BuChE-IN-2
BuChE-IN-2 is an excellent butyrylcholinesterase (BuChE) inhibitor (IC50s of 1.28 μM and 0.67 μM for BuChE and NO). BuChE-IN-2 can inhibit the aggregation of Aβ, ROS formation and chelate Cu2+, exhibiting proper blood-brain barrier (BBB) penetration. BuChE-IN-2 has potential to research Alzheimer’s disease.
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- CAS 番号: 2745118-93-6
- 分子式: C28H20F4N6O3
- 分子量:564.49
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
IC50: 1.28 μM (BuChE), 0.67 μM (NO)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BV-2 | IC50 |
0.67 μM
Compound: F9
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Inhibition of NO production in LPS-induced mouse BV-2 cells pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
Inhibition of NO production in LPS-induced mouse BV-2 cells pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
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[PMID: 34752955] |
| BV-2 | IC50 |
1.61 μM
Compound: F9
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Inhibition of LPS-induced IL-1beta secretion in mouse BV-2 cells preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
Inhibition of LPS-induced IL-1beta secretion in mouse BV-2 cells preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
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[PMID: 34752955] |
| BV-2 | IC50 |
4.15 μM
Compound: F9
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Inhibition of LPS-induced TNF-alpha secretion in mouse BV-2 cells preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
Inhibition of LPS-induced TNF-alpha secretion in mouse BV-2 cells preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
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[PMID: 34752955] |
体外実験
BuChE-IN-2 (compound f9) (5-50 μM; 24 hours) shows obvious neuroprotection on H2O2-induced PC12 cells at 20 μM[1].
BuChE-IN-2 (100 μM; 48 hours) can inhibit Aβ aggregation[1].
BuChE-IN-2 (0.1-20 μM; 24 hours) has the obviously inhibitory effect on the secretion of inflammatory factors and IL-1β (IC50=1.61 μM) and TNF-α (IC50=4.15 μM) in BV2 cells[1].
BuChE-IN-2 (1-10 μM; 1 hour) can significantly reduce the expression of COX-2 and iNOS in a concentration-dependent manner[1].
BuChE-IN-2 (1-50 μM; 6 hours) has a significant inhibitory effect on ROS accumulation at 20 μM[1].
BuChE-IN-2 (10-1000 μM; 2 hours) decreases the DPPH concentration dramatically from 86.09% to 34.62% when the concentration of BuChE-IN-2 increases from 10 μM to 1000 μM[1].
BuChE-IN-2 (75 μM; 2 hours; MDCKII-MDR1 cells) exhibits proper blood-brain barrier permeability[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:PC12 cells[1]
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Concentration:5, 20, 25, 50 μM
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Incubation Time:24 hour
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Result:Showed obvious neuroprotection on H2O2-induced PC12 cells at 20 μM.
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Cell Line:BV2 cells[1]
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Concentration:1, 3, and 10 μM
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Incubation Time:1 hour
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Result:Significantly reduced the expression of COX-2 and iNOS in a concentration-dependent manner.
体内実験
BuChE-IN-2 (10 and 30 mg/kg; i.g., single) can remarkably improve the cognitive impairment in scopolamine-induced mouse models according to Morris water maze experiment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL mice (8-week-old, 18-23 g)[1]
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Dosage:100, 80, 64, 51.2, 40.96 mg/kg
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Administration:i.g.; single
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Result:The median Lethal Dose (LD50) of BuChE-IN-2 was 75.372 (62.383-101.673) mg/kg (95% confidence limit).
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Animal Model:Male C57BL mice (8-week-old, 18-23 g)[1]
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Dosage:30 mg/kg, 10 mg/kg
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Administration:i.g., single
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Result:BuChE-IN-2 could remarkably improve the cognitive impairment in scopolamine-induced mouse models according to Morris water maze experiment.
化学情報
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CAS 番号 2745118-93-6
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分子量 564.49
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分子式 C28H20F4N6O3
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SMILES
O=C(NC1=CC=C(C2=NC(C3=CC(NC4=CC=C(OC(F)(F)F)C=C4)=NC=C3)=NO2)C=C1)CNC5=CC=C(F)C=C5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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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)
BuChE-IN-2 関連分類
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