| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
3.7 μM (Bovine LOX), 3.4 μM (rh LOXL1), 0.4 μM (rh LOXL2), 1.5 μM (rh LOXL3), 0.3 μM (rh LOXL4)[1]
|
|---|---|
| ln Vitro |
PXS-6302 has excellent permeability through cell monolayers such MDCKII or Caco-2 cells[1].
|
| ln Vivo |
In pig models of excisional and burn injury, PXS-6302 inhibits LOX, lowers crosslinking, and enhances the appearance of scars[1]. In murine models of injury and fibrosis, topical application of PXS-6302 (1.5%, oil in water cream; 500 mg cream applied to 16 cm2; external application; once daily, for 28 days) reduces collagen deposition and cross-linkin[1]. PXS-6302 (0.5, 1.5, or 3%, oil in water cream; 400 mg cream applied to 16 cm2; external application; once daily, for 12 weeks) also dramatically reduces scar appearance without compromising tissue strength in pig injury models under topical administration[1].
|
| 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; once dayly, for 12 weeks Experimental Results: demonstrated Dramatically higher scores for the 3% treated scars suggesting significant improvement in scar appearance. |
| References |
| Molecular Formula |
C10H10F3NO2S
|
|---|---|
| Molecular Weight |
265.252111911774
|
| Exact Mass |
265.038
|
| CAS # |
2584947-54-4
|
| Related CAS # |
PXS-6302 hydrochloride;2584947-79-3
|
| PubChem CID |
155585072
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
1.2
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
17
|
| Complexity |
381
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC=C(C=C1)S(=O)(=O)C(/C(=C/CN)/F)(F)F
|
| InChi Key |
CQBDTOILYHIRIW-TWGQIWQCSA-N
|
| InChi Code |
InChI=1S/C10H10F3NO2S/c11-9(6-7-14)10(12,13)17(15,16)8-4-2-1-3-5-8/h1-6H,7,14H2/b9-6-
|
| Chemical Name |
(Z)-4-(benzenesulfonyl)-3,4,4-trifluorobut-2-en-1-amine
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~377.0 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (9.43 mM) 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; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 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 2: 2.5 mg/mL (9.43 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 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 | 3.7700 mL | 18.8501 mL | 37.7003 mL | |
| 5 mM | 0.7540 mL | 3.7700 mL | 7.5401 mL | |
| 10 mM | 0.3770 mL | 1.8850 mL | 3.7700 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
