2. Neuronal Signaling
  3. Monoamine Oxidase
  4. 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 LOX 的 IC50 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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PXS-4787 相关抗体

Top Publications Citing Use of Products

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MAO-A MAO-B

  • 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.

PXS-4787 相关抗体:

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.
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 25 mg/mL (109.04 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.3617 mL 21.8083 mL 43.6167 mL
5 mM 0.8723 mL 4.3617 mL 8.7233 mL
查看完整储备液配制表

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

PXS-4787 相关分类

完整储备液配制表

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.3617 mL 21.8083 mL 43.6167 mL 109.0417 mL
5 mM 0.8723 mL 4.3617 mL 8.7233 mL 21.8083 mL
10 mM 0.4362 mL 2.1808 mL 4.3617 mL 10.9042 mL
15 mM 0.2908 mL 1.4539 mL 2.9078 mL 7.2694 mL
20 mM 0.2181 mL 1.0904 mL 2.1808 mL 5.4521 mL
25 mM 0.1745 mL 0.8723 mL 1.7447 mL 4.3617 mL
30 mM 0.1454 mL 0.7269 mL 1.4539 mL 3.6347 mL
40 mM 0.1090 mL 0.5452 mL 1.0904 mL 2.7260 mL
50 mM 0.0872 mL 0.4362 mL 0.8723 mL 2.1808 mL
60 mM 0.0727 mL 0.3635 mL 0.7269 mL 1.8174 mL
80 mM 0.0545 mL 0.2726 mL 0.5452 mL 1.3630 mL
100 mM 0.0436 mL 0.2181 mL 0.4362 mL 1.0904 mL
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:

PXS-47872409963-50-2PXS4787PXS 4787Monoamine OxidaseMAOskin treatmentpenetrating skincollagen depositionscar appearancescar tissuemurine models of injury and fibrosisporcine injury modelsInhibitorinhibitorinhibit

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目录号：
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