2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. Toll-like Receptor (TLR) NF-κB Keap1-Nrf2 Reactive Oxygen Species (ROS)
  4. TLR4/NF-κB-IN-2

TLR4/NF-κB-IN-2 is an orally active TLR4/NF-κB inhibitor and Nrf2/HO-1 activator. TLR4/NF-κB-IN-2 combats oxidative stress and exerts anti-inflammatory effects by regulating the Nrf2/HO-1 and TLR4/NF-κB pathways. TLR4/NF-κB-IN-2 reduces Aβ aggregation and protects neurons. TLR4/NF-κB-IN-2 can be used in the research of Alzheimer's disease.

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TLR4/NF-κB-IN-2

TLR4/NF-κB-IN-2 Chemical Structure

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TLR4/NF-κB-IN-2 Related Antibodies

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Description

TLR4/NF-κB-IN-2 is an orally active TLR4/NF-κB inhibitor and Nrf2/HO-1 activator. TLR4/NF-κB-IN-2 combats oxidative stress and exerts anti-inflammatory effects by regulating the Nrf2/HO-1 and TLR4/NF-κB pathways. TLR4/NF-κB-IN-2 reduces Aβ aggregation and protects neurons. TLR4/NF-κB-IN-2 can be used in the research of Alzheimer's disease[1].

In Vitro

TLR4/NF-κB-IN-2 (Compound G-12) (5 μM; 1 h pre-incubation, 24 h LPS stimulation) potently inhibits LPS-induced NO production in BV2 cells with an IC50 of 1.39 ± 0.11 μM[1].
TLR4/NF-κB-IN-2 (2.5-10 μM; 3 h pre-incubation, 24 h H2O2 exposure) potently protects PC12 cells from H2O2-induced death with an IC50 of 1.29 ± 0.02 μM, increasing cell viability in a concentration-dependent manner[1].
TLR4/NF-κB-IN-2 (2.5-10 μM; 2 h pre-incubation, 6 h LPS stimulation) dose-dependently reduces LPS-induced intracellular ROS accumulation in BV2 cells[1].
TLR4/NF-κB-IN-2 (2.5-10 μM; 2 h pre-incubation, 24 h LPS stimulation) activates the Nrf2/HO-1 signaling pathway in LPS-stimulated BV2 cells, enhancing Nrf2 nuclear translocation and HO-1 expression in a concentration-dependent manner[1].
TLR4/NF-κB-IN-2 (2.5-10 μM; 2 h pre-incubation, 24 h LPS stimulation) inhibits the LPS-induced TLR4/NF-κB signaling pathway in BV2 cells, reducing TLR4 expression and the phosphorylation of downstream IκBα and p65 in a concentration-dependent manner[1].

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

TLR4/NF-κB-IN-2 Related Antibodies

Cell Viability Assay[1]

Cell Line: PC12 rat pheochromocytoma cells
Concentration: 2.5, 5 and 10 μM
Incubation Time: 3 h (pre-incubation); 24 h (H2O2 exposure)
Result: Increased the viability of H2O2-treated PC12 cells from 50.66% to 73.85% (2.5 μM), 86.92% (5 μM), and 94.16% (10 μM).
Achieved an IC50 of 1.29 μM for protection against H2O2-induced cell death.

Western Blot Analysis[1]

Cell Line: BV2 mouse microglial cells
Concentration: 2.5, 5 and 10 μM
Incubation Time: 2 h (pre-incubation); 24 h (LPS stimulation)
Result: Enhanced LPS-induced nuclear translocation of Nrf2 in a concentration-dependent manner.
Increased HO-1 protein expression in a concentration-dependent manner, with HO-1/β-actin ratio increasing from ~0.8 (LPS-only group) to ~1.0 (2.5 μM), ~1.0 (5 μM), and ~1.2 (10 μM).\nReduced LPS-induced TLR4 protein expression in a concentration-dependent manner, with TLR4/β-actin ratio decreasing from ~1.0 (LPS-only group) to ~0.5 (10 μM).
Decreased the phosphorylation of IκBα in a concentration-dependent manner, with P-IκBα/IκBα ratio decreasing from ~1.1 (LPS-only group) to ~0.8 (10 μM).
Decreased the phosphorylation of p65 in a concentration-dependent manner, with P-p65/p65 ratio decreasing from ~1.1 (LPS-only group) to ~0.7 (10 μM).
Parmacokinetics
Species Dose Route T1/2 AUC0-t AUC0-∞ Vz CL Vss Cmax Bioavailability
Mice[1] 1 mg/kg i.v. 0.33 h 197 ng·h/mL 198 ng·h/mL 3.20 L/kg 167 mL/min/kg 1.88 L/kg / /
Mice[1] 5 mg/kg p.o. 0.25 h 128.5 ng·h/mL 155.3 ng·h/mL / / / 267.4 ng/mL 15.7 %
In Vivo

TLR4/NF-κB-IN-2 (Compound G-12) (2.5-10 mg/kg; p.o.; once daily for 7 consecutive days) dose-dependently improves cognitive function, reduces Aβ1-42 accumulation, protects hippocampal neurons, inhibits glial cell activation and neuroinflammation, and alleviates oxidative stress in Aβ1-42-induced Alzheimer's disease model mice[1].

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

Animal Model: ICR mice (male, 6-8 weeks old, 18-25 g, intracerebroventricular injection of Aβ1-42 peptide-induced)[1]
Dosage: 2.5 mg/kg; 10 mg/kg
Administration: p.o.; once daily for 7 consecutive days
Result: Reversed Aβ1-42-induced reductions in total ambulatory distance, mean speed, and central zone movement distance in the open-field test.
Reduced escape latency over 5 days of Morris water maze training, increased the number of platform crossings, and increased time spent in the target quadrant during the probe trial.
Reduced hippocampal Aβ1-42 concentrations from ~70 μg/L to ~60 μg/L (2.5 mg/kg) and to ~48 μg/L (10 mg/kg); reduced whole-brain Aβ1-42 concentrations from ~42 μg/L to ~38 μg/L (2.5 mg/kg) and to ~31 μg/L (10 mg/kg).
Increased neuronal counts in the DG, CA1, and CA3 regions of the hippocampus; at 10 mg/kg, increased DG neuronal counts from ~240 to ~460 and CA1 neuronal counts from ~80 to ~150.
Dose-dependently reduced the percentage of GFAP-positive astrocytes and Iba-1-positive microglia in the hippocampus, shifting glial cells from a reactive to a resting morphological state.
Reduced hippocampal TNF-α levels from ~185 pg/mL to ~148 pg/mL (2.5 mg/kg) and to ~105 pg/mL (10 mg/kg); reduced IL-6 levels from ~228 pg/mL to ~165 pg/mL (2.5 mg/kg) and to ~135 pg/mL (10 mg/kg).
Reduced hippocampal MDA levels from ~180 nmol/mgprot to ~165 nmol/mgprot (2.5 mg/kg) and to ~120 nmol/mgprot (10 mg/kg); increased SOD activity from ~2.8 U/mgprot to ~3.8 U/mgprot (2.5 mg/kg) and to ~4.2 U/mgprot (10 mg/kg).
Molecular Weight

437.55

Formula

C27H32FNO3
SMILES

O=C(C(O)=C1[C@@H]2C=C(C)CC[C@H]2C(C)=C)C(CCCCC)=C(NC3=CC=C(F)C=C3)C1=O
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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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TLR4/NF-κB-IN-2 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:

TLR4/NF-κB-IN-2Toll-like Receptor (TLR)NF-κBKeap1-Nrf2Reactive Oxygen Species (ROS)Nuclear factor-κBNuclear factor-kappaBTLR4-MD-2 complexhippocampal neuronsPC12 cellsTLR4/NF-κB pathwayAML-12 cellsAlzheimer's diseaseNrf2/HO-1 pathwayAβ aggregationBV2 cellsneuroinflammationInhibitorinhibitorinhibit

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