1. Metabolic Enzyme/Protease
  2. MMP
  3. CP-471474

CP-471474 是一个口服有效的、广泛的 MMP 抑制剂,IC50 值分别为1170 nM (MMP-1)、0.7 nM (MMP-2)、16 nM (MMP-3)、13 nM (MMP-9) 和 0.9 nM (MMP-13)。

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CP-471474 Chemical Structure

CP-471474 Chemical Structure

CAS No. : 210755-45-6

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CP-471474 is an orally active and pan MMP inhibitor, with IC50 values of 1170 nM (MMP-1), 0.7 nM (MMP-2), 16 nM (MMP-3), 13 nM (MMP-9) and 0.9 nM (MMP-13), respectively[1][2].

IC50 & Target[1]

MMP-2

0.7 nM (IC50)

MMP-13

0.9 nM (IC50)

MMP-9

13 nM (IC50)

MMP-3

16 nM (IC50)

MMP-1

1170 nM (IC50)

体内研究
(In Vivo)

CP-471474 plasma levels following subcutaneous injection are 2,020 ng/mL (1 h postdose) to 160 ng/mL (6 h postdose)[2].
CP-471,474 significantly reduces both the extent and severity of inflammation at 2 months. At 4 months, a spontaneous reduction of the inflammatory response is observed in both treated and untreated animals, and consequently no difference is observed between both[2].
CP-471474 significantly decreases the destructive lesions mainly at 2 months and also at 4 months[2].

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

Animal Model: Guinea pigs weighing 400 to 450 g (COPD)[2].
Dosage: 20 mg/kg (also supplemented daily by the diet (200 mg/200 g powdered chow)).
Administration: Subcutaneously (in 20% ethanol/80% polyethylene glycol), once a day during the entire course.
Result: Lungs derived from smoking animals treated with the compound demonstrated a statistically significant reduction in the destructive lesions.
Showed an increase of both pro–MMP-9 and its active form (lanes 5 to 8) as compared with control animals.
分子量

368.38

Formula

C16H17FN2O5S

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

CP-471474 相关分类

  • 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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