PJ17
PJ17 is a potent dual-target inhibitor of AChE and GSK-3β, with IC50 values of 8.84 μM and 4.19 μM, respectively. PJ17 shows no significant neurotoxic effect in primary cerebellar granule neuron cultures. PJ17 serves as a template for the design of multitarget drugs. PJ17 can be used for the research of Alzheimer's disease.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2248983-31-3
- 分子式: C15H13FN4O2
- 分子量:300.29
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
AChE 8.84 μM (IC50) |
GSK-3β 4.19 μM (IC50) |
体外実験
PJ17 (30-100 μM) potently inhibits AChE with an IC50 of 8.84 μM[1].
PJ17 (10 μM) potently inhibits human recombinant GSK-3β with an IC50 of 4.19 μM, achieving 85.95% inhibition at 10 μM[1].
PJ17 (2.5-50 μM; 24-48 h) does not induce neurotoxicity in primary CGN cultures at concentrations up to 50 μM, and increases cell viability at 10-50 μM[1].
PJ17 (2.5-50 μM; 1-24 h pretreatment) does not exhibit significant neuroprotective activity against Rotenone (HY-B1756)-induced toxicity in primary CGN cultures at concentrations up to 50 μM[1].
PJ17 does not significantly inhibit rat MAO-A, MAO-B and human recombinant BACE-1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:Primary cerebellar granule neurons (CGNs) cultures
-
Concentration:2.5, 5, 10, 25, 50 μM
-
Incubation Time:24 h, 48 h
-
Result:Showed no significant decrease in cell viability after 24 or 48 h of incubation at any tested concentration.
Increased cell viability at 10-50 μM.
-
Cell Line:Primary cerebellar granule neurons (CGNs) cultures
-
Concentration:2.5, 5, 10, 25, 50 μM
-
Incubation Time:1 h pretreatment, 24 h pretreatment; 24 h Rotenone (HY-B1756) exposure
-
Result:Did not significantly prevent rotenone-induced cell viability reduction.
化学情報
-
CAS 番号 2248983-31-3
-
分子量 300.29
-
分子式 C15H13FN4O2
-
SMILES
O=C(C1CC1)NC2=NC=CC(C(NC3=C(C=NC=C3)F)=O)=C2
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
-
Neurotoxicity Study
This protocol assesses in vitro neurotoxicity by combining neuronal viability, mitochondrial/metabolic activity, neurite outgrowth, and optional neuronal network function readouts. Calcein-AM or resazurin/PrestoBlue readouts estimate viable or metabolically active cells; βIII-tubulin immunofluorescence detects neuronal morphology and neurite networks; TMRE detects mitochondrial membrane potential; and MEA recordings detect functional changes in neuronal network activity.
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Cerebellar Granule Neuron Culture
Cerebellar granule neuron culture is a primary neuronal culture method in which postnatal rodent cerebella are dissected, meninges are removed, tissue is enzymatically and mechanically dissociated, and neurons are plated on poly-cation-coated surfaces in medium that supports neuronal attachment, maturation, neurite-network formation, and biochemical or imaging analysis. Cultured CGNs are used to study neuronal development, survival, apoptosis, differentiation, neurotransmitter release, and toxin-sensitive synaptic proteins; mature cultures develop dense neuritic networks, neuronal activity, glutamate release, and neuronal marker expression. A common survival paradigm uses depolarizing extracellular potassium: CGNs maintained in high potassium medium survive and differentiate, whereas switching mature cultures from 25 mM KCl to 5 mM KCl induces apoptotic death that can be used as a readout of activity-dependent neuronal survival.
-
Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Keywords
- PJ17
- 2248983-31-3
- PJ 17
- PJ-17
- Cholinesterase (ChE)
- GSK-3
- nAChR7
- primary cerebellar granule neuron cultures
- acetylcholinesterase
- human glycogen synthase kinase 3 beta
- electric eel acetylcholinesterase
- glycogen synthase kinase 3 beta
- BOSC-23 cells
- Alzheimer's disease
- Electrophorus electricus
- GSK-3β
- Inhibitor
- inhibitor
- inhibit