ZK824859

Cas No.:	2254001-81-3
Chemical Name:	(2R)-2-[(6-{[3'-(Aminomethyl)-3-biphenylyl]oxy}-3,5-difluoro-2-pyridinyl)oxy]butanoic acid
Synonyms:	ZK824859;BCP30356;BDBM50467212;(2R)-2-[6-[3-[3-(aminomethyl)phenyl]-5-methylphenoxy]-3,5-difluoropyridin-2-yl]oxybutanoic acid;(2R)-2-[(6-{[3'-(Aminomethyl)-3-biphenylyl]oxy}-3,5-difluoro-2-pyridinyl)oxy]butanoic acid
SMILES:	FC1C([H])=C(C(=NC=1O[C@@]([H])(C(=O)O[H])C([H])([H])C([H])([H])[H])OC1=C([H])C(C([H])([H])[H])=C([H])C(=C1[H])C1=C([H])C([H])=C([H])C(C([H])([H])N([H])[H])=C1[H])F
Formula:	C23H22F2N2O4
M.Wt:	428.428593158722
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	ZK824859 (ZK-824859) is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively[1].
Target:	IC50: 237 nM (uPA), 1600 nM (tPA), 1850 nM (Plasmin)[1]
In Vivo:	ZK824859 (2 mg/kg; PO) exhibits a relatively high oral availability and a moderate half time (T1/2=2.8 h)[1]. Animal Model: Rats with experimental autoimmune encephalomyelitis (EAE) model[1] Dosage: 2 mg/kg (Pharmacokinetic Analysis) Administration: PO Result: Oral availability F = 55%; Cmax= 0.64 g/mL and AUC = 2.2 h*g/mL; T1/2=2.8 h.
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.