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Art. -Nr.: HY-176238

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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).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₃H₂₄N₆O₃
Molecular Weight:432.48

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

CX116 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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) 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.

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

Species	Dose	Route	C_max	T_1/2	AUC_0-t	AUC_0-∞	MRT_0-∞	T_max	F
Rat^[1]	2 mg/kg	i.v.	289.11 ng/mL	1.91 h	165.39 ng·h/mL	192.68 ng·h/mL	1.74 h	/	/
Rat^[1]	20 mg/kg	p.o.	170.50 ng/mL	6.29 h	784.58 ng·h/mL	1274.25 ng·h/mL	13.52 h	0.5 h	66.13 %

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.

Chemical Information

Molecular Weight 432.48
Formel C₂₃H₂₄N₆O₃
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lou Y, et al. Discovery of Novel Potent Molecule for Treating Cisplatin-Induced Acute Kidney Injury Driven by Phenotypic Screening. J Med Chem. 2025 Jun 12;68(11):12100-12124. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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MOQ

Minimum order quantity

100 mg

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