BAY-678 - Elastase 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBAY-678Cat. No.: HY-111457ACAS No.: 675103-36-3分式: CHFNO分量: 400.35作靶点: Elastase作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (249.78 mM)* means sol

2、uble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4978 mL 12.4891 mL 24.9781 mL5 mM 0.4996 mL 2.4978 mL 4.9956 mL10 mM 0.2498 mL 1.2489 mL 2.4978 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 BAY-678具有服物活性的、效的、选择性的、中性粒细胞弹性蛋酶 (HNE) 的细胞渗透性抑制剂，其 IC

3、50 值为 20 nM。BAY-678 也是被基因结构组学联盟 (SGC) 推荐的化学探针。IC50 & Target IC50: 20 nM (HNE) 1.体外研究BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEelastase (HNE), with an IC50 of 20 nM. The Ki value of BAY-

4、678 for MNE is 700 nM. BAY-678 is the 4thgeneration inhibitor of HNE 1. BAY-678 is also nominated as a chemical probe to the public via theStructural Genomics Consortium (SGC) 2. BAY-678 has more than 2,000-fold selectivity in a panel of 21serine proteases 3.体内研究 BAY-678 (17) reveals significant eff

5、icacy in preclinical models of ALI and lung emphysema, demonstratingtheir anti-inflammatory and anti-remodeling mode of action. Additionally, BAY-678 (17) has shown significantbeneficial pulmonary hemodynamic and vascular effects in models of PAH in rats and mice 2.REFERENCES1. von Nussbaum F, et al

6、. Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective andPotent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases. ChemMedChem. 2015 Jul;10(7):1163-73.2. von Nussbaum F, et al. Neutrophil elastase inhibitors for the treatment of (cardio)pulmonary diseases: Into clinical testing with pre-adaptive pharmacophores. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4370-81.3. BAY-678 Selective chemical probe for Human Neutrophil Elastase.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use on