CGS 21680A
CGS 21680A Basic information
- Product Name:
- CGS 21680A
- Synonyms:
-
- CGS 21680 (HCl salt)
- CGS 21680A
- 4-[2-[[6-Amino-9-(N-ethyl-beta-D-ribofuranuronamidosyl)-9H-purin-2-yl]amino]ethyl]benzenepropanoic acid monohydrochloride
- Benzenepropanoic acid, 4-[2-[[6-amino-9-(N-ethyl-b-D-ribofuranuronamidosyl)-9H-purin-2-yl]amino]ethyl]- hydrochloride (1:1)
- [3H]-CGS 21680A
- CGS 21680A;CGS 21680 HCL
- CGS 21680 HCl NEW
- 100688
- CAS:
- 124431-80-7
- MF:
- C23H30ClN7O6
- MW:
- 535.99
- Product Categories:
-
- Carbohydrates & Derivatives
- Chiral Reagents
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Inhibitors
- Mol File:
- 124431-80-7.mol
CGS 21680A Chemical Properties
- Melting point:
- 204-206°C
- storage temp.
- Inert atmosphere,2-8°C
- solubility
- DMSO (Slightly, Heated), Methanol (Slightly, Heated)
- form
- Solid
- color
- White to Light Beige
- Stability:
- Hygroscopic
- CAS DataBase Reference
- 124431-80-7
CGS 21680A Usage And Synthesis
Chemical Properties
White to Off-White Solid
Uses
A selective A2A receptor agonist.
Uses
Adenosine receptors are related to many diseases such as cardiovascular, autoimmune, and cancer. CGS 21680 is a potent and selective agonist of the adenosine A2A receptor, a member of G protein coupled receptor (1,2,3).
Uses
CGS 21680A is a potent, selective agonist of the adenosine A2A receptor (Ki = 11-46 nM). It is less effective at adenosine A1 and A3 receptors (Kis = 0.5-3.1 and 0.6-1 μM, respectively) and is without effect at adenosine A2B (Ki > 10 μM). CGS 21680A is commonly used to study the actions of the adenosine A2A receptor in cells and tissues.[Cayman Chemical]
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].
storage
-20°C (desiccate)
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.
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