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UK-371804 HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
UK-371804 HCl图片
CAS NO:256476-36-5
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)422.29
FormulaC14H16ClN5O4S.HCl
CAS No.256476-36-5;
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 42 mg/mL (99.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILES Code CC(C)(NS(=O)(C1=CC2=C(C=C1)C(Cl)=CN=C2/N=C(N)\N)=O)C(O)=O.[H]Cl
Synonyms UK371804; UK-371804; UK 371804; UK-371,804; UK 371,804; UK371,804.
实验参考方法
In Vitro

In vitro activity: UK-371804 is a potent and selective inhibitor of urokinase-type plasmogen activator (uPA) with excellent potency (Ki=10 nM in an enzyme assay) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin). UK-371804 is able to inhibit exogenous uPA in human chronic wound fluid (IC50=0.89 microM) in vitro. In a porcine acute excisional wound model in vivo, upon topical administration, UK-371804 is able to penetrate into pig wounds and inhibit exogenous uPA activity with no adverse side effects on wound healing parameters.


Kinase Assay: 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.


Cell Assay:

In VivoIn 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
Animal model Pig
Formulation & DosageTwo 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.
References J Med Chem. 2007 May 17;50(10):2341-51.