PXS-5153A monohydrochloride

Name: PXS-5153A monohydrochloride
Brand: TargetMol
SKU: T12585L
Rating: 4.5 (1 reviews)

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Catalog No. T12585L

Alias PXS-5153A monohydrochloride (2125956-82-1 free base)

PXS-5153A monohydrochloride is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC 50 of <40 nM for LOXL2 across all mammalian species and an IC 50 of 63 nM for human LOXL3. PXS-5153A monohydrochloride dose-dependently reduced LOXL2-mediated collagen oxidation and collagen crosslinking in vitro which may represent an innovative therapeutic approach for the treatment of fibrosis

PXS-5153A monohydrochloride

😃Good

Catalog No. T12585LAlias PXS-5153A monohydrochloride (2125956-82-1 free base)

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$987	10-14 weeks	10-14 weeks
50 mg	$1,360	10-14 weeks	10-14 weeks
100 mg	$1,860	10-14 weeks	10-14 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Product Introduction

Bioactivity

Description	PXS-5153A monohydrochloride is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC 50 of <40 nM for LOXL2 across all mammalian species and an IC 50 of 63 nM for human LOXL3. PXS-5153A monohydrochloride dose-dependently reduced LOXL2-mediated collagen oxidation and collagen crosslinking in vitro which may represent an innovative therapeutic approach for the treatment of fibrosis
In vitro	PXS-5153A demonstrates potent inhibition of LOXL2 across various mammalian species, with an IC50 value of less than 40 nM. It also effectively inhibits human LOXL3, having an IC50 of 63 nM. This compound exhibits significant selectivity, being more than 40-fold more selective for LOXL2 over LOX and LOXL1, and exhibits over 700-fold selectivity against other related amine oxidases. Additionally, PXS-5153A acts rapidly, nearly completely inhibiting enzymatic activity within 15 minutes [1].
In vivo	As expected, rhLOXL2 induces collagen oxidation in a dose-dependent manner while PXS-5153A impedes collagen oxidation in a dose-dependent manner. Therapeutic treatment of PXS-5153A substantially reduces immature crosslink formation compared with the CCl 4 treated animals. Mature crosslink formation is also reduced by PXS-5153A treatment. All groups with therapeutic treatment of PXS-5153A show a significant reduction in DHLNL formation compared to the CCl 4 treated animals. Treatment with PXS-5153A causes a significantly reduction in HYP compared to the CCl 4 group. In addition, the amount of fibrillar collagen is markedly augmented by disease as seen by the 2.2-fold increase in percentage coverage area by Picrosirius red staining, which is reduced by PXS-5153A [1].
Synonyms	PXS-5153A monohydrochloride (2125956-82-1 free base)

Chemical Properties

Storage & Solubility Information

Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Solubility Information	DMSO: 250 mg/mL, Sonication is recommended.
In Vivo Formulation	10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL, Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc