| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
For LOXL2, PXS-5153A monohydrochloride exhibits an IC50 of less than 40 nM in all tested mammalian species. With an IC50 of 63 nM, PXS-5153A monohydrochloride also inhibits human LOXL3. More than 700 times more selective than other comparable amine oxidases, PXS-5153A monohydrochloride is more than 40 times more selective for LOXL2 than LOX and LOXL1. The fast-acting inhibitor PXS-5153A monohydrochloride blocks enzyme activity almost entirely in 15 minutes [1].
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| ln Vivo |
PXS-5153A monohydrochloride dose-dependently inhibited collagen oxidation, whereas rhLOXL2 dose-dependently promoted it. When compared to animals treated with CCl4, treatment with PXS-5153A monohydrochloride dramatically decreased the production of immature cross-links. The treatment with PXS-5153A monohydrochloride also decreased the amount of mature cross-links that formed. When comparing the DHLNL formation of all groups receiving PXS-5153A monohydrochloride to the animals treated with CCl4, a substantial reduction was observed. When HYP was treated with PXS-5153A monohydrochloride, it was much lower than in the CCl4 group. Additionally, a 2.2-fold increase in the proportion of Sirius red stained area covered indicates that the disease considerably increases the amount of fibrillar collagen, whereas PXS-5153A decreases the area covered [1].
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| 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.
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| Molecular Formula |
C20H24CLFN4O2S
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|---|---|
| Molecular Weight |
438.95
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| Related CAS # |
PXS-5153A;2125956-82-1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~125 mg/mL (~284.77 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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