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

PXS-6302 hydrochloride 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 hydrochloride has readily skin penetrability, reduces collagen deposition and significantly improves scar appearance.

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

PXS-6302 hydrochloride Chemical Structure

PXS-6302 hydrochloride Chemical Structure

CAS No. : 2584947-79-3

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Based on 1 publication(s) in Google Scholar

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Description

PXS-6302 hydrochloride 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 hydrochloride has readily skin penetrability, reduces collagen deposition and significantly improves scar appearance[1].

In Vitro

PXS-6302 hydrochloride 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 hydrochloride inhibits LOX, reduces crosslinking and improves scar appearance in porcine models of excisional and burn injury[1].
PXS-6302 hydrochloride (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 hydrochloride (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. 2584947-54-4 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. Purity & Documentation Data Sheet (270 KB)Handling Instructions (2659 KB) References [1]. Chaudhari N, et al. Topical application of an irreversible small molecule inhibitor of lysyl oxidases ameliorates skin scarring and fibrosis. Nat Commun. 2022 Sep 22;13(1):5555. [Content Brief]
Molecular Weight

301.71

Formula

C10H11ClF3NO2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC/C=C(C(F)(S(=O)(C1=CC=CC=C1)=O)F)\F.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (331.44 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 3.3144 mL 16.5722 mL 33.1444 mL
5 mM 0.6629 mL 3.3144 mL 6.6289 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (4.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 1.25 mg/mL (4.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3144 mL 16.5722 mL 33.1444 mL 82.8610 mL
5 mM 0.6629 mL 3.3144 mL 6.6289 mL 16.5722 mL
10 mM 0.3314 mL 1.6572 mL 3.3144 mL 8.2861 mL
15 mM 0.2210 mL 1.1048 mL 2.2096 mL 5.5241 mL
20 mM 0.1657 mL 0.8286 mL 1.6572 mL 4.1431 mL
25 mM 0.1326 mL 0.6629 mL 1.3258 mL 3.3144 mL
30 mM 0.1105 mL 0.5524 mL 1.1048 mL 2.7620 mL
40 mM 0.0829 mL 0.4143 mL 0.8286 mL 2.0715 mL
50 mM 0.0663 mL 0.3314 mL 0.6629 mL 1.6572 mL
60 mM 0.0552 mL 0.2762 mL 0.5524 mL 1.3810 mL
80 mM 0.0414 mL 0.2072 mL 0.4143 mL 1.0358 mL
100 mM 0.0331 mL 0.1657 mL 0.3314 mL 0.8286 mL
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PXS-6302 hydrochloride Related Classifications

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PXS-6302 hydrochloride
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