| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
LOX (lysyl oxidase), LOXL1, LOXL2, LOXL3, LOXL4.
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|---|---|
| ln Vitro |
Caco-2 or MDCKII cell monolayers are extremely permeable to PXS-6302 hydrochloride [1].
PXS-6302 hydrochloride inhibits bovine LOX with an IC50 of 3.7 μM, and recombinant human LOXL1, LOXL2, LOXL3, and LOXL4 with IC50 values of 3.4 μM, 0.4 μM, 1.5 μM, and 0.3 μM, respectively. This broad-spectrum inhibition of the LOX family makes it a powerful tool for studying the role of these enzymes in extracellular matrix remodeling and fibrosis. |
| ln Vivo |
In pig resection and burn models, PXS-6302 hydrochloride inhibits LOX, lowers cross-linking, and enhances the appearance of scars[1]. PXS-6302 hydrochloride (1.5%, oil-in-water cream; 500 mg cream applied to 16 cm2; topical; once daily for 28 days) decreases collagen deposition and cross-linked proteins in a mouse injury model following topical treatment Fibrosis[1]. PXS-6302 hydrochloride (0.5, 1.5 or 3%, oil-in-water cream; 400 mg cream, administered to 16 cm2; topical; once daily for 12 weeks) also considerably improves scar appearance without compromising scar localization Tissue strength of pig injury model during application[1].
In porcine models of excisional and burn injury, PXS-6302 hydrochloride effectively inhibits LOX activity, reduces crosslinking, and significantly improves scar appearance. In a mouse injury model, topical application of PXS-6302 hydrochloride (1.5% in an oil-in-water cream) reduces collagen deposition and crosslinked protein, thereby decreasing local fibrosis. |
| Enzyme Assay |
In vitro enzyme assays are performed to determine the inhibitory activity of PXS-6302 hydrochloride against LOX and LOXL isoenzymes. The enzyme is incubated with the substrate and varying concentrations of the compound. The inhibition of enzyme activity is measured by monitoring the production of hydrogen peroxide or the formation of fluorescent products, and IC50 values are calculated from the concentration-response curves.
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| Cell Assay |
For in vitro cellular assays, fibroblasts or other cell types that produce LOX are treated with PXS-6302 hydrochloride. The effect of the compound on LOX activity and collagen crosslinking is assessed by measuring the levels of specific crosslinks or by analyzing the extracellular matrix composition. This helps to understand the cellular effects of LOX inhibition.
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| Animal Protocol |
Animal/Disease Models: Porcine excision injury model (female Juvenile pigs, 18-20 kg)[1].
Doses: 0.5, 1.5, or 3%, oil in water cream; 400 mg cream applied to 16 cm2 Route of Administration: External application; 1, 2 and 3 weeks post-injury; one time/day, for 12 weeks Experimental Results: demonstrated Dramatically higher scores for the 3% treated scars suggesting significant improvement in scar appearance. In vivo studies are conducted in animal models of wound healing and fibrosis. PXS-6302 hydrochloride is typically applied topically (e.g., as a cream) to the affected area. The effects on scar formation, collagen deposition, and tissue remodeling are evaluated histologically and biochemically. Its skin penetrability makes it suitable for topical applications. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for PXS-6302 hydrochloride. As a compound designed for topical application, its local absorption and systemic exposure would be key parameters to study. Its skin penetrability suggests it can reach the target tissues in the dermis.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available. However, its mechanism of action as an irreversible LOX inhibitor suggests a potential for on-target toxicity related to the essential role of LOX in connective tissue maintenance. Standard toxicology studies would be required to assess its safety for therapeutic use.
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| References | |
| Additional Infomation |
PXS-6302 hydrochloride is a promising preclinical candidate for the treatment of fibrosis and scarring. Its potent and irreversible inhibition of LOX and LOXL isoforms, combined with its skin penetrability, makes it a valuable tool for studying these conditions. It is not approved for clinical use and is currently for research purposes only. Its in vivo efficacy in improving scar appearance highlights its therapeutic potential.
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| Molecular Formula |
C10H11CLF3NO2S
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|---|---|
| Molecular Weight |
301.713051080704
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| Exact Mass |
301.015
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| CAS # |
2584947-79-3
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| Related CAS # |
PXS-6302;2584947-54-4
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| PubChem CID |
155585071
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
18
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| Complexity |
381
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)S(=O)(=O)C(/C(=C/CN)/F)(F)F.Cl
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| InChi Key |
UOENLHPLNJYJTC-BORNJIKYSA-N
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| InChi Code |
InChI=1S/C10H10F3NO2S.ClH/c11-9(6-7-14)10(12,13)17(15,16)8-4-2-1-3-5-8;/h1-6H,7,14H2;1H/b9-6-;
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| Chemical Name |
(Z)-4-(benzenesulfonyl)-3,4,4-trifluorobut-2-en-1-amine;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~331.4 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (4.14 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (12.5 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (4.14 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (12.5 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 1.25 mg/mL (4.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (12.5 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3144 mL | 16.5722 mL | 33.1444 mL | |
| 5 mM | 0.6629 mL | 3.3144 mL | 6.6289 mL | |
| 10 mM | 0.3314 mL | 1.6572 mL | 3.3144 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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