In vitro: UK-3718046 is able to inhibit exogenous uPA in human chronic wound fluid (IC50=0.89 µM). In vivo: In Vivo, in a porcine acute excisional wound model, following topical delivery, UK-3718046 is able to penetrate into pig wounds and inhibit exogenous uPA activity with no adverse effect on wound healing parameters.
|Animal models||A porcine acute excisional wound model|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||42 mg/mL in DMSO|
Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines.
Fish PV, et al. J Med Chem. 2007 May 17;50(10):2341-51. PMID: 17447747.
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