) (1 mg/kg, s.c.))[1]
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Dosage:5 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:i.p.; single administration 60 min before testing
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Result:Produced longer step‑through latency during the retention trial in the PA task for the 10 and 30 mg/kg doses compared with scopolamine‑treated control mice; the 5 mg/kg dose exerted no effect.
Elicited preference for the novel object and a high discrimination index comparable to vehicle‑treated mice across 5, 10, and 30 mg/kg doses in the NOR task, whereas scopolamine‑treated control mice displayed a negative discrimination index.
Chemical Information
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CAS. Nr. 3137514-33-8
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Molecular Weight 324.42
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Formel C20H24N2O2
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SMILES
CC1=CC=CC=C1NC(OC[C@@H]2CN(CC3=CC=CC=C3)CC2)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
BChE-IN-56 Related Classifications
HY-190798 Related Classifications
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