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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- CAS No.: 1044870-65-6
- 화학식: C21H24N4O3
- 분자량:380.44
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
IC50 & Target
|
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
|
[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. Further protocols information, click here.
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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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CAS No. 1044870-65-6
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분자량 380.44
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Research Protocol for Neurological Diseases
PINK1/Parkin-mediated mitophagy pathway is a mitochondrial quality-control signaling axis in which mitochondrial depolarization stabilizes PINK1 on damaged mitochondria, activates Parkin recruitment and E3 ubiquitin ligase activity, promotes ubiquitination of outer mitochondrial membrane proteins, recruits selective autophagy adaptors, and drives lysosomal degradation of damaged mitochondria. In neurological disease research, this pathway is experimentally important because neurons, especially dopaminergic neurons, are highly dependent on mitochondrial integrity, and defective mitochondrial turnover can lead to mitochondrial dysfunction, oxidative stress, impaired neuronal survival, α-synuclein accumulation, and neuroinflammatory damage-associated signals. The genetic disease link is strongest in Parkinson’s disease because mutations in PRKN/parkin cause autosomal recessive juvenile parkinsonism, mutations in PINK1 cause hereditary early-onset Parkinson’s disease, and Drosophila studie
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)