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 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.

For research use only. We do not sell to patients.

JWX-A0108

JWX-A0108 Chemical Structure

CAS No. : 2055045-42-4

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JWX-A0108 Related Antibodies

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Description

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

 

In Vitro

JWX-A0108 (0.1-30 μM; 2-5 days) selectively enhances α7 nAChR-mediated currents in Xenopus laevis oocytes expressing human α7 nAChR, with an EC50 of 4.35 μM, and shows no activity on other tested nAChR subtypes or 5-HT3A receptors[1].
JWX-A0108 potently enhances acetylcholine-activated current in Xenopus oocytes expressing human α7 nAChR as a type I positive allosteric modulator with an EC50 of 5.7 μM and 6-fold current amplification[3].

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

JWX-A0108 Related Antibodies
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 %
In Vivo

JWX-A0108 (0.03-010 mg/kg, i.p.) significantly ameliorates Dizocilpine (HY-15084B)-induced auditory gating deficits, spatial working memory impairments, and hyperactivity in mice[1].
JWX-A0108 (5 mg/kg; i.p.; once daily; for 19 consecutive days) improves spatial memory impairment (reduced escape latency) in APP/PS1 mice, alleviates neuroinflammation via inhibition of the α7 nAChR-mediated NF-κB signaling pathway, and protects hippocampal neurons[2].

MedChemExpress (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).
Molecular Weight

400.86

Formula

C19H14ClFN4OS
CAS No.
SMILES

O=C1C2=C(N=CN1C3=C(C)C=CC=C3Cl)N=C(NC4=CC=C(C)C(F)=C4)S2
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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JWX-A0108 Related Classifications

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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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