2. NF-κB Stem Cell/Wnt MAPK/ERK Pathway Apoptosis Anti-infection
  3. NF-κB ERK Apoptosis Bacterial
  4. OP-1118

OP-1118 (Fidaxomicin metabolite OP-1118) 是一种口服有效的 NF-κB 和 ERK1/2 双重抑制剂，其全身血浆暴露量低、无蓄积且主要经粪便排泄。OP-1118 通过抑制 NF-κB 和 ERK1/2 的磷酸化及降低促炎细胞因子表达，发挥出显著的抗炎、细胞保护、抗凋亡和抗菌活性。在难辨梭状芽孢杆菌 (Clostridium difficile) 感染模型中，OP-1118 能有效阻断毒素介导的肠道炎症、细胞变圆、组织学损伤及细胞凋亡，且其保护作用可被 PMA (HY-18739) 逆转。

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OP-1118

OP-1118 Chemical Structure

CAS No. : 1030825-28-5

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OP-1118 相关抗体

Top Publications Citing Use of Products

查看 NF-κB 亚型特异性产品:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

OP-1118 (Fidaxomicin metabolite OP-1118) is an orally effective dual inhibitor of NF-κB and ERK1/2, with low systemic plasma exposure, no accumulation, and primary excretion via feces. By inhibiting the phosphorylation of NF-κB and ERK1/2 and reducing the expression of pro-inflammatory cytokines, OP-1118 exerts significant anti-inflammatory, cytoprotective, anti-apoptotic and antibacterial activities. In Clostridium difficile infection models, OP-1118 effectively blocks toxin-mediated intestinal inflammation, cell rounding, histological damage and apoptosis, and its protective effect can be reversed by PMA (HY-18739)[1][2][3].

IC50 & Target

ERK1

 

ERK2

 

体外研究
(In Vitro)

OP-1118 (60-120 μM; 预处理 30 min+4 h) 可剂量依赖性地抑制艰难梭菌 (C. difficile) 毒素 A 和毒素 B 介导的促炎细胞因子表达和 NF-κB 的磷酸化，以及新鲜人结肠外植体的组织学损伤[1]。
OP-1118 (120 μM; 预处理 30 min+4 h/1 h) 可阻断 C. difficile 毒素 A 诱导 RAW264.7 小鼠巨噬细胞中的 TNF-α 表达及 NF-κB 磷酸化和 ，且该效应可被 NF-κB 激活剂 PMA (HY-18739) 逆转[1]。
OP-1118 (120 μM; 预处理 30 min+8 h) 可抑制 C. difficile 毒素 A 和毒素 B 诱导人结肠上皮细胞 NCM460 中的细胞凋亡，且该效应可被 NF-κB 激活剂 PMA (HY-18739) 逆转[1]。
OP-1118 对艰难梭菌 (C. difficile) 的 MIC 范围为 0.25 至 2 μg/mL[1]。
OP-1118 (120 μM; 预处理 30 min+6 h) 可保护人结肠 CCD-18Co 成纤维细胞免受艰难梭菌毒素 A 介导的细胞变圆影响[2]。

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

OP-1118 相关抗体:

Apoptosis Analysis[1]

Cell Line: NCM460 human colonic epithelial cells
Concentration: 120 μM
Incubation Time: 30 min pretreatment followed by 8 h toxin A or B exposure
Result: Significantly reduced toxin A- and B-mediated apoptosis in NCM460 cells, as detected by TUNEL assay.
Lost antiapoptotic effect on toxin-exposed NCM460 cells when cells were pretreated with PMA.
体内研究
(In Vivo)

OP-1118 (6120 μM; 回肠袢内注射; 提前 30 min 注射) 可显著抑制雄性 C57BL/6 小鼠中艰难梭菌 (C. difficile) 毒素 A 介导的回肠组织学损伤、IL-1β 表达以及 ERK1/2 磷酸化[2]。
OP-1118 由 Fidaxomicin (HY-17580) 经口服给药产生，Fidaxomicin (30-75 mg/kg; p.o.; 单次) 与 OP-1118 的联合峰浓度分别可达 920 μg/g 和 1,600 μg/g[4]。

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

Animal Model: C57BL/6 (10-week-old male)[2]
Dosage: 60 μM; 120 μM
Administration: Intra-ileal loop injection; single dose; 30 minutes prior to toxin A
Result: Reduced mean histology score at 120 μM.
Reduced toxin A-induced ileal IL-1β protein expression and IL-1β mRNA expression at 120 μM.
Diminished toxin A-induced ERK1/2 phosphorylation in ileal mucosal tissues at 120 μM.
Failed to produce statistically significant reductions in toxin A-mediated histologic damage, IL-1β protein, or IL-1β mRNA expression at 60 μM.
Reduced basal ileal IL-1β protein expression in sham control mice at 120 μM.
分子量

987.95

Formula

C48H68Cl2O17
CAS 号
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

OP-1118 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

OP-11181030825-28-5Fidaxomicin metabolite OP-1118OP1118OP 1118Fidaxomicin metabolite OP1118Fidaxomicin metabolite OP 1118NF-κBERKApoptosisBacterialNuclear factor-κBNuclear factor-kappaBExtracellular signal regulated kinasesmale C57BL/6 miceproinflammatory cytokineERK1/2Clostridioides difficile infectionClostridium difficileNCM460 human colonic epithelial cellsRAW264.7 mouse macrophagesTNF-αhuman colonic CCD-18Co fibroblastsInhibitorinhibitorinhibit

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