UK-371804

• CAT Number: I012069
• CAS Number: 256477-09-5
• Molecular Formula: C14H16ClN5O4S
• Molecular Weight: 385.83
• Purity: ≥95%
• Synonyms: 2-[[4-chloro-1-(diaminomethylideneamino)isoquinolin-7-yl]sulfonylamino]-2-methylpropanoic acid
• InChI: InChI=1S/C14H16ClN5O4S/c1-14(2,12(21)22)20-25(23,24)7-3-4-8-9(5-7)11(19-13(16)17)18-6-10(8)15/h3-6,20H,1-2H3,(H,21,22)(H4,16,17,18,19)
• InChIKey: XSDAXWRCPTYNOD-UHFFFAOYSA-N
• SMILES: CC(C)(C(=O)O)NS(=O)(=O)C1=CC2=C(C=C1)C(=CN=C2N=C(N)N)Cl

UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.
UK-371804 is able to inhibit exogenous uPA in human chronic wound fluid (IC50=0.89 μM). UK-371804 has its excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin)[1].
In a porcine acute excisional wound model, following topical delivery, UK-371804 is able to penetrate into pig wounds and inhibit exogenous uPA activity with no adverse effect on wound healing parameters. Concentrations of UK-371804 in the dermis are 41.8 μM[1].

Reference

[1]. Fish PV, et al. Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines. J Med Chem. 2007 May 17;50(10):2341-51.
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