| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C10H11ClF3NO2S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
PXS-6302 hydrochloride is an irreversible lysyl oxidase inhibitor, with IC50 values of 3.7 μM against bovine LOX, 3.4 μM against recombinant human LOXL1, 0.4 μM against recombinant human LOXL2, 1.5 μM against recombinant human LOXL3, and 0.3 μM against recombinant human LOXL4. It readily penetrates skin, reduces collagen deposition, and significantly improves scar appearance[1]. It is supplied as a white to off-white solid (C10H11ClF3NO2S, MW 301.71) at 99.57% purity.
Physical & Chemical Properties
| CAS Number | 2584947-79-3 |
|---|---|
| Molecular Formula | C10H11ClF3NO2S |
| Molecular Weight | 301.71 g/mol |
| Purity | 99.57% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | NC/C=C(C(F)(S(=O)(C1=CC=CC=C1)=O)F)\F.[H]Cl |
| Signaling Pathway | Neuronal Signaling |
| Solubility | In Vitro: DMSO: 100 mg/mL (331.44 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (331.44 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 1.25 mg/mL (4.14 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1.25 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (12.5 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 1.25 mg/mL (4.14 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1.25 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (12.5 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 1.25 mg/mL (4.14 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1.25 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (12.5 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
PXS-6302 hydrochloride shows high permeability across a monolayer of cells, such as Caco-2 or MDCKII cells[1].
In Vivo
In porcine models of excisional and burn injury, PXS-6302 hydrochloride inhibits LOX, reduces crosslinking, and improves scar appearance[1]. Topical PXS-6302 hydrochloride (1.5% oil in water cream) applied externally once daily for 28 days, at 500 mg cream per 16 cm2, reduces collagen deposition and cross-linking in murine models of injury and fibrosis[1]. Topical PXS-6302 hydrochloride (0.5, 1.5, or 3% oil in water cream) applied externally at 400 mg cream per 16 cm2 once daily for 12 weeks also significantly improves scar appearance in porcine injury models, without reducing tissue strength[1].
| Animal Model | Porcine excision injury model (female Juvenile pigs, 18-20 kg)[1]. |
|---|---|
| Dosage | 0.5, 1.5, or 3%, oil in water cream; 400 mg cream applied to 16 cm2 |
| Administration | External application; 1, 2 and 3 weeks post-injury; once dayly, for 12 weeks |
| Result | Showed significantly higher scores for the 3% treated scars suggesting significant improvement in scar appearance. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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