1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. PDE4-IN-6

PDE4-IN-6 是一种有效、安全且具有中等选择性的 PDE4 抑制剂,对 PDE4B 和 PDE4D 的 IC50 分别为 0.125和0.43 µM。PDE4-IN-6 可下调 TNF-α 和 IL-6 的表达水平。PDE4-IN-6 具有强大的免疫调节活性,具有抗类风湿性关节炎的研究潜力。还具有抗炎、抗关节炎的作用。

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PDE4-IN-6 Chemical Structure

PDE4-IN-6 Chemical Structure

1.  客户无需承担相应的运输费用。

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

规格 是否有货
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PDE4-IN-6 is a potent, safe and moderately selective PDE4 inhibitor with IC50s of 0.125 and 0.43 µM for PDE4B and PDE4D, respectively. PDE4-IN-6 can downregulate the expression level of TNF-α and IL-6. PDE4-IN-6 has potent immunomodulatory activity thereby its potential against rheumatoid arthritis. Anti-inflammatory and anti-arthritic effects[1].

IC50 & Target

PDE4B

0.125 μM (IC50)

PDE4D

0.43 μM (IC50)

体外研究
(In Vitro)

PDE4-IN-6 (compound 5f) (0.1-10 µM; 1 hour) has concentration-dependent inhibition on TNF-α in Raw 264.7 cells, with 42.3, 49.6, 57.2 and 68.7% inhibition at concentration of 0.3, 1, 3 and 10 µM[1].

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

RT-PCR

Cell Line: Raw 264.7 cells[1]
Concentration: 0.1-10 µM
Incubation Time: 1 hour
Result: Showed concentration-dependent inhibition on TNF-α, with 42.3, 49.6, 57.2 and 68.7% inhibition at concentration of 0.3, 1, 3 and 10 µM.
体内研究
(In Vivo)

PDE4-IN-6 (10 and 30 mg/kg; i.p.; daily from day 11 until day 20) can improve body weight and reduce paw swelling, also ameliorate joint space narrowing, cartilage degeneration and joint structural deformity in AIA rats at dosing 30 mg/kg[1].
PDE4-IN-6 (1-100 μM; incubated 4 days, 3 days or 4 hours) does not induce teratogenicity, hepatotoxicity and cardiac toxicity in zebrafish embryos[1].

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

Animal Model: Adjuvant-induced arthritis (AIA) albino wistar rats (150-200 g)[1]
Dosage: 10 and 30 mg/kg
Administration: i.p.; daily from day 11 until day 20
Result: Improved body weight and reduced paw swelling, also ameliorated joint space narrowing, cartilage degeneration and joint structural deformity at dosing 30 mg/kg, depicting the anti-inflammatory and anti-arthritic effects in AIA model.
分子量

465.49

Formula

C25H20FNO5S

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:
PDE4-IN-6
目录号:
HY-115913
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