2. Apoptosis
  3. Apoptosis
  4. 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 appropriate pharmacokinetic properties, 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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CX116 Chemical Structure

CX116 Chemical Structure

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CX116 Related Antibodies

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Description

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 appropriate pharmacokinetic properties, 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)[1].

In Vitro

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) can attenuate Cisplatin-induced cell apoptosis in a dose-dependent manner in HK-2 cells. CX116 decreases the expressions of P53, c-caspase 3, and Bax proteins, and leads to a significant increase in the expression of the antiapoptotic protein Bcl-2 and a sharp decrease in the Bax/Bcl-2 ratio. CX116 alone does not induce cell apoptosis[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.

CX116 Related Antibodies

Western Blot Analysis[1]

Cell Line: HK-2 cells
Concentration: 2.5, 5, 10 μM, pretreatment with 10 μM Cisplatin
Incubation Time: 24 h
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.
Parmacokinetics[1]
Species Dose Route Indicator value
Rat 2 mg/kg i.v. Cmax 289.11 ng/mL
Rat 20 mg/kg p.o. T1/2 6.29 hr
Rat 2 mg/kg i.v. T1/2 1.91 hr
Rat 20 mg/kg p.o. Cmax 170.50 ng/mL
Rat 2 mg/kg i.v. AUC0-t 165.39 ng·h/mL
Rat 20 mg/kg p.o. Tmax 0.5 hr
Rat 2 mg/kg i.v. AUC0-∞ 192.68 ng·h/mL
Rat 20 mg/kg p.o. AUC0-t 784.58 ng·h/mL
Rat 2 mg/kg i.v. MRT0-∞ 1.74 hr
Rat 20 mg/kg p.o. AUC0-∞ 1274.25 ng·h/mL
Rat 20 mg/kg p.o. F 66.13 %
Rat 20 mg/kg p.o. MRT0-∞ 13.52 hr
In Vivo

CX116 (Compound 83) (1500 mg/kg, p.o., single high-dose) causes no death, toxic effects or significant weight loss of C57BL/6 mice[1].
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.

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
Dosage: 25, 50 mg/kg
Administration: Oral gavage (i.g.), every day, from 3 days before the Cisplatin administration and three days after Cisplatin injection
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.
Molecular Weight

432.48

Formula

C23H24N6O3
SMILES

NC1=NC=C(C=C1C(NC2=CC=C(C=C2)NC(C)=O)=O)C3=CC=C(N=C3)N4CCOCC4
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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CX116 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:

CX116CX 116CX-116ApoptosisAcute kidney injury (cis-AKI)Cisplatin-based cancerPhenotypic screeningInhibitorinhibitorinhibit

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