Description
ZK824859 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.
Product information
CAS Number: 2271122-53-1
Molecular Weight: 428.43
Formula: C23H22F2N2O4
Chemical Name: (2R)-2-[(6-{[3'-(aminomethyl)-5-methyl-[1,1'-biphenyl]-3-yl]oxy}-3,5-difluoropyridin-2-yl)oxy]butanoic acid
Smiles: CC1C=C(C=C(C=1)OC1N=C(O[C@H](CC)C(O)=O)C(F)=CC=1F)C1C=C(CN)C=CC=1
InChiKey: CVNXUNVHFJANHX-HXUWFJFHSA-N
InChi: InChI=1S/C23H22F2N2O4/c1-3-20(23(28)29)31-22-19(25)11-18(24)21(27-22)30-17-8-13(2)7-16(10-17)15-6-4-5-14(9-15)12-26/h4-11,20H,3,12,26H2,1-2H3,(H,28,29)/t20-/m1/s1
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:
ZK824859 is 5 fold less potent and has lost selectivity in mouse: uPA IC50=410 nM; tPA IC50=910 nM; plasmin IC50=1600 nM compared to human IC50 values of 79 nM, 1580 nM and 1330 nM respectively.
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.
Products are for research use only. Not for human use.
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