2. Apoptosis
  3. Apoptosis
  4. CX116

CX116 是一种口服有效且具备显著抗炎活性的抗炎剂。CX116 通过抑制炎症反应、降低氧化应激、保护线粒体功能以及抑制细胞凋亡 (apoptosis) 来发挥其作用。CX116 具有可接受的毒性以及适宜的药代动力学特性，并且可以显著保护小鼠肾组织免受顺铂 (Cisplatin) (HY-17394) 的损害。CX116 可用来研究由顺铂导致的急性肾损伤。

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CX116 Chemical Structure

CX116 Chemical Structure

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CX116 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

CX116 (Compound 83) (10 μM, 1 h) 显示出对脂多糖 (LPS) 刺激下 RAW 264.7 细胞的保护作用和其产生的 NO 的抑制作用，其 EC50 为 0.8 μM, IC50 为 1.1 μM[1]。
CX116 (Compound 83) (1.25-10 μM, pretreatment with 10 μM Cisplatin, 1 h) 抑制顺铂诱导的 HK-2 细胞中与顺铂诱导的急性肾损伤相关的促炎细胞因子 (TNF-α、IL-1β、IL-6 和 MCP-1) 的水平，并且呈浓度依赖性[1]。
CX116 (2.5-10 μM, 10 μM 顺铂前处理) 可剂量依赖性地降低顺铂诱导的ROS水平[1]。
CX116 (2.5-10 μM, 10 μM 顺铂前处理) 在 HK-2 细胞中对线粒体的结构和功能有强保护作用:
CX116 (2.5-10 μM, 10 μM 顺铂前处理, 24 h) 可剂量依赖性地逆转被顺铂降低的 sirtuin3、Opa1 和 ATP5A1 蛋白含量[1]。
CX116 (2.5-10 μM, 10 μM 顺铂前处理) 以剂量依赖性减弱顺铂诱导的 HK-2 细胞凋亡。CX116 剂量依赖性降低了 P53、c-caspase 3 和 Bax 蛋白的表达量。CX116 显著增加了抗凋亡蛋白 Bcl-2 的表达，同时显著降低 Bax/Bcl-2 比值。CX116 单独作用时不会诱导细胞凋亡[1]。
CX116 (24 h) 对5种主要细胞色素 P450 酶（CYPs）亚型的 IC50 值分别为 26.8 μM (LA-2)、14.2 μM (2C9)、13.7 μM (2C19)、34.5 μM (2D6) 和 ＞ 50 (3A4)[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CX116 相关抗体:

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.
药代动力学
(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
体内研究
(In Vivo)

CX116 (Compound 83) (1500 mg/kg, p.o., 单次高剂量) 没有造成C57BL/6小鼠的死亡、毒性作用和显著的体重减轻[1]。
CX116 (25, 50 mg/kg, i.g., 每天给药，共给药6天) 显著减轻小鼠体内顺铂诱导的肾毒性并发挥了显著的肾保护作用[1]。

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.
分子量

432.48

Formula

C23H24N6O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CX116 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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