This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
PXS-4787
Catalog No. T60296 CAS
2409963-50-2
PXS-4787 is a potent and selective inhibitor of lysyl oxidase (LOX) with broad-spectrum activity. It effectively suppresses lysyl oxidase activity by acting on its mechanisms. The compound displays inhibitory effects with IC50 values of 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), and 0.2 μM (rh LOXL4), respectively [1].
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage
& Solubility Information
Description
PXS-4787 is a potent and selective inhibitor of lysyl oxidase (LOX) with broad-spectrum activity. It effectively suppresses lysyl oxidase activity by acting on its mechanisms. The compound displays inhibitory effects with IC50 values of 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), and 0.2 μM (rh LOXL4), respectively [1].
In vitro
PXS-4787, in a concentration and time-dependent manner, inhibits lysyl oxidase—a key enzyme in stabilizing collagen in scar tissue, thereby affecting scar stiffness and appearance. This compound exhibits consistent inhibitory effects across different species. When tested on primary human dermal fibroblasts, PXS-4787 is well-tolerated, and specific dosages (e.g., 10 μM for up to 11 days) can significantly reduce collagen formation, deposition, and crosslinking in these cells. Additionally, a particular dose (10 μM for 48 hours) alters the expression of certain genes in fibroblasts and keratinocytes, such as COL1A1, LOX, GAPDH, and PGK1, indicating its potential for modifying cellular responses related to scarring. Immunofluorescence and RT-PCR studies further confirm the compound's efficacy in reducing collagen in treated groups and in inducing gene expression changes, underscoring its therapeutic potential in managing scar formation and appearance.
In vivo
PXS-4787, a 3% oil-in-water cream applied topically once daily, reduces collagen deposition and cross-linking in murine injury and fibrosis models over 28 days and enhances scar appearance without compromising tissue strength in porcine injury models over 12 weeks, suggesting a target-driven benefit. In a specific porcine excision injury model using female juvenile pigs weighing 18-20 kg, a 400 mg dose of the cream was applied externally to a 16 cm^2 area once daily starting 1, 2, and 3 weeks post-injury for a duration of 12 weeks. The results indicate an improved scar appearance in relevant in vivo models, supporting the compound's therapeutic potential in wound healing and fibrosis.
Molecular Weight
229.27
Formula
C10H12FNO2S
CAS No.
2409963-50-2
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dose Conversion
You can also refer to dose conversion for different animals.
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Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
Tween 80,mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL Corn oil,mix and clarify.
Note:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.