Neuraminidase-IN-11 (15e) 是一种有效的选择性神经氨酸酶 (NA) 抑制剂,作用于 H1N1、H5N1 和 H5N8 病毒的 NAIC50值分别是 4.7 nM、8.46 nM、1.5 nM。
产品描述
Neuraminidase-IN-11 (15e) is a potent and selective neuraminidase ( NA ) inhibitor with the IC 50 values of 4.7 nM, 8.46 nM and 1.5 nM against H1N1, H5N1 and H5N8 NAs respectively [1].
体外活性
Neuraminidase-IN-11 (15e) (0-6 μM, 40 min)has anti-NA (Neuraminidase) activity against H1N1-H274Y mutant and H5N1-H274Y mutant with the IC 50 values of 1.07 μM and 0.61 μM, respectively [1]. Neuraminidase-IN-11 (15e) (0-20 μM, 48 h) inhibits chicken embryo fibroblasts (CEFs) infected H5N1 or H5N8 with the IC 50 values of 4.4 μM and 0.57 μM respectively, and inhibits Madin Darby canine kidney (MDCK) cells infected H1N1 or H3N2 with the IC 50 values of 0.05 μM and 12.65 μM respectively [1]. Neuraminidase-IN-11 (15e) has no significant inhibitory effect on the major CYP enzymes which acts on CYP1A2, CYP2C9 and CYP2C19 with the IC 50 values of 28.9 μM, 47.3 μM and 47.8 μM, respectively [1]. The metabolic stability parameters of Neuraminidase-IN-11 (15e) in human liver microsomes (HLM) [1]. Parameters Neuraminidase-IN-11 (15e) t 1/2 (min) >145 CL int(mic) (μL/min/kg)<9.6 CL int(liver) (mL/min/kg)<8.6 remaining (T = 60 min) (%) 79.3
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years