| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
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LOX-IN-3 (PXS5505; PXS-5505) dihydrochloride is a novel and oral inhibitor of lysyl oxidase (LOX) with potential usefulness for treatment of a variety of disorders, e.g., fibrosis, cancer and angiogenesis in human subjects as well as in pets and livestock.
| ln Vitro |
LOX-IN-3 dihydrochloride monohydrate (compound 33) has an IC50 value of less than 10 μM for bovine LOX and less than 1 μM for human LOXL2 activity [1]. LOXL1 and LOXL2 are consistently inhibited by LOX-IN-3 dihydrochloride monohydrate [1]. The monohydrate of LOX-IN-3 dihydrochloride has reduced activity in relation to SSAO/VAP-1 and MAO-B [1].
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| ln Vivo |
LOX-IN-3 dihydrochloride monohydrate (Compound 33) (30 mg/kg; oral; once) suppresses rat lysyl oxidase activity [1]. LOX-IN-3 dihydrochloride monohydrate (10 mg/kg; oral; once daily for 14 days) decreases renal fibrosis in a mouse model of unilateral ureteral obstruction (UUO) [1]. LOX-IN-3 dihydrochloride monohydrate (15 mg/kg; orally; once daily for 21 days) decreases lung fibrosis in rats [1].
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| Animal Protocol |
Animal/Disease Models: Male Wistar rat[1]
Doses: 30 mg/kg Route of Administration: Orally, single dose Experimental Results:Complete elimination of lysyl oxidase activity. Plasma concentrations of the test compound were well below the IC50 after 8 hrs (hrs (hours)), and the recovery half-life was between 2-3 days (ear) and 24 hrs (hrs (hours)) (aorta). Animal/Disease Models: Mouse unilateral ureteral obstruction (UUO) model of acute renal fibrosis [1] Doses: 10 mg/kg Route of Administration: po (oral gavage), one time/day for 14 days Experimental Results: Increased kidney weight and thickness, fiber The area is diminished. Animal/Disease Models: C57Bl/6 mice, bleomycin-induced pulmonary fibrosis model. Doses: 15 mg/kg. Route of Administration: po (oral gavage), one time/day for 21 days. Experimental Results: Dramatically diminished Ashcroft score and lung weight. |
| References |
[1]. Alison Dorothy Findlay, et al. Haloallylamine sulfone derivative inhibitors of lysyl oxidases and uses thereof. WO2020024017A1.
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| Molecular Formula |
C13H14CLFN2O2S
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|---|---|
| Molecular Weight |
316.7789
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| CAS # |
2409964-23-2
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| Related CAS # |
LOX-IN-3;2409963-83-1;LOX-IN-3 dihydrochloride monohydrate;2414974-55-1
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| SMILES |
Cl[H].S(C([H])([H])/C(=C(\[H])/C([H])([H])N([H])[H])/F)(C1=C([H])C([H])=C([H])C2C([H])=C([H])C([H])=NC1=2)(=O)=O
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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) |
H2O : ≥ 100 mg/mL (~283.09 mM)
DMSO : ~33.33 mg/mL (~94.36 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.08 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 25.0 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: ≥ 2.5 mg/mL (7.08 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1568 mL | 15.7838 mL | 31.5676 mL | |
| 5 mM | 0.6314 mL | 3.1568 mL | 6.3135 mL | |
| 10 mM | 0.3157 mL | 1.5784 mL | 3.1568 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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