UK-371804-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEUK-371804Cat. No.: HY-101214CAS No.: 256477-09-5分式: CHClNOS分量: 385.83作靶點(diǎn): Ser/Thr Protease作通路: Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 10 mg/mL (25.92 mM; N

2、eed ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.5918 mL 12.9591 mL 25.9182 mL5 mM 0.5184 mL 2.5918 mL 5.1836 mL10 mM 0.2592 mL 1.2959 mL 2.5918 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 UK-371804是尿嘧啶型纖溶酶原激活物 (uPA) 的抑制劑，Ki值為10 nM。IC50 & Targe

3、t Ki: 10 nM (uPA) 1體外研究 UK-371804 is able to inhibit exogenous uPA in human chronic wound fluid (IC50=0.89 M). UK-371804 hasits excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versusplasmin) 1.1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體內(nèi)研究 In a

4、porcine acute excisional wound model, following topical delivery, UK-371804 is able to penetrate into pigwounds and inhibit exogenous uPA activity with no adverse effect on wound healing parameters.Concentrations of UK-371804 in the dermis are 41.8 M 1.PROTOCOLAnimal Pigs: Two female pigs are subjec

5、ted to eight excisional wounds. The wounds are dressed and treated dailyAdministration 1 for 10 days with either 1 mL of a 10 mg/mL formulation of UK-371804 in hydrogel vehicle, or hydrogel vehiclealone (control). On day 11 the animals are sacrificed, terminal blood samples are taken to assess anysy

6、stemic exposure of the compounds, and the wounds are excised from the surrounding normal skin 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. 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.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: