默沙东也不例外,采用不同的Assay,包括LDL uptake,LDLR降解等实验,经过数次筛选几百万化合物的化合物库都无果。最后用一个Biacore的Binding assay终于找到了一个很弱的PCSK9的结合分子,该小分子的结合部位不在PCSK9与LDLR 的接触区,因此没有显示出抑制LDLR降解的生物...
Notably, the LDLr has been proposed to promote the presecretory degradation and the reuptake of apoB, in addition to its well-defined role in plasma LDL uptake (25). Furthermore, increased apoB production is observed in FH patients carrying mutations on the LDLr, resulting in a virtual ...
Loaded Human LDL R, Fc Tag (Cat. No.LDR-H5254) on Protein A Biosensor, can bind Cynomolgus PCSK9, His Tag (Cat. No.PC9-C5223) with an affinity constant of 1.46 nM as determined in BLI assay (ForteBio Octet Red96e) (Routinely tested). PCSK9高生物活性:经FACS验证 FACS analysis shows...
Introduction Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a key negative regulator of lipid uptake through low-density lipoprotein (LDL) receptor (LDLR), and has recently been implicated in regulating cytokine production during sepsis. We hypothesize that PCSK9 affects cytokine production ...
LDLuptakeassaykit购于Biovision,Cat.No.K585-100 Pcsk9抗体购于R&D公司,Cat.No.AF3888 4.1将HepG2细胞按照40,000个细胞/孔的密度种于96孔透明细胞培养板中,37度CO 2 细胞培养箱中培养过夜。 4.2第二天,弃去HepG2培养基更换为含有10%脱脂血清的培养基,继续培养18小时。 4.3第三天, (1)配置终浓度为100μ...
It has an effect in a cell-based LDL uptake assay by enhancing Dil-LDL cellular endocytosis in HepG2 cell line. In addition, BCD-096 has demonstrated good aggregation stability and may be formulated at concentration above 100 mg/ml making it suitable for subcutaneous administration. Evaluation ...
LDL-C : Low-density lipoprotein Cholesterol CVDs : Cardiovascular diseases non-HDL-C : Non-High-Density Lipoprotein Cholesterol ApoB : Apolipoprotein B LDLR : Low-density lipoprotein receptor NARC-1 : Neural apoptosis-regulated convertase-1 GOF : Gain of function FH : Familial hyperchole...
LDL-uptake assay. The LDL-uptake test in HepG2 cell models. The horizontal axis represents six different groups. The vertical axis represents mean fluorescence intensity (MFI) of the intracellular LDL-BODIPY, which reflects the levels of the LDL-c metabolism. The right two groups were respective...
对于降低胆固醇这样的有临床证明的有效治疗方式,口服药的优势是巨大的。从PCSK9 靶标的提出,许多大公司就开始在各自的化合物库筛选小分子药苗。默沙东也不例外,采用不同的Assay,包括LDL uptake,LDLR降解等实验,经过数次筛选几百万化合物的化合物库都无果。
Presently, PCSK9 inhibitors have been proven to significantly reduce LDL-C levels by 61% and reduce the incidence of cardiovascular events (CVEs) in the background of statin treatment during~1 year of therapy27,28. However, the relationship between circulating PCSK9 and pathophysiological mechanism...