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Shanghai Chaolan Chemical Technology Center Gold
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| Products Intro: |
Product Name:PS-5505
CAS:2409964-23-2
Purity:98% Package:50MG;100MG,1G,5G,100G
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| | PS-5505 Basic information |
| Product Name: | PS-5505 | | Synonyms: | PS-5505;PXS5505 HCl;LOX-IN-3 dihydrochloride;lysyl,LOXIN3 dihydrochloride,Inhibitor,oxidase,MAO,Monoamine Oxidase,fibrosis,inhibit,LOXL2,LOX IN 3 dihydrochloride;(Z)-3-Fluoro-4-(quinolin-8-ylsulfonyl)but-2-en-1-amine dihydrochloride;LOX-IN-3 dihydrochloride, 10 mM in DMSO | | CAS: | 2409964-23-2 | | MF: | C13H14ClFN2O2S | | MW: | 316.78 | | EINECS: | | | Product Categories: | | | Mol File: | 2409964-23-2.mol |  |
| | PS-5505 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO : 100 mg/mL (283.09 mM; Need ultrasonic) | | form | Solid | | color | Off-white to light yellow | | InChI | InChI=1S/C13H13FN2O2S.ClH/c14-11(6-7-15)9-19(17,18)12-5-1-3-10-4-2-8-16-13(10)12;/h1-6,8H,7,9,15H2;1H/b11-6-; | | InChIKey | WEFLTRNHDTUNKA-AVHZNCSWSA-N | | SMILES | S(C1=CC=CC2C=CC=NC1=2)(=O)(=O)C/C(/F)=C/CN.Cl |
| | PS-5505 Usage And Synthesis |
| Uses | LOX-IN-3 dihydrochloride is an orally active lysyl oxidase (LOX) inhibitor. LOX-IN-3 dihydrochloride can be used for fibrosis, cancer and angiogenesis research[1]. | | Biological Activity | LOX-IN-3 dihydrochloride is an orally active lysyl oxidase (LOX) inhibitor. LOX-IN-3 dihydrochloride can be used for fibrosis, cancer and/or angiogenesis research[1].
LOX-IN-3 (Compound 33) inhibits the bovine LOX and human LOXL2 activities with IC50 values of <10 μM and <1 μM, respectively. LOX-IN-3 is less active against SSAO/VAP-1 and MAO-B activities[1].
In young male Wistar rats, a single high (30 mg/kg) dose of LOX-IN-3 (Compound 33) completely abolishes lysyl oxidase activity. While plasma concentrations of LOX-IN-3 are far below the IC50 after 8 hours, the half-life of recovery is between 2-3 days (ear) and 24 hours (aorta)[1].In a 14-day unilateral ureteric obstruction (UUO) model, LOX-IN-3 (Compound 33, 10 mg/kg daily; orally) treatment increases kidney weight and thickness and reduces the area of fibrosis as measured by Picrosirius Red[1].In BALB/c mice bearing hepatic fibrosis, LOX-IN-3 (Compound 33, 20 mg/kg daily, i.p.) treatment significantly reduces liver fibrosis. At the end of week 4 a mouse breast cancer cell line (4tl) is injected orthotopically. LOX-IN-3 (Compound 33) treatment significantly reduces liver fibrosis, collagen cross-links and the metastatic load in the liver[1]. | | in vivo | LOX-IN-3 dihydrochloride monohydrate (Compound 33) (30 mg/kg; orally; once) inhibits lysyl oxidase activity in rats[1].
LOX-IN-3 dihydrochloride monohydrate (10 mg/kg; orally; daily for 14 days) reduces kidney fibrosis in unilateral ureteric obstruction (UUO) mice model[1].
LOX-IN-3 dihydrochloride monohydrate (15 mg/kg; orally; daily for 21 days) reduces lung fibrosis in mice[1]. | Animal Model: | Male Wistar rats[1] | | Dosage: | 30 mg/kg | | Administration: | Oral administration, single dose | | Result: | Completely abolished lysyl oxidase activity. Plasma concentrations of tested compound are far below the IC50 after 8 hours, the half-life of recovery is between 2-3 days (ear) and 24 hours (aorta). |
| Animal Model: | Unilateral ureteric obstruction (UUO) model of acute kidney fibrosis in mice[1] | | Dosage: | 10 mg/kg | | Administration: | Oral gavage, daily for 14 days | | Result: | Increased kidney weight and thickness and reduced the area of fibrosis. |
| Animal Model: | C57Bl/6 mice, Bleomycin-induced lung fibrosis model | | Dosage: | 15 mg/kg | | Administration: | Oral gavage, daily for 21 days | | Result: | Significantly reduced the Ashcroft score and the lung weight. |
| | References | [1]. Alison Dorothy Findlay, et al. Haloallylamine sulfone derivative inhibitors of lysyl oxidases and uses thereof. WO2020024017A1. |
| | PS-5505 Preparation Products And Raw materials |
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