251992-66-2 Usage
Uses
Used in Pharmaceutical Industry:
A-205804 is used as a reagent for the preparation of selective inhibitors of cell adhesion molecule expression in human endothelial cells. This application is significant because it helps in the development of targeted therapies for various diseases, including those involving the immune system and inflammation.
Used in Research and Development:
A-205804 is used as a research tool to study the role of E-selectin and ICAM-1 in cellular processes and their involvement in disease progression. By inhibiting these molecules, researchers can gain insights into the underlying mechanisms of various pathologies and develop novel therapeutic strategies.
Used in Drug Discovery:
A-205804 serves as a starting point for the development of new drugs that target E-selectin and ICAM-1. By understanding the structure-activity relationship of A 205804, chemists can design and synthesize more potent and selective inhibitors with improved pharmacological properties.
Used in Diagnostic Applications:
A-205804 can be employed in the development of diagnostic tools to detect the expression levels of E-selectin and ICAM-1 in human vascular endothelial cells. This can help in the early detection of diseases and the monitoring of treatment responses in patients.
Biological Activity
Selective inhibitor of E-selectin and ICAM-1 expression (IC 50 values are 20, 25 and > 1000 nM for TNF- α -induced E-selectin, ICAM-1 and VCAM-1 expression respectively). Effective inhibitor of cell-cell adhesion in an in vitro flow experiment.
references
[1]. stewart, a.o., et al., discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. selective inhibition of icam-1 and e-selectin expression. j med chem, 2001. 44(6): p. 988-1002.[2]. chang, c.z., et al., valproic acid attenuates intercellular adhesion molecule-1 and e-selectin through a chemokine ligand 5 dependent mechanism and subarachnoid hemorrhage induced vasospasm in a rat model. j inflamm (lond), 2015. 12: p. 27.[3]. zhu, g.d., et al., selective inhibition of icam-1 and e-selectin expression in human endothelial cells. 2. aryl modifications of 4-(aryloxy)thieno[2,3-c]pyridines with fine-tuning at c-2 carbamides. j med chem, 2001. 44(21): p. 3469-87. [4]. zhu, g.d., et al., synthesis and mode of action of (125)i- and (3)h-labeled thieno[2,3-c]pyridine antagonists of cell adhesion molecule expression. j org chem, 2002. 67(3): p. 943-8.
Check Digit Verification of cas no
The CAS Registry Mumber 251992-66-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,5,1,9,9 and 2 respectively; the second part has 2 digits, 6 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 251992-66:
(8*2)+(7*5)+(6*1)+(5*9)+(4*9)+(3*2)+(2*6)+(1*6)=162
162 % 10 = 2
So 251992-66-2 is a valid CAS Registry Number.
InChI:InChI=1/C15H12N2OS2/c1-9-2-4-10(5-3-9)19-13-7-17-8-14-11(13)6-12(20-14)15(16)18/h2-8H,1H3,(H2,16,18)
251992-66-2Relevant academic research and scientific papers
Cell adhesion-inhibiting antiinflammatory compounds
-
, (2008/06/13)
Compounds having Formula I are useful for treating inflammation. Also disclosed are pharmaceutical compositions comprising compounds of Formula I, and methods of inhibiting/treating inflammatory diseases in a mammal.
Discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. Selective inhibition of ICAM-1 and E-selectin expression
Stewart,Bhatia,McCarty,Patel,Staeger,Arendsen,Gunawardana,Melcher,Zhu,Boyd,Fry,Cool,Kiflie,Lartey,Marsh,Kempf-Grote,Kilgannon,Wisdom,Meyer,Gallatin,Okasinskit
, p. 988 - 1002 (2007/10/03)
A critical early event in the inflammatory cascade is the induced expression of cell adhesion molecules on the lumenal surface of vascular endothelial cells. These adhesion molecules include E-selectin, ICAM-1, and VCAM-1, which serve to recruit circulati
