1. Neuronal Signaling
  2. Monoamine Oxidase
  3. PXS-4787

PXS-4787 是一种特异、有效的泛赖氨酸氧化酶 (lysyl oxidase) 抑制剂,能够消除赖氨酸氧化酶活性。PXS-4787 抑制 LOXIC50 分别为 2 μM (Bovine LOX),3.2 μM (rh LOXL1),0.6 μM (rh LOXL2),1.4 μM (rh LOXL3),0.2 μM (rh LOXL4)。

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PXS-4787 Chemical Structure

PXS-4787 Chemical Structure

CAS No. : 2409963-50-2

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查看 Monoamine Oxidase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PXS-4787 is a specific and effective pan-LOX (lysyl oxidase) inhibitor for abolishing lysyl oxidase activity. PXS-4787 inhibits LOX with IC50s of 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), 0.2 μM (rh LOXL4), respectively[1].

IC50 & Target

2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), 0.2 μM (rh LOXL4)[1]

体外研究
(In Vitro)

Lysyl oxidases stabilize the main component of scar tissue, collagen, and drive scar stiffness and appearance[1].
PXS-4787 (0-10 μM; 15 min-4 h) dose- and time-dependently inhibits lysyl oxidase and displays comparable inhibitory activity across species[1].
PXS-4787 (0-100 μM; 72 h) is well tolerated by primary human dermal fibroblasts, (10 μM; 11 d) reduces collagen formation, deposition and crosslinking in primary human dermal fibroblasts cultured in vitro[1].
PXS-4787 (10 μM; 48 h) induces differential gene expression in fibroblasts and keratinocytes, including COL1A1, LOX, GAPDH, PGK1[1].

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

Immunofluorescence[1]

Cell Line: Primary human dermal fibroblasts cultured in vitro
Concentration: 0, 1, 10 μM
Incubation Time: 11 days
Result: Significantly reduced in the 10 µM treatment group.

RT-PCR[1]

Cell Line: Cultured fibroblasts and keratinocytes (isolated from five different patients)
Concentration: 10 μM
Incubation Time: 48 hours
Result: Resulted four genes with significant differential expression in fibroblasts and two differentially expressed genes in keratinocytes.
体内研究
(In Vivo)

PXS-4787 (3%, oil in water cream; external application; once daily, for 28 days) reduces collagen deposition and cross-linkin in murine models of injury and fibrosis under topical application[1].
PXS-4787 (3%, oil in water cream; external application; once daily, for 12 weeks) also significantly improves scar appearance without reducing tissue strength in porcine injury models under topical application[1].

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

Animal Model: Porcine excision injury model (female Juvenile pigs, 18-20 kg)[1]
Dosage: 3%, oil in water cream; 400 mg cream applied to 16 cm2
Administration: External application; 1, 2 and 3 weeks post-injury; once dailly, for 12 weeks
Result: Improved the appearance of scar in relevant in vivo models, indicative of a targetdriven, as opposed to compound-specific, effect.
分子量

229.27

Formula

C10H12FNO2S

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

PXS-4787 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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产品名称:
PXS-4787
目录号:
HY-151498
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