MR2938
MR2938 is a potent AChE inhibitor, with an IC50 of 5.04 μM. MR2938 also suppresses NO production obviously (IC50 = 3.29 μM). MR2938 suppresses the neuroinflammation through blocking MAPK/JNK and NF-κB signaling pathways. MR2938 can be used for Alzheimer’s disease (AD) research.
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- No. CAS: 1044870-65-6
- Fòrmula: C21H24N4O3
- Peso molecular:380.44
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
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AChE 5.04 ± 0.7 μM (IC50) |
BChE >20 μM (IC50) |
NF-κB |
IL-1β |
IL-6 |
NLRP3 |
JNK |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
3.29 μM
Compound: B12; MR2938
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Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 24 hrs followed by LPS stimulation by Griess reagent-based colorimetric assay
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 24 hrs followed by LPS stimulation by Griess reagent-based colorimetric assay
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[PMID: 37043994] |
In Vitro
MR2938 (0-10 μM, 24 h) decreases the mRNA levels of pro-inflammatory cytokines IL-1β, TNF-α, IL-6 and CCL2 at 1.25 μM[1].
MR2938 (10 μM, 24 h) blocks NF-κB signaling pathway in LPS-induced BV-2 cells[1].
MR2938 (20 μM) shows inhibitory activities against AChE and BChE, with inhibitory rates of 91.8 ± 2.68% and 38.7 ± 11.7%, respectively[1].
MR2938 (0-10 μM) has little effect on cell viability on BV2 cell line[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BV-2 cells
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Concentration:0, 1.25, 2.5, 5, and 10 μM
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Incubation Time:24 h
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Result:Dramatically and dose dependently reduced the mRNA levels of inflammatory factors stimulated by LPS (1 μg/mL). Compared with TNF-α, the inhibitory effect of MR2938 on IL-1β, IL-6 and CCL2 was much potent.
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Cell Line:BV-2 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Suppressed the expression level of p65 protein, and reduced the p-p65 level. Reduced NLRP3 expression obviously. Reduced the phosphorylation level of JNK induced by LPS stimulation, while the level of JNK protein was hardly changed.
Chemical Information
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No. CAS 1044870-65-6
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Peso molecular 380.44
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Fòrmula C21H24N4O3
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SMILES
COC1=CC(OC)=C2C(NC(C3=CC=C(C=C3)N4CCN(CC4)C)=NC2=C1)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MR2938 Related Classifications
HY-149087 Related Classifications
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