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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- No. CAS: 3122563-80-5
- Fòrmula: C24H29NO4
- Peso molecular:395.49
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
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.
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Cell Line:BV-2 microglial were treated with 200 ng/mL LPS
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Concentration:0.01 μM, 0.1 μM, 1 μM
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Incubation Time:24 h
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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 (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.
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Animal Model:Male Balb/c mice (6-8 weeks; 22-25 g) (METH-induced neuroinflammation and addiction-like behaviors)[1]
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Dosage:0.005 mg/kg, 0.02 mg/kg, 0.2 mg/kg
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Administration:Intraperitoneal (i.p.)
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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).
Chemical Information
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No. CAS 3122563-80-5
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Peso molecular 395.49
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Fòrmula C24H29NO4
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SMILES
O=C1[C@](OC2=C(OCC(C)C)C=CC3=C24)([H])[C@]54CCN(CC6CC6)[C@](C3)([H])[C@@]5(O)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CIAC101 Related Classifications
HY-179646 Related Classifications
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