Identification | Back Directory | [Name]
CGS 21680A | [CAS]
124431-80-7 | [Synonyms]
100688 CS-2433 CGS 21680A [3H]-CGS 21680A CGS 21680 HCl NEW CGS 21680 (HCl salt) CGS 21680A USP/EP/BP CGS 21680A;CGS 21680 HCL CGS21680;CGS-21680;CGS 21680 CGS-21680 hydrochloride CGS21680 CGS-21680,Inhibitor,CGS 21680,inhibit,CGS21680,CGS 21680 Hydrochloride,Adenosine Receptor,P1 receptor 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) | [Molecular Formula]
C23H30ClN7O6 | [MOL File]
124431-80-7.mol | [Molecular Weight]
535.981 |
Chemical Properties | Back Directory | [Melting point ]
204-206°C | [storage temp. ]
Refrigerator | [solubility ]
DMSO (Slightly, Heated), Methanol (Slightly, Heated) | [form ]
Solid | [color ]
White to Light Beige | [Stability:]
Hygroscopic | [CAS DataBase Reference]
124431-80-7 |
Hazard Information | Back Directory | [Chemical Properties]
White to Off-White Solid | [Uses]
A selective A2A receptor agonist. | [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]
Store at -20°C | [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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