| Identification | Back Directory | [Name]
Butanoic acid, 2-[[6-[[3'-(aminomethyl)-5-methyl[1,1'-biphenyl]-3-yl]oxy]-3,5-difluoro-2-pyridinyl]oxy]-, hydrochloride (1:1), (2R)- | [CAS]
2436760-76-6 | [Synonyms]
ZK824859 hcl
Butanoic acid, 2-[[6-[[3'-(aminomethyl)-5-methyl[1,1'-biphenyl]-3-yl]oxy]-3,5-difluoro-2-pyridinyl]oxy]-, hydrochloride (1:1), (2R)- | [Molecular Formula]
C23H23ClF2N2O4 | [MOL File]
2436760-76-6.mol | [Molecular Weight]
464.89 |
| Hazard Information | Back Directory | [Uses]
ZK824859 hydrochloride is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79?nM, 1580?nM and 1330?nM for human uPA, tPA, and plasmin, respectively[1]. | [in vivo]
ZK824859 (50, 25 and 10?mg/kg; b.i.d.; 25 days) is used in a chronic mouse EAE model. ZK 824859 completely prevents the development of disease. However, two lower doses (25 and 10?mg/kg) have no effect on clinical scores[1]. | Animal Model: | Female SJL mice with chronic mouse EAE model[1] | | Dosage: | 50, 25 and 10?mg/kg | | Administration: | B.i.d.; 25 days | | Result: | Prevented the development of disease at 50?mg/kg completely. However, 25 and 10?mg/kg had no effect on clinical scores. |
| [References]
[1] Islam I, et al. Discovery of selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis. Bioorg Med Chem Lett. 2018 Nov 1;28(20):3372-3375. DOI:10.1016/j.bmcl.2018.09.001 |
|
|