1. Neuronal Signaling
  2. Monoamine Oxidase
  3. PXS-6302

PXS-6302 is an irreversible lysyl oxidase inhibitor with IC50s of 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), respectively. PXS-6302 has readily skin penetrability, reduces collagen deposition and significantly improves scar appearance.

For research use only. We do not sell to patients.

PXS-6302 Chemical Structure

PXS-6302 Chemical Structure

CAS No. : 2584947-54-4

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Description

PXS-6302 is an irreversible lysyl oxidase inhibitor with IC50s of 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), respectively. PXS-6302 has readily skin penetrability, reduces collagen deposition and significantly improves scar appearance[1].

IC50 & Target

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]

In Vitro

PXS-6302 demonstrates high permeability to across a monolayer of cells, such as Caco-2 or MDCKII cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PXS-6302 inhibits LOX, reduces crosslinking and improves scar appearance in porcine models of excisional and burn injury[1].
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 in murine models of injury and fibrosis under topical application[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 significantly improves scar appearance without reducing tissue strength in porcine injury models under topical application[1].

MedChemExpress (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: 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.
Molecular Weight

265.25

Formula

C10H10F3NO2S

CAS No.
SMILES

NC/C=C(C(F)(S(=O)(C1=CC=CC=C1)=O)F)\F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (377.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table
  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (9.43 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (9.43 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7700 mL 18.8501 mL 37.7003 mL 94.2507 mL
5 mM 0.7540 mL 3.7700 mL 7.5401 mL 18.8501 mL
10 mM 0.3770 mL 1.8850 mL 3.7700 mL 9.4251 mL
15 mM 0.2513 mL 1.2567 mL 2.5134 mL 6.2834 mL
20 mM 0.1885 mL 0.9425 mL 1.8850 mL 4.7125 mL
25 mM 0.1508 mL 0.7540 mL 1.5080 mL 3.7700 mL
30 mM 0.1257 mL 0.6283 mL 1.2567 mL 3.1417 mL
40 mM 0.0943 mL 0.4713 mL 0.9425 mL 2.3563 mL
50 mM 0.0754 mL 0.3770 mL 0.7540 mL 1.8850 mL
60 mM 0.0628 mL 0.3142 mL 0.6283 mL 1.5708 mL
80 mM 0.0471 mL 0.2356 mL 0.4713 mL 1.1781 mL
100 mM 0.0377 mL 0.1885 mL 0.3770 mL 0.9425 mL
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PXS-6302 Related Classifications

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.

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PXS-6302
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