2. Neuronal Signaling Membrane Transporter/Ion Channel Immunology/Inflammation Apoptosis
  3. Cholinesterase (ChE) nAChR Interleukin Related TNF Receptor
  4. 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).

For research use only. We do not sell to patients.

BChE-IN-44

BChE-IN-44 Chemical Structure

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BChE-IN-44 Related Antibodies

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AChE BChE

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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Description

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)[1].

IC50 & Target

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.

BChE-IN-44 Related Antibodies

Cell Viability Assay[1]

Cell Line: PC12 cells, SH-SY5Y cells
Concentration: 50 μM
Incubation Time: 24 h
Result: Led to about 15 % cell toxicity in PC12 and SH-SY5Y.

ELISA Assay[1]

Cell Line: BV2 cells
Concentration: 5 μM, 10 μM, 20 μM
Incubation Time: 24 h
Result: Significantly reduced the levels of inflammatory factors (NO, IL-6, and TNF-α) in LPS-induced BV2 cells.

Cell Viability Assay[1]

Cell Line: PC12 cells
Concentration: 20 nM
Incubation Time: 24 h
Result: Showed significant neuroprotective efficacy against Aβ1-42-induced injury in PC12 cells.
In Vivo

BChE-IN-44 (5-20 mg/kg, i.p., once daily for 14 days) can effectively reverse Scopolamine-induced cognitive impairment, anxiety, and learning and memory deficits in mice, inhibit BChE activity, increase ACh levels, and reduce neuroinflammation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].
Dosage: 5 mg/kg, 10 mg/kg, 20 mg/kg
Administration: I.p., once daily for 14 days, 30 mins after Scopolamine
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.
Molecular Weight

393.44

Formula

C22H23N3O4
SMILES

CC1=CC(O)=C(C=C1)C(NCCC2=CNC3=CC=C(C=C23)OC(N4CCC4)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BChE-IN-44 Related Classifications

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BChE-IN-44Cholinesterase (ChE)nAChRInterleukin RelatedTNF ReceptorNicotinic acetylcholine receptorsILTumor Necrosis Factor ReceptorTNFRAlzheimer's diseaseCarbamateHighly selective BChE inhibitorNeuroinflammatoryInhibitorinhibitorinhibit

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