PXS-5153A monohydrochloride

Name: PXS-5153A monohydrochloride
Brand: MedChemExpress
SKU: HY-114286A
Rating: 4.5 (1 reviews)

Cat. No.: HY-114286A Purity: 99.67%: FAQs
Data Sheet SDS COA Handling Instructions

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PXS-5153A monohydrochloride is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC₅₀ of <40 nM for LOXL2 across all mammalian species and an IC₅₀ of 63 nM for human LOXL3. PXS-5153A monohydrochloride could reduce crosslinks and ameliorates fibrosis.

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

PXS-5153A monohydrochloride Chemical Structure

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 338	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 338	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 990	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1650	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2250	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of PXS-5153A monohydrochloride:

PXS-5153A Get quote

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

In Vitro

PXS-5153A exhibits an IC₅₀ of <40 nM for LOXL2 across all mammalian species tested. PXS-5153A also inhibits human LOXL3 with an IC₅₀ value of 63 nM. PXS-5153A is >40-fold selective for LOXL2 over both LOX and LOXL1 and >700-fold selective over other related amine oxidases. PXS-5153A is a fast acting inhibitor, with enzymatic activity almost entirely blocked within 15 minutes ^[1].

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

In Vivo

As expected, rhLOXL2 dose-dependently induce oxidation of collagen with PXS-5153A dose-dependently impeding collagen oxidation. Therapeutic treatment of PXS-5153A substantially reduces immature crosslink formation compared with the CCl₄ 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 CCl₄ treated animals. Treatment with PXS-5153A causes a significantly reduction in HYP compared to the CCl₄ 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].

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

Molecular Weight

438.95

Formula

C₂₀H₂₄ClFN₄O₂S

Appearance

Solid

Color

Off-white to yellow

SMILES

CC(N1C/C(F)=C/CN)=C(C2=CC=CC(S(N(C)C)(=O)=O)=C2)C3=C1C=CC=N3.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 : 125 mg/mL (284.77 mM; ultrasonic and warming and heat to 60°C; 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	2.2782 mL	11.3908 mL	22.7816 mL
5 mM	0.4556 mL	2.2782 mL	4.5563 mL
10 mM	0.2278 mL	1.1391 mL	2.2782 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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: ≥ 2.08 mg/mL (4.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). 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 (20.8 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

Animal weight
(per animal)

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

Purity: 99.67%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (257 KB) LCMS (240 KB)

Handling Instructions (2659 KB)

References

[1]. Schilter H, et al. The lysyl oxidase like 2/3 enzymatic inhibitor, PXS-5153A, reduces crosslinks and ameliorates fibrosis. J Cell Mol Med. 2018 Dec 9. [Content Brief]

Animal Administration
^[1]

Rats^[1]
Sprague Dawley rats are orally administered with 0.25 μL/g Carbon tetrachloride (CCl₄) in olive oil solution, starting from day 0, 3 times per week for 6 weeks. PXS-5153A is given by oral gavage after 3 weeks of CCl₄ administration and continued throughout the remainder of the study at 3 mg/kg (low dose) or 10 mg/kg (high dose) once a day or 10 mg/kg (high dose) three times a week. Alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels were assessed in the plasma.
Mice
NASH is established in male C57/BL6 mice by a single subcutaneous injection of 200 μg streptozotocin after birth and with a high fat diet ad libitum after 4 weeks of age (day 28 ± 2) until 14 weeks of age. Mice are orally administered with 10 mg/kg PXS-5153A once daily from 8 to 14 weeks of age. ALT levels are assessed in the plasma.
Mice
Myocardial infarction (MI) is induced in C57/BL6 mice by occluding the left coronary artery. At 24 hours post-surgery, animals receive echocardiography. Infarcted mice with high cardiac function (FS > 40%) or low cardiac function (FS<10%) are excluded from the study. The remaining mice are treated q.d., p.o., with 25 mg/kg of PXS-5153A for 4 weeks. At the end of the experiment, echocardiography is performed on mice to assess left ventricular function and remodelling, followed by heart collection. The heart is fixed with 10% formalin. Fibrosis is assessed in the non-infarct area^[1].

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

References

[1]. Schilter H, et al. The lysyl oxidase like 2/3 enzymatic inhibitor, PXS-5153A, reduces crosslinks and ameliorates fibrosis. J Cell Mol Med. 2018 Dec 9. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2782 mL	11.3908 mL	22.7816 mL	56.9541 mL
	5 mM	0.4556 mL	2.2782 mL	4.5563 mL	11.3908 mL
	10 mM	0.2278 mL	1.1391 mL	2.2782 mL	5.6954 mL
	15 mM	0.1519 mL	0.7594 mL	1.5188 mL	3.7969 mL
	20 mM	0.1139 mL	0.5695 mL	1.1391 mL	2.8477 mL
	25 mM	0.0911 mL	0.4556 mL	0.9113 mL	2.2782 mL
	30 mM	0.0759 mL	0.3797 mL	0.7594 mL	1.8985 mL
	40 mM	0.0570 mL	0.2848 mL	0.5695 mL	1.4239 mL
	50 mM	0.0456 mL	0.2278 mL	0.4556 mL	1.1391 mL
	60 mM	0.0380 mL	0.1898 mL	0.3797 mL	0.9492 mL
	80 mM	0.0285 mL	0.1424 mL	0.2848 mL	0.7119 mL
	100 mM	0.0228 mL	0.1139 mL	0.2278 mL	0.5695 mL