CX116
CX116 is an orally active anti-inflammatory agent. CX116 exerts its effects by inhibiting the inflammatory response, reducing oxidative stress, protecting mitochondrial function, and counteracting apoptosis. CX116 bears acceptable toxicity, and can significantly protect renal tissue from Cisplatin (HY-17394)-induced damage. CX116 can be used for the study of Cisplatin-induced acute kidney injury (cis-AKI).
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- Fòrmula: C23H24N6O3
- Peso molecular:432.48
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
CX116 (Compound 83) (10 μM, 1 h) demonstrates potent anti-inflammatory and cytoprotective effects, with an NO inhibition IC50 of 1.1 μM and an EC50 of 0.8 μM (lip-opolysaccharide (LPS)-stimulated RAW 264.7 cell)[1].
CX116 (1.25-10 μM, pretreatment with 10 μM Cisplatin, 1 h) suppresses levels of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, and MCP-1) associated with cis-AKI in cis-induced HK-2 cells, and shows concentration-dependent[1].
CX116 (2.5-10 μM, pretreatment with 10 μM Cisplatin) in a dose-dependent manner reduces the levels of p-P65, COX-2, and iNOS proteins[1].
CX116 (2.5-10 μM, pretreatment with 10 μM Cisplatin) in a dose-dependent manner reduces ROS levels elevated by 10 μM Cisplatin induction[1].
CX116 (2.5-10 μM, pretreatment with 10 μM Cisplatin) has strong protective effect on the structure and function of mitochondria in HK-2 cells:[1].
CX116 (2.5-10 μM, pretreatment with 10 μM Cisplatin, 24 h) increases sirtuin3, Opa1 and ATP5A1 expression levels in a concentration-dependent manner.
CX116 (2.5-10 μM, pretreatment with 10 μM Cisplatin) reduces the expression levels of P53, c-caspase 3 and Bax proteins, and increases the expression of Bcl-2 protein, thereby weakening the apoptosis of HK-2 cells induced by Cisplatin[1].
CX116 (2.5-10 μM, pretreatment with 10 μM Cisplatin) significantly alleviates the tail dragging phenomenon of DNA in the head region and reduced the degree of DNA damage[1].
CX116 (24 h) exhibits IC50 values of 26.8 μM (LA-2), 14.2 μM (2C9), 13.7 μM (2C19), 34.5 μM (2D6) and ＞ 50 (3A4), respectively for the five cytochrome P450 enzyme (CYP) subtypes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HK-2 cells
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Concentration:2.5, 5, 10 μM, pretreatment with 10 μM Cisplatin
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Incubation Time:24 h
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Result:Reduced P65 levels in a dose-dependent manner upon stimulation by Cisplatin.
Inhibited the expression of COX-2 and INOS in a dose-dependent manner.
CX116 (25, 50 mg/kg, i.g., every day, for 6 days) significantly alleviates Cisplatin-induced nephrotoxicity in mice and exerts a remarkable reno-protective effect[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse model (male C57BL/6 mice aged 6 to 8 weeks, weighing between 18 and 20 g) by a single intraperitoneal injection of 20 mg/kg of Cisplatin
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Dosage:25, 50 mg/kg
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Administration:Oral gavage (i.g.), every day, from 3 days before the Cisplatin administration and three days after Cisplatin injection
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Result:Closer to the kidneys of normal mice in appearance with high-dose. Capable of ameliorating the damage to renal cells and the infiltration of inflammatory cells evaluated by decreasing the levels of BUN and SCR. Slightly superior to the activity of Amifostine (HY-B0639) with high-dose group. Reduced the levels of pro-inflammatory factors TNF-α and IL-1β. Reduced the expressions of KIM-1 and NGAL.
Chemical Information
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Peso molecular 432.48
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Fòrmula C23H24N6O3
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SMILES
NC1=NC=C(C=C1C(NC2=CC=C(C=C2)NC(C)=O)=O)C3=CC=C(N=C3)N4CCOCC4
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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)
CX116 Related Classifications
HY-176238 Related Classifications
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