2. Immunology/Inflammation NF-κB Apoptosis
  3. Toll-like Receptor (TLR) NO Synthase NF-κB TNF Receptor Interleukin Related
  4. CIAC101

CIAC101 is a potent and brain-penetrant TLR4 antagonist with an IC50 of 17.0 nM in NO assay. CIAC101 blocks Lipopolysaccharides (HY-D1056) (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.

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CIAC101

CIAC101 Chemical Structure

CAS No. : 3122563-80-5

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CIAC101 Related Antibodies

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Description

CIAC101 is a potent and brain-penetrant TLR4 antagonist with an IC50 of 17.0 nM in NO assay. CIAC101 blocks Lipopolysaccharides (HY-D1056) (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].

IC50 & Target[1]

TLR4

17 nM (IC50)

NF-κB

 

iNOS

 

TNF-α

 

IL-1β

 

IL-6

 

In Vitro

CIAC101 inhibits Lipopolysaccharides (HY-D1056) (LPS)-induced NO overproduction in microglia BV-2 cells with an IC50 of 17 nM[1].
CIAC101 (0.1 nM-10 μM; 24 h) dose-dependently blocks LPS-induced NF-κB activation (IC50 of 65.5 nM) and reduces the expression of pro-inflammatory mediators in HEK-BluehTLR4 cells. CIAC101 does not show significant cytotoxicity[1].
In a BV-2 NF-κB luciferase reporter cellline, CIAC101 (0.1 nM-10 μM; 24 h) dose-dependently suppresses LPS-induced NF-κB activation without apparent cytotoxicity, with an IC50 of 90.2 nM[1].
In the BV-2 microglial model challenged with LPS, CIAC101 (0.01-1 μM; 24 h) reduces LPS-evoked mRNA expression of iNOS, IL-1β, TNF-α, and IL-6 in a concentration-dependent manner[1].

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

CIAC101 Related Antibodies

RT-PCR[1]

Cell Line: BV-2 microglial were treated with 200 ng/mL LPS
Concentration: 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 24 h
Result: Reduced LPS-evoked mRNA expression of iNOS, IL-1β, TNF-α, and IL-6.
Parmacokinetics
Species Dose Route Note Cmax T1/2 CL Vd AUC0-inf Tmax F
Mice 2 mg/kg i.v. 文献审核 109 ng/mL 2.83 h 326 mL/min/kg 51.3 L/kg 363 ng·h/mL / /
Mice 20 mg/kg p.o. 文献审核 64.3 ng/mL 5.16 h / / 115 ng·h/mL 0.25 h 9.05 %
In Vivo

CIAC101 (0.005-0.2 mg/kg, intraperitoneal, from day 4 to day 10) effectively counteracts METH-driven neurobehavioral adaptations and neuroinflammation in mice (Balb/c, METH-induced neuroinflammation and addiction-like behaviors)[1].
CIAC101 (20 mg/kg; i.p.; daily; for 14 days) is well tolerated with no evidence of acute systemic or organ toxicity in Balb/c mice[1].

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

Animal Model: Male Balb/c mice (6-8 weeks; 22-25 g) (METH-induced neuroinflammation and addiction-like behaviors)[1]
Dosage: 0.005 mg/kg, 0.02 mg/kg, 0.2 mg/kg
Administration: Intraperitoneal (i.p.)
Result: Significantly reduced METH-induced behavioral sensitization and conditioned place preference (CPP).
Also attenuated microglial activation and proinflammatory gene expression (IL-1β, TNF-α, and IL-6) in the medial prefrontal cortex (mPFC) and ventral tegmental area (VTA).
Molecular Weight

395.49

Formula

C24H29NO4
CAS No.
SMILES

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

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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CIAC101 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:

CIAC1013122563-80-5CIAC 101CIAC-101Toll-like Receptor (TLR)NO SynthaseNF-κBTNF ReceptorInterleukin RelatedNitric oxide synthasesNOSNuclear factor-κBNuclear factor-kappaBTumor Necrosis Factor ReceptorTNFRILareacortexmethamphetamineaddictionsensitizationBV-2prefrontaltegmentalMETHconditionedantineuroinflammatoryneuroimmunemicrogliapreferencemedialplaceTLR4ventralbehavioralInhibitorinhibitorinhibit

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