CGS 21680A Property

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

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

CGS 21680A Chemical Properties,Usage,Production

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.