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CIAC101

CIAC101 is a potent and brain-penetrant TLR4 antagonist with an IC50 of 17.0 nM in NO assay. CIAC101 blocks Lipopolysaccharides (LPS) -induced NF-κB activation and reduces the expression of pro-inflammatory mediators (iNOS, IL-1β, TNF-α, and IL-6). CIAC101 robust antineuroinflammatory activity with efficacy against drug-evoked neurobehavioral adaptations. CIAC101 can be used for the research of addiction and neurological disease[1].

Product Specifications

UNSPSC

12352005

Target

Interleukin Related; NF-κB; NO Synthase; TNF Receptor; Toll-like Receptor (TLR)

Related Pathways

Apoptosis; Immunology/Inflammation; NF-κB

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Smiles

O=C1[C@](OC2=C(OCC(C)C)C=CC3=C24)([H])[C@]54CCN(CC6CC6)[C@](C3)([H])[C@@]5(O)C=C1

Molecular Formula

C24H29NO4

Molecular Weight

395.49

References & Citations

[1]Gao J, et al. Nanomolar TLR4 Antagonist CIAC101 Derived from (+) -Naltrexone Blocks Microglial Activation and Methamphetamine Addiction. J Med Chem. 2025;68 (23) :25469-25484.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

IL-1; IL-6; iNOS; NF-κB; TLR4; TNFRSF5/CD40

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