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Antibody

6.5 - 270 kDa 범위를 커버하는 3가지 컬러 밴드를 포함하며,
최대 100%까지의 transfer 효과를 개런티하는 Prestained protein ladder를 소개합니다.

특징 


  • Liver steatosis (간지방증), Hepatitis (간염), Liver fibrosis (간섬유증)에 대한 in vitro panel을 이용하여 NASH 표적 약물을 테스트 해 드립니다.
  • Pathogenesis (병인성)의 다양성에 맞추어 총 26가지 분석 타겟을 제공합니다.
  • Binding, enzymatic, cell-based functional assay를 제공합니다.
  • 임상관련성이 높은 타겟으로 구성되어 있습니다.

  

 


 


Lipid metabolism and NASH progression. A. The free fatty acids are released via lipolysis from adipocyte and fat tissue, B. lipid uptake from circulation, (C. and D.) de novo lipogenesis from sugars to triacylglycerol. These three pathways are the primary source of hepatic lipid. E. Lipids are cleared by b-oxidation via mitochondria and exported by very low-density lipoprotein (VLDL). Pathogenesis of NAFL is owing to the accumulation of fatty acids (>5%), which results in lipotoxicity in the hepatocytes (steatosis). NASH is a more progressive form of liver steatosis. F. Progressive liver injury caused by lipotoxicity leads to hepatocyte ballooning and activation of inflammatory responses (hepatitis). G. The inflammatory response stimulates activation of hepatic stellate cell (HSC) and generates extensive extracellular matrix (ECM) remodeling, leading to the more severe liver fibrosis. The figure is modified from Esler WP and Bence, KK, 2019.6

 

 

 

NASH 서비스 패널 종류


1. Liver Steatosis Panel (#PP270)

  • 간지방증 (liver steatosis) 유발과 관련된 6가지 타겟군에 속하는 13가지 target에 대한 스크리닝을 진행합니다.

Family Target MOA Organism Assay Sub Type Item
Carboxylase ACC1 Inhibitor Human Enzymatic 101800
GPCR GLP1R Activator Human Binding 231710
TGR5 Activator Human Cell Based 304100-0
Kinase AMPK Activator Human Enzymatic 199100-0
FGFR1 Activator Human Cell Based 339210-0
FGFR4 Activator Human Cell Based 339240-0
Lipase Lipase Inhibitor Human Enzymatic 133000
NHR FXR Activator Human Protein-Protein Interaction 311600-0
PPARalpha Activator Human Protein-Protein Interaction 338210-0
PPARdelta Activator Human Cell Based 338260-0
PPARgamma Activator Human Binding 267500
THRB Activator Human Binding 285940
Transporter IBAT Inhibitor Human Cell Based 314100-1

 

 

 

Demonstrated data for the Liver Steatosis Panel
Demonstrated data for the Liver Steatosis Panel. A. Two reported ACC1 inhibitors were validated by an enzymatic ACC1 inhibition assay. Firsocostat is a potent ACC1 inhibitor in Phase I trials for NASH. B. and D. Thyroid hormone mimetics and incretin analogues were examined by radioligand-based THRβ and GLP1R binding assays, respectively. C. Known AMPK activator, A769662, and endogenous agonist, AMP, were characterized via a biochemical AMPK activation assay. E. Two potential candidates of IBAT transporter inhibition were validated by a cell-based IBAT uptake assay. Odevixibat is a candidate against NASH in Phase II trials while Linerixibat is Phase II trials for T2DM.

  

 

  

2. Hepatitis Panel (#PP271)   

  • Hepatitis 발생과 관련된 6가지 타겟군에 속하는 11가지 target에 대한 스크리닝을 진행합니다.   

 

Family Target MOA Organism Assay Sub Type Item
Caspase Caspase 3 Inhibitor Human Enzymatic 163200
Caspase 7 Inhibitor Human Enzymatic 163400
Caspase 8 Inhibitor Human Enzymatic 163500
GPCR CCR2 Inhibitor Human Binding 217550
CCR5 Inhibitor Rhesus Macaque Binding 217730
CysLT1 Inhibitor Human Binding 250460
Kinase ASK1 Inhibitor Human Enzymatic 167150
Oxidoreductase VAP-1 Inhibitor Human Enzymatic 197000
PDE PDE4A Inhibitor Human Enzymatic 154100
PDE4B Inhibitor Human Enzymatic 154200
Transcription Factor NRF2 Inhibitor Human Cell Based 362000-0

 

  

Demonstrated data for the Hepatitis Panel. A. and B. Binding affinity of known CCR2 and CCR5 agonists were validated by radioligand-based binding assays. C. Reported VAP-1 inhibitors were examined by an enzymatic VAP-1 inhibition assay. PXS4728A is a Phase II candidate for NASH. 

  

 

 

3. Liver Fibrosis Panel (#PP272)   

  • Liver fibrosis와 관련된 2가지 target에 대한 스크리닝을 진행합니다.  

 

Family Target MOA Organism Assay Sub Type Item
Cell Based Phenotypic Liver Fibrosis Model Inhibitor Human Cell Based 331740-1
Oxidase LOXL2 Inhibitor Human Enzymatic 138700

 

 

Demonstrated data for the Liver Fibrosis Panel
 

Demonstrated data for the Liver Fibrosis Panel. A. ECM remodeling enzyme, LOXL2, was measured by the IC50 of two inhibitors by an enzymatic LOXL2 inhibition assay. PAT-1251 is in Phase I trials for lung fibrosis. B. Human HSC LX-2 cells were activated by 0.3 nM TGFβ for 48-hr. Fibrogenesis was monitored by evaluating the fibrogenetic marker collagen, type 1, α1 (COL1A1) expression level and analyzed by high-content imaging (Blue: Nuclei; Red: COL1A1). TGFβ successfully induced liver fibrosis with a high level of COL1A1 expression (Image, middle). Induced COL1A1 expression was dose-dependently inhibited by two TGFβ inhibitors, SB525334 and SB-431542, respectively.

 

 

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0.5 ml Elite Pre-stained Protein Ladder (2 x 0.25 ml) PAL-EPL-500 0.5ml 500
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