PXS-5153A monohydrochloride
Based on 1 publication(s) in Google Scholar
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.
- Purity: 99.14%
- Formula: C20H24ClFN4O2S
- Molecular Weight:438.95
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PXS-5153A monohydrochloride
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Biological Activity
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Molecular Weight 438.95
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Formula C20H24ClFN4O2S
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Color Off-white to yellow
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SMILES
CC(N1C/C(F)=C/CN)=C(C2=CC=CC(S(N(C)C)(=O)=O)=C2)C3=C1C=CC=N3.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Neuron
2024 Sep 25;112(18):3089-3105.e7. PMID: 39191260
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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 | 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 |
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