124431-80-7 Usage
Description
CGS 21680A is a potent and selective agonist of the adenosine A2A receptor, characterized by its high affinity (Ki = 11-46 nM) and minimal effects on other adenosine receptors (A1, A3, and A2B). It is a white to off-white solid and is widely utilized in the study of adenosine A2A receptor actions in various cells and tissues.
Uses
Used in Pharmaceutical Research:
CGS 21680A is used as a research tool for studying the adenosine A2A receptor's role in various diseases, including cardiovascular, autoimmune, and cancer-related conditions. Its high selectivity and potency make it an ideal candidate for investigating the receptor's function and potential therapeutic applications.
Used in Drug Development:
In the pharmaceutical industry, CGS 21680A is used as a lead compound for the development of new drugs targeting the adenosine A2A receptor. Its selectivity and potency can help in designing more effective and safer medications for treating adenosine receptor-related diseases.
Used in Diagnostic Applications:
CGS 21680A can be employed in the development of diagnostic tools and tests that specifically target the adenosine A2A receptor. This can aid in the early detection and monitoring of diseases associated with this receptor, leading to better patient outcomes and more personalized treatment strategies.
Used in Cell and Tissue Studies:
In the field of cell biology and tissue engineering, CGS 21680A is used as a selective agonist to study the adenosine A2A receptor's actions in different cell types and tissues. This can provide valuable insights into the receptor's role in cellular processes and contribute to a better understanding of its potential therapeutic applications.
Biological Activity
cgs 21680 hcl is a selective agonist of a2 adenosine receptor with ic50 value of 22nm [1].in rat striatal membranes, cgs 21680 potently prevents ligands from binding to a2 adenosine receptors with ic50 value of 22nm. in the binding assay, cgs 21680 shows no effect to other putative neurotransmitter/neuromodulator sites in brain membranes such as adrenergic, dopamine and serotonin. in the rat heart model, cgs 21680 is effective in increasing coronary flow with ec25 value of 2nm [1].
in vivo
the hydrochloride salt of cgs 21680 has potent efficacy to decrease blood pressure in the anesthetized normotensive rat with ed50 value of 9μg/kg. it also causes heart rate increasing up to 15%. besides that, cgs 21680 hcl significantly lower the blood pressure at dose of 10mg/kg in the spontaneously hypertensive rat. a transient elecation of heart rate is also observed at 30 min in the model [1].
references
[1] hutchison a j, webb r l, oei h h, et al. cgs 21680c, an a2 selective adenosine receptor agonist with preferential hypotensive activity. journal of pharmacology and experimental therapeutics, 1989, 251(1): 47-55.
Check Digit Verification of cas no
The CAS Registry Mumber 124431-80-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,2,4,4,3 and 1 respectively; the second part has 2 digits, 8 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 124431-80:
(8*1)+(7*2)+(6*4)+(5*4)+(4*3)+(3*1)+(2*8)+(1*0)=97
97 % 10 = 7
So 124431-80-7 is a valid CAS Registry Number.
124431-80-7Relevant articles and documents
An Fc domain protein-small molecule conjugate as an enhanced immunomodulator
Chiang, Meng-Jung,Holbert, Marc A.,Kalin, Jay H.,Ahn, Young-Hoon,Giddens, John,Amin, Mohammed N.,Taylor, Martin S.,Collins, Samuel L.,Chan-Li, Yee,Waickman, Adam,Hsiao, Po-Yuan,Bolduc, David,Leahy, Daniel J.,Horton, Maureen R.,Wang, Lai-Xi,Powell, Jonathan D.,Cole, Philip A.
supporting information, p. 3370 - 3373 (2014/03/21)
Proteins as well as small molecules have demonstrated success as therapeutic agents, but their pharmacologic properties sometimes fall short against particular drug targets. Although the adenosine 2a receptor (A 2AR) has been identified as a pr
