2. Membrane Transporter/Ion Channel Neuronal Signaling Immunology/Inflammation Apoptosis NF-κB
  3. nAChR Interleukin Related TNF Receptor NF-κB
  4. JWX-A0108

JWX-A0108 是一种选择性人源 α7 nAChR 正变构调节剂，其 EC50 为 4.35 μM。JWX-A0108 仅在乙酰胆碱存在的情况下增强 α7 nAChR 电流，无直接激活作用，也不会改变脱敏效应。JWX-A0108 通过增加自发性抑制性突触后电流，增强海马 GABA 能突触传递。JWX-A0108 可通过阻断 NF-κB 信号通路，降低 IL-1β、TNF-α、IL-6 的脑内表达水平，并通过下调 Iba1 来减少小胶质细胞的激活。JWX-A0108 可有效改善精神分裂症和阿尔茨海默病小鼠模型的认知缺陷、神经炎症及海马神经元损伤。JWX-A0108 可用于精神分裂症、阿尔茨海默病的相关研究。

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JWX-A0108

JWX-A0108 Chemical Structure

CAS No. : 2055045-42-4

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JWX-A0108 相关抗体

Top Publications Citing Use of Products

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JWX-A0108 is a selective human α7 nAChR positive allosteric modulator with an EC50 of 4.35 μM. JWX-A0108 potentiates α7 nAChR currents only in the presence of acetylcholine, with no direct activating effect or alteration of desensitization. JWX-A0108 enhances hippocampal GABAergic synaptic transmission by increasing spontaneous inhibitory postsynaptic currents. JWX-A0108 reduces the brain expression levels of IL-1β, TNF-α, and IL-6 by blocking the NF-κB signaling pathway, and reduces microglial activation by downregulating Iba1. JWX-A0108 effectively improves cognitive deficits, neuroinflammation, and hippocampal neuronal damage in mouse models of schizophrenia and Alzheimer's disease. JWX-A0108 can be used for research related to schizophrenia and Alzheimer's disease[1][2][3].

IC50 & Target[3]

IL-1β

 

TNF-α

 

NF-κB

 

体外研究
(In Vitro)

JWX-A0108 (0.1-30 μM; 2-5 days) 可选择性增强表达人源 α7 nAChR 的非洲爪蟾卵母细胞中 α7 nAChR 介导的电流，其 EC50 为 4.35 μM，且对其他受试 nAChR 亚型或 5-HT3A 受体无活性[1]。
JWX-A0108 可强效增强表达人源 α7 nAChR 的爪蟾卵母细胞中乙酰胆碱激活的电流，其为 I 型正变构调节剂，EC50 为 5.7 μM，电流放大倍数达 6 倍[3]。

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

JWX-A0108 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Cmax Tmax AUClast AUC0-∞ MRT Vz CL Vz/F CL/F F
Rat[1] 1 mg/kg i.v. 2.7 h 231.5 mg/L 0.25 h 280.2 mg·h/L 293.8 mg·h/L 2.7 h 0.013 L/kg 0.004 L/h/kg / / /
Rat[1] 10 mg/kg i.g. 1.9 h 145.1 mg/L 1.3 h 368.1 mg·h/L 395.2 mg·h/L 3.3 h / / 0.071 L/kg 0.028 L/h/kg 13.4 %
体内研究
(In Vivo)

JWX-A0108 (0.03-10 mg/kg, i.p.) 可显著改善 Dizocilpine (HY-15084B) 诱导的小鼠听觉门控缺陷、空间工作记忆障碍和运动过度活跃[1]。
JWX-A0108 (5 mg/kg；腹腔注射；每日一次；连续 19 天) 可改善 APP/PS1 小鼠的空间记忆损伤 (逃逸潜伏期缩短)，并通过 α7 nAChR 介导的 NF-κB 信号通路抑制作用减轻神经炎症，同时保护海马神经元[2]。

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

Animal Model: C57BL/6J (male, adult)[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.p.
Result: Reversed Dizocilpine-induced percent prepulse inhibition (PPI) reduction from 19% to 25% (1 mg/kg), 32% (3 mg/kg), and 37% (10 mg/kg) across five prepulse intensities.
Significantly increased average percent PPI across all prepulse levels in a dose-dependent manner compared to the MK-801-only group.
Animal Model: C57BL/6J (male, adult)[1]
Dosage: 0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg
Administration: i.p.
Result: Reversed Dizocilpine-induced reduction of time spent in the novel arm from 45% to 49% (0.03 mg/kg), 53% (0.1 mg/kg), and 61% (0.3 mg/kg).
Attenuated Dizocilpine-induced increase in total travel distance at the 0.03 mg/kg dose.
Animal Model: APP/PS1 double transgenic mice (9-month-old, on C57BL/6J background)[2]
Dosage: 5 mg/kg
Administration: i.p.; daily; 19 days
Result: Shortened escape latency of APP/PS1 mice in the Morris Water Maze test.
Reduced mRNA and protein levels of pro-inflammatory cytokines IL-1β, TNF-α, and IL-6 in cerebral cortex and hippocampus.
Decreased protein expression and hippocampal fluorescence intensity of microglial activation marker Iba1.
Improved hippocampal CA3 region neuronal damage with increased Nissl body counts and reduced vacuolar degeneration.
Reduced phosphorylation levels of NF-κB p65 (Ser536) and IκBα (Ser32/36).
分子量

400.86

Formula

C19H14ClFN4OS
CAS 号
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

JWX-A0108 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

JWX-A01082055045-42-4nAChRInterleukin RelatedTNF ReceptorNF-κBNicotinic acetylcholine receptorsILTumor Necrosis Factor ReceptorTNFRNuclear factor-κBNuclear factor-kappaBMK-801GABAA receptorα3β4 nAChRα7 nicotinic acetylcholine receptorXenopus laevis oocytesAPP/PS1 miceNF-κB signalingα4β2 nAChR5-HT3A receptorhippocampal pyramidal neuronsInhibitorinhibitorinhibit

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