2. MAPK/ERK Pathway Apoptosis Immunology/Inflammation
  3. p38 MAPK TNF Receptor Interleukin Related
  4. CBS-3408

CBS-3408 是一种具有口服活性的 p38α MAPK 抑制剂。CBS-3408 可抑制 TNFα 和 IL-1β 的释放。\nCBS-3408 可降低小鼠关节炎的疾病严重程度。CBS-3408 在大鼠内毒素血症模型中实现对 TNFα 释放的抑制。CBS-3408 可用于内毒素血症、关节炎的相关研究。

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CBS-3408

CBS-3408 Chemical Structure

CAS No. : 452056-93-8

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CBS-3408 相关抗体

Top Publications Citing Use of Products

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CBS-3408 is an orally active p38α MAPK inhibitor. CBS-3408 inhibits the release of TNFα and IL-1β.\nCBS-3408 reduces the disease severity of arthritis in mice. CBS-3408 inhibits TNFα release in a rat endotoxemia model. CBS-3408 can be used in studies related to endotoxemia and arthritis[1].

体外研究
(In Vitro)

CBS-3408 (Compound 3) 可抑制人全血中 LPS (HY-D1056) 诱导的 IL-1β 释放和 TNFα 释放[1]。
CBS-3408 (10 μM) 对 JNK3 和 p38β 激酶的抑制率超过 70%[1]。
CBS-3408 (10 μM) 可抑制 CYP2C9 (46%) 和 CYP2D6 (45%)，对 CYP1A2 的抑制作用较弱 (18%)，对 CYP2C19 或 CYP3A4 无相关活性[1]。

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

CBS-3408 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Tmax Cmax AUC0-t T1/2
Rat[1] 30 mg/kg p.o. 1.0 h 738 ng/mL 4928 ng·h/mL 3.0 h
体内研究
(In Vivo)

CBS-3408 (10 mg/kg；口服；单次给药) 可在 LPS 诱导的雄性 Wistar 大鼠内毒素血症模型中实现对 TNFα 释放的 97%抑制[1]。
CBS-3408 (50 mg/kg；口服；每日 2 次) 可显著降低雄性 DBA/1 小鼠 Collagen (HY-NP003) 诱导关节炎的疾病严重程度[1]。

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

Animal Model: Wistar (male)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose
Result: Achieved 97% inhibition of plasma TNFα concentrations compared to control animals.
Animal Model: DBA/1 (male)[1]
Dosage: 50 mg/kg
Administration: p.o.; twice daily
Result: Substantially reduced arthritic disease severity, with a notably lower arthritic score compared to vehicle control animals over the course of the study.
Showed no treatment-related toxicity aside from body weight loss identical to controls.
分子量

356.42

Formula

C18H17FN4OS
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

CBS-3408 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:

CBS-3408452056-93-8CBS3408CBS 3408p38 MAPKTNF ReceptorInterleukin RelatedTumor Necrosis Factor ReceptorTNFRILTNFαcollagen-induced arthritisp38α MAPKIL-1βDBA/1 micep38β MAPKJNK3LPS-stimulated human whole bloodWistar ratsLPS-induced endotoxemiaendotoxemiaarthritisInhibitorinhibitorinhibit

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