BChE/p38-α MAPK-IN-1
BChE/p38-α MAPK-IN-1 is a selective dual inhibitor of hBChE (IC50 = 772 nM) and p38α MAPK (IC50 = 191 nM). BChE/p38-α MAPK-IN-1 reduces the production of pro-inflammatory cytokines (IL-1β, IL-6, IL-8, TNF-α) in cells. BChE/p38-α MAPK-IN-1 improves Scopolamine (HY-N0296)-induced cognitive impairment, as well as alleviates LPS (HY-D1056)-induced spatial learning impairment and exerts anti-neuroinflammatory effects in mice. BChE/p38-α MAPK-IN-1 can be used for the study of Alzheimer’s disease (AD) by targeting both cholinergic deficit and neuroinflammation.
For research use only. We do not sell to patients.
- CAS No.: 3077831-11-6
- Formula: C26H32F2N4O
- Molecular Weight:454.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Help & FAQs
Biological Activity
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p38α MAPK 191 nM (IC50) |
hBCHE 772 nM (IC50) |
BChE/p38-α MAPK-IN-1 (Compound 95) shows inhibitory potency against hBChE (IC50 = 772 nM) and p38α MAPK (IC50 = 191 nM)[1].
BChE/p38-α MAPK-IN-1 (1-5 μM, 18 h) reduces the production of pro-inflammatory cytokines (IL-1β, IL-6, IL-8, TNF-α) and slightly increases anti-inflammatory cytokine IL-12 in Phytohemagglutinin (PHA) (HY-N7038)-stimulated human peripheral blood mononuclear cells (PBMCs)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Phytohemagglutinin (PHA) (HY-N7038)-stimulated human peripheral blood mononuclear cells (PBMCs)
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Concentration:1, 2.5, 5 μM
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Incubation Time:18 h
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Result:Reduced the production of pro-inflammatory cytokines (IL-1β, IL-6, IL-8, TNF-α) and slightly increases anti-inflammatory cytokine IL-12.
BChE/p38-α MAPK-IN-1 (10 mg/kg, i.p., once daily for 10 days) alleviates LPS (HY-D1056)-induced spatial learning impairment and exerts anti-neuroinflammatory effects in adult male C57BL/6J mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Albino Swiss (CD-1) mice were subcutaneously injected with scopolamine (1 mg/kg) 30 min before the acquisition trial of passive avoidance (PA) and novel object recognition (NOR) tasks to induce cholinergic deficit-related cognitive impairment[1]
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Dosage:5, 10 mg/kg
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Administration:i.p., 60 min before acquisition trial
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Result:Prolonged the step-through latency of mice in the memory retention trial at a dose of 10 mg/kg.
Improved scopolamine-induced long-term contextual memory impairment.
Increased the discrimination index of mice at a dose of 10 mg/kg.
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Animal Model:Adult male C57BL/6J mice were intraperitoneally injected with LPS at doses of 2.5 mg/kg (2 days), 2 mg/kg (2 days), and 1.5 mg/kg (2 days) respectively[1]
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Dosage:10 mg/kg
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Administration:i.p., once daily for 10 days
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Result:Reduced the escape latency of mice in morris water maze spatial learning task.
Reduced the expression levels of inflammation-related proteins (TLR4, COX-2, and NLRP3) in mouse brains.
Had no obvious effect on the expression of cPLA2 protein.
Chemical Information
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CAS No. 3077831-11-6
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Molecular Weight 454.56
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Formula C26H32F2N4O
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SMILES
O=C(C1=CC2=C(C=C1CC3=CC=C(F)C=C3F)C=NN2CC4CCCCC4)NCCN(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BChE/p38-α MAPK-IN-1 Related Classifications
HY-175655 Related Classifications
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