CX116 is an orally effective anti-inflammatory agent with significant anti-inflammatory properties. It exerts its effects by inhibiting inflammatory responses, reducing oxidative stress, protecting mitochondrial function, and preventing apoptosis (apoptosis). CX116 demonstrates acceptable toxicity and favorable pharmacokinetic characteristics, and it significantly safeguards mouse kidney tissue from Cisplatin-induced damage. CX116 is suitable for studying acute kidney injury caused by Cisplatin.

CX116 (Compound 83) exhibits protective effects on LPS-stimulated RAW 264.7 cells and inhibits NO production with an EC₅₀ of 0.8 μM and an IC₅₀ of 1.1 μM when used at 10 μM for 1 hour. When pretreated with 10 μM Cisplatin for 1 hour, CX116 at concentrations ranging from 1.25 to 10 μM inhibits levels of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, and MCP-1) associated with cisplatin-induced acute kidney injury in HK-2 cells in a concentration-dependent manner. At 2.5 to 10 μM and with 10 μM cisplatin pretreatment, CX116 decreases cisplatin-induced ROS levels in a dose-dependent way and provides robust protection to mitochondrial structure and function in HK-2 cells. Additionally, CX116 reverses cisplatin-reduced proteins such as sirtuin3, Opa1, and ATP5A1 dose-dependently after 24 hours while also reducing cisplatin-induced apoptosis in HK-2 cells by decreasing P53, c-caspase 3, and Bax protein expression while increasing anti-apoptotic Bcl-2 protein levels significantly, thereby lowering the Bax/Bcl-2 ratio. CX116 does not induce apoptosis on its own. Regarding major cytochrome P450 enzymes (CYPs), the IC₅₀ values for CX116 after 24 hours are 26.8 μM for LA-2, 14.2 μM for 2C9, 13.7 μM for 2C19, 34.5 μM for 2D6, and greater than 50 for 3A4.

CX116 (Compound 83) at a high single dose of 1500 mg/kg administered orally did not result in mortality, toxicity, or significant weight loss in C57BL/6 mice. Furthermore, CX116 administered intragastrically at doses of 25 and 50 mg/kg daily for six days significantly reduced cisplatin-induced nephrotoxicity in mice and provided substantial renal protection.