1. Immunology/Inflammation Metabolic Enzyme/Protease
  2. COX Phospholipase
  3. VI-60

VI-60 是一种具有口服活性的 cPLA2COX-2 双效抑制剂,通过抑制 p38 MAPK/cPLA2/COX-2/PGE2 通路表达抗炎症活性。

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VI-60 Chemical Structure

VI-60 Chemical Structure

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2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VI-60 is a dual, orally active inhibitor of cPLA2 and COX-2, which reveals an anti-inflammtory efficacy through the inhibition of p38 MAPK/cPLA2/COX-2/PGE2 pathway[1].

IC50 & Target

COX-2

 

cPLA2

 

体外研究
(In Vitro)

VI-60 (10 μΜ,24-48 h) 抑制 LPS 诱导的炎症介质 NO (IC50 为 3.85 μM) 和 PGE2 的产生,在 RAW264.7 中没有显著的细胞毒性[1]

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

Cell Cytotoxicity Assay[1]

Cell Line: RAW264.7
Concentration: 30 μΜ
Incubation Time: 24-48 h
Result: Exhibite cell viability of nearly 100%, in compare to the verhicle group.

Western Blot Analysis[1]

Cell Line: RAW264.7
Concentration: 30 μΜ, 2.5-10 μM
Incubation Time: 30 μM for 2 h, 2.5-10 μM for 1 h
Result: Downregulated the phosphor-p38-MAPK, cPLA2 and COX2, stabilized the cPLA2 and COX2 proteins when heated.
体内研究
(In Vivo)

VI-60 (20 mg/kg,口服,每天或每两天) 改善佐剂诱导的关节炎,对 Lewis 大鼠具有镇痛作用[1]
VI-60 (20 mg/kg,口服,每天) 用过抑制 p38 MAPK/cPLA2/COX-2/PGE2 通路调节 Th17 和 Tregs 平衡,减少 IL-17 表达[1]
VI-60 在 Wistar 鼠体内表现出较低的溃疡可能性 (50 mg/kg),不具有肝毒性或肾毒性 (20 mg/kg,口服)[1]

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

Animal Model: Adjuvant-induced arthritis in Lewis rats[1]
Dosage: 20 mg/kg
Administration: p.o., every 24 h or 48 h for 20 days
Result: Inhibited the weight loss and the edema of paws, increased the mechanical withdrawal threshold (MWT), decreased the spleen weights.
Animal Model: Male mistar rats[1]
Dosage: 20 mg/kg
Administration: p.o., for 3 days
Result: Revealed identical indexes of glutamic pyruvic transaminase (GPT), glutamic oxalacetic transaminase (GOT), and blood urea nitrogen (BUN) as of normal rats.
分子量

592.73

Formula

C37H43F3O3

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
VI-60
目录号:
HY-162228
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