1. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Neuronal Signaling
  2. Reactive Oxygen Species Cholinesterase (ChE)
  3. NLRP3-IN-33

NLRP3-IN-33 (Compound 12o) 是具有血脑屏障透过性的 AChEBChE 抑制剂,其对 hAChEhBChEIC50 值分别为 1.02 μM 和 7.03 μM。NLRP3-IN-33 具有抗氧化、抗炎和金属螯合活性,可以用于阿尔兹海默症 (AD) 的研究。

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NLRP3-IN-33 Chemical Structure

NLRP3-IN-33 Chemical Structure

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查看 Cholinesterase (ChE) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NLRP3-IN-33 (Compound 12o) is a blood-brain barrier permeable inhibitor of AChE and BChE, with IC50 values of 1.02 μM and 7.03 μM against hAChE and hBChE respectively. NLRP3-IN-33 possesses antioxidant, anti-inflammatory, and metal chelating activities, making it a potential candidate for research in Alzheimer's disease (AD)[1].

IC50 & Target

IC50: 1.02 Μm (hAChE)[1].
IC50: 7.03 μM (hBChE)[1].

体外研究
(In Vitro)

NLRP3-IN-33 (12o) (1-30 μM; 24 h) 在 PC-12 细胞中没有明显的细胞毒作用[1]
NLRP3-IN-33 具有抗氧化活性,能抑制自由基的产生,IC50 值为 6.19 μM,12o (1-20 μM; 24 h) 在 PC-1 细胞有效减轻 H2O2 (600 μM; 24 h) 诱导的氧化应激具有神经保护作用[1]
NLRP3-IN-33 (1-20 μM; 24 h) 在 PC-1 细胞中还抑制了 NLRP3 炎症小体的激活,并减轻了由 LPS (1 μg/mL) 和 ATP (5 mM) 在 HMC-3 细胞中引起的线粒体诱导的活性氧 (ROS) 和线粒体膜电位 (MMP) 损伤[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HMC-3
Concentration: 12.5 μM, 25 μM
Incubation Time: 24 h
Result: Inhibited the NLRP3 inflammasome activation and caspase-1 release.
Significantly decreased the expression of NF-κB and NLRP3 proteins.
体内研究
(In Vivo)

NLRP3-IN-33 (12o) (0.05-0.02 mg/mL) 在低剂量下 (0.05 mg/mL) 能够更有效地减少果蝇 AD 模型中的线粒体和细胞氧化应激[1]
LRP3-IN-33 (5 mg/kg; 腹腔注射; 一天一次连续 22 天) 能够改善 Scopolamine (HY-N0296) (1.4 mg/kg; 腹腔注射; 一天一次连续 5 天) 诱导的 AD 小鼠模型的记忆障碍和认知障碍[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Alzheimer's disease (AD) fractional model[1]
Dosage: 1 mg/kg, 5 mg/kg
Administration: Intraperitoneal injection (i.p.); Once daily for 22 days. Received scopolamine (HY-N0296) (1.4 mg/kg; i.p.; once daily for 5 days) on the last 5 days of the experiment (day 18 to day 22).
Result: Significantly shortened escape latency time as compared to the scopolamine-treated group.
分子量

393.39

Formula

C21H19N3O5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
NLRP3-IN-33
目录号:
HY-162402
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