256477-09-5

256477-09-5 structure

Name: UK-371804
Chemical Name: UK-371804
CAS Number: 256477-09-5
Molecular Formula: C₁₄H₁₆ClN₅O₄S
Molecular Weight: 385.823
Catalog: Signaling Pathways Metabolic Enzyme/Protease Ser/Thr Protease
Create Date: 2018-01-26 22:25:17
Modify Date: 2024-01-07 15:39:57
UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.

Name	UK-371804
Synonyms	2-[[4-chloro-1-(diaminomethylideneamino)isoquinolin-7-yl]sulfonylamino]-2-methylpropanoic acid

Description	UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Ser/Thr Protease Research Areas >> Inflammation/Immunology
Target	Ki: 10 nM (uPA)[1]
In Vitro	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].
Animal Admin	Pigs: Two female pigs are subjected to eight excisional wounds. The wounds are dressed and treated daily for 10 days with either 1 mL of a 10 mg/mL formulation of UK-371804 in hydrogel vehicle, or hydrogel vehicle alone (control). On day 11 the animals are sacrificed, terminal blood samples are taken to assess any systemic exposure of the compounds, and the wounds are excised from the surrounding normal skin[1].
References	[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.