Product Name :
PXS-5120A
Description:
PXS-5120A is a potent, irreversible fluoroallylamine inhibitor of Lysyl Oxidase-like 2/3 (LOXL2/3) with anti-fibrotic activity. PXS-5120A is >300-fold selective for LOXL2 (Ki of 83 nM; pIC50 of 8.4) over LOXL (pIC50 of 5.8).
CAS:
2125955-70-4
Molecular Weight:
481.97
Formula:
C22H25ClFN3O4S
Chemical Name:
1-[(2Z)-4-amino-2-fluorobut-2-en-1-yl]-3-[3-(dimethylsulfamoyl)phenyl]-2-methyl-1H-indole-5-carboxylic acid hydrochloride
Smiles :
Cl.CN(C)S(=O)(=O)C1=CC(=CC=C1)C1C2=CC(=CC=C2N(C/C(/F)=C/CN)C=1C)C(O)=O
InChiKey:
PWSRWJMEGVKWES-WPTDRQDKSA-N
InChi :
InChI=1S/C22H24FN3O4S.ClH/c1-14-21(15-5-4-6-18(11-15)31(29,30)25(2)3)19-12-16(22(27)28)7-8-20(19)26(14)13-17(23)9-10-24;/h4-9,11-12H,10,13,24H2,1-3H3,(H,27,28);1H/b17-9-;
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Luteolin} MedChemExpress|{Luteolin} Apoptosis|{Luteolin} Technical Information|{Luteolin} In Vitro|{Luteolin} custom synthesis|{Luteolin} Autophagy}
Shelf Life:
≥12 months if stored properly.{{Halo tag TMR} MedChemExpress|{Halo tag TMR} {Fluorescent Dye}|{Halo tag TMR} Purity & Documentation|{Halo tag TMR} References|{Halo tag TMR} custom synthesis|{Halo tag TMR} Cancer}
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
PXS-5120A is a potent, irreversible fluoroallylamine inhibitor of Lysyl Oxidase-like 2/3 (LOXL2/3) with anti-fibrotic activity. PXS-5120A is >300-fold selective for LOXL2 (Ki of 83 nM; pIC50 of 8.4) over LOXL (pIC50 of 5.8).|Product information|CAS Number: 2125955-70-4|Molecular Weight: 481.PMID:27102143 97|Formula: C22H25ClFN3O4S|Chemical Name: 1-[(2Z)-4-amino-2-fluorobut-2-en-1-yl]-3-[3-(dimethylsulfamoyl)phenyl]-2-methyl-1H-indole-5-carboxylic acid hydrochloride|Smiles: Cl.CN(C)S(=O)(=O)C1=CC(=CC=C1)C1C2=CC(=CC=C2N(C/C(/F)=C/CN)C=1C)C(O)=O|InChiKey: PWSRWJMEGVKWES-WPTDRQDKSA-N|InChi: InChI=1S/C22H24FN3O4S.ClH/c1-14-21(15-5-4-6-18(11-15)31(29,30)25(2)3)19-12-16(22(27)28)7-8-20(19)26(14)13-17(23)9-10-24;/h4-9,11-12H,10,13,24H2,1-3H3,(H,27,28);1H/b17-9-;|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|PXS-5120A (Compound 12k) is a potent inhibitor of the LOXL2/3 enzyme and a moderate blocker of LOXL4. PXS-5120A inhibits recombinant human LOXL2, human fibroblast LOXL2, recombinant mouse LOXL2, recombinant rat LOXL2, collagen oxidation assay, recombinant human LOXL3 and recombinant human LOXL4 with IC50s of 5 nM, 9 nM, 6 nM, 6 nM, 13 nM, 16 nM and 280 nM, respectively.|In Vivo:|PXS-5129A is readily absorbed following oral gavage, and once in the circulation, rapidly hydrolyzed to release PXS-5120 (free base) in vivo, affording plasma concentrations well above the LOXL2 IC50 (6 nM) for a prolonged period (>6 h) in mice, while remaining well below the IC50 for LOX throughout.|Products are for research use only. Not for human use.|
