| Bioactivity | UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM. | ||||||||||||
| Target | Ki: 10 nM (uPA) | ||||||||||||
| Invitro | 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 Vivo | 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]. | ||||||||||||
| Name | UK-371804 | ||||||||||||
| CAS | 256477-09-5 | ||||||||||||
| Formula | C14H16ClN5O4S | ||||||||||||
| Molar Mass | 385.83 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |