BChE-IN-44
BChE-IN-44 is a potent, brain-penetrant, highly selective BChE inhibitor [equine BChE IC50 = 18.00 pM, human BChE IC50 = 1.50 nM]. BChE-IN-44 shows neuroprotective effects against the Aβ1-42-induced injury model and inhibitory effects on Aβ1-42 self-aggregation. BChE-IN-44 reduces the levels of inflammatory factors (NO, IL-6, and TNF-α) in Lipopolysaccharides (HY-D1056)-induced BV2 cells. BChE-IN-44 can significantly ameliorate Scopolamine (HY-N0296)-induced cognition impairment. BChE-IN-44 exhibits capacity in the regulation of BChE and acetylcholine levels in the mouse hippocampus. BChE-IN-44 can be used for the study of Alzheimer’s disease (AD).
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- Formule: C22H23N3O4
- Masse moléculaire:393.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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IL-6 |
RatBuChE |
In Vitro
BChE-IN-44 (Compound N14) (50 μM, 24 h) lead to about 15 % cell toxicity in PC12 and SH-SY5Y, suggesting that BChE-IN-44 possesses a high safety profile in vitro[1].
BChE-IN-44 shows a Kc of 0.017 μM, indicating that BChE-IN-44 possesses a higher affinity for BChE[1].
BChE-IN-44 (5-20 μM, 24 h) significantly reduces the levels of inflammatory factors (NO, IL-6, and TNF-α) in Lipopolysaccharides (LPS)-induced BV2 cells[1].
BChE-IN-44 (20 μM, 24 h) demonstrates significant neuroprotective efficacy against Aβ1–42-induced injury in PC12 cells[1].
BChE-IN-44 (20 μM, 48 h) effectively inhibits Aβ1-42 aggregation, confirming the good inhibitory effects of the carrier scaffold on Aβ1–42 aggregation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC12 cells, SH-SY5Y cells
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Concentration:50 μM
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Incubation Time:24 h
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Result:Led to about 15 % cell toxicity in PC12 and SH-SY5Y.
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Cell Line:BV2 cells
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Concentration:5 μM, 10 μM, 20 μM
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Incubation Time:24 h
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Result:Significantly reduced the levels of inflammatory factors (NO, IL-6, and TNF-α) in LPS-induced BV2 cells.
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Cell Line:PC12 cells
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Concentration:20 nM
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Incubation Time:24 h
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Result:Showed significant neuroprotective efficacy against Aβ1-42-induced injury in PC12 cells.
Parmacokinetics
| Species | Dose | Route | AUC0-t | MRT0-t | T1/2 | Cmax | Tmax | F |
|---|---|---|---|---|---|---|---|---|
| Rat | 5 mg/kg | i.v. | 9.94 μg·h/mL | 0.75 h | 3.1 h | 27.87 μg/mL | 0.033 h | / |
| Rat | 50 mg/kg | i.p. | 16.36 μg·h/mL | 2.57 h | 4.43 h | 12.93 μg/mL | 0.25 h | 16.46 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Thirty-six six-week-old male Kunming mice (weighing 25-30 g) were intraperitoneally injected with scopolamine (3 mg/kg) to mimic AD-like cognitive deficits[1].
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Dosage:5 mg/kg, 10 mg/kg, 20 mg/kg
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Administration:I.p., once daily for 14 days, 30 mins after Scopolamine
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Result:Increased the spontaneous alternation rate to 72.6%, indicating improved working memory.
Increased central region dwell time and travel distance, and reduced anxiety-like behaviors.
Shortened escape latency, reduced travel distance, and increased platform crossings, showing improved spatial learning memory.
Behavioral trajectory plots showed more organized.
Increases ACh levels and decreases AChE and BChE activities.
Reduces IL-6 and TNF-α levels and inhibits neuroinflammation.
Chemical Information
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Masse moléculaire 393.44
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Formule C22H23N3O4
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SMILES
CC1=CC(O)=C(C=C1)C(NCCC2=CNC3=CC=C(C=C23)OC(N4CCC4)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BChE-IN-44 Related Classifications
HY-178356 Related Classifications
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