CGS 21680 HCl

A2 adenosine receptor agonist CAS# 124431-80-7

CGS 21680 HCl

Catalog No. BCC4316----Order now to get a substantial discount!

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Chemical structure

CGS 21680 HCl

3D structure

Chemical Properties of CGS 21680 HCl

Cas No. 124431-80-7 SDF Download SDF
PubChem ID 10256643 Appearance Powder
Formula C23H30ClN7O6 M.Wt 535.98
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 20 mg/mL (37.31 mM)
H2O : < 0.1 mg/mL (insoluble)
*"≥" means soluble, but saturation unknown.
Chemical Name 3-[4-[2-[[6-amino-9-[(2R,3R,4S,5S)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]purin-2-yl]amino]ethyl]phenyl]propanoic acid;hydrochloride
SMILES CCNC(=O)C1C(C(C(O1)N2C=NC3=C2N=C(N=C3N)NCCC4=CC=C(C=C4)CCC(=O)O)O)O.Cl
Standard InChIKey QPHVMNOEKKJYJO-MJWSIIAUSA-N
Standard InChI InChI=1S/C23H29N7O6.ClH/c1-2-25-21(35)18-16(33)17(34)22(36-18)30-11-27-15-19(24)28-23(29-20(15)30)26-10-9-13-5-3-12(4-6-13)7-8-14(31)32;/h3-6,11,16-18,22,33-34H,2,7-10H2,1H3,(H,25,35)(H,31,32)(H3,24,26,28,29);1H/t16-,17+,18-,22+;/m0./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of CGS 21680 HCl

DescriptionA2A adenosine receptor agonist (Ki = 27 nM). Has affinity for A1 and A3 adenosine receptors but can be used to distinguish A2A- and A2B-mediated effects.

CGS 21680 HCl Dilution Calculator

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CGS 21680 HCl Molarity Calculator

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Preparing Stock Solutions of CGS 21680 HCl

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.8657 mL 9.3287 mL 18.6574 mL 37.3148 mL 46.6435 mL
5 mM 0.3731 mL 1.8657 mL 3.7315 mL 7.463 mL 9.3287 mL
10 mM 0.1866 mL 0.9329 mL 1.8657 mL 3.7315 mL 4.6644 mL
50 mM 0.0373 mL 0.1866 mL 0.3731 mL 0.7463 mL 0.9329 mL
100 mM 0.0187 mL 0.0933 mL 0.1866 mL 0.3731 mL 0.4664 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on CGS 21680 HCl

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.

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References on CGS 21680 HCl

Adenosine receptors and their ligands.[Pubmed:11111832]

Naunyn Schmiedebergs Arch Pharmacol. 2000 Nov;362(4-5):382-91.

The regulatory actions of adenosine are mediated via four subtypes of G protein-coupled receptors distinguished as A1, A2A, A2B and A3 receptors. Their presence on basically every cell makes them an interesting target for the pharmacological intervention in many pathophysiological situations. A large number of ligands have been synthesized over the last two decades and provide agonists and antagonists that are more or less selective for the known receptor subtypes. In addition, many radioligands are available in tritiated or radioiodinated form. The comparative pharmacological characterization of all four human adenosine receptor subtypes revealed that some of the compounds thought to be selective from data in other species have unexpected potencies at human receptors. As a result, compounds that exhibit high affinity to only one subtype are an exception. Although the selection of ligands is immense, it is less than satisfying for most subtypes of adenosine receptors.

Effects of CGS 21680, a selective A2A adenosine receptor agonist, on cardiac output and vascular resistance in acute heart failure in the anaesthetized rat.[Pubmed:9605574]

Br J Pharmacol. 1998 Apr;123(8):1666-72.

1. The effects of CGS 21680, a selective A2A adenosine receptor agonist, on cardiac output, blood pressure, mean circulatory filling pressure (Pmcf), arterial and venous resistances, heart rate and left ventricular end-diastolic pressure were assessed in rats with acute heart failure by means of coronary artery occlusion. 2. Animals (n=6 in each group) were divided into five groups: group I, sham-operated vehicle-treated (0.9% saline; 0.018 mL min(-1)); groups II-V, subject to coronary artery occlusion and treated with vehicle (0.9% saline; 0.018 ml min(-1)) and CGS 21680 (0.1, 0.3 and 1.0 microg kg(-1) min(-1)), respectively. Haemodynamic measurements were taken one hour after completion of surgery, ninety minutes after coronary artery occlusion (except in group I), and fifteen minutes after infusion of saline or CGS 21680. 3. Baseline haemodynamic measurements before occlusion were found not to differ significantly between the different groups of animals. However, after occlusion, cardiac output, rate of rise in left ventricular pressure (+ dP/dt) and blood pressure were significantly reduced when compared to corresponding values in sham-operated animals. In addition, occlusion of the coronary artery resulted in a significant elevation in venous resistance, Pmcf and left ventricular end-diastolic pressure as compared to corresponding values in sham-operated animals. 4. Infusion with CGS 21680 at the highest dose significantly reduced blood pressure, arterial resistance and left ventricular end-diastolic pressure when compared to occluded vehicle-treated animals (group II). Administration of CGS 21680 at the highest dose also significantly increased cardiac output (28%) and heart rate (10%) in comparison to occluded vehicle-treated animals. In addition, the highest dose of CGS 21680 significantly reduced Pmcf (9%) and venous resistance (62%) in comparison to occluded vehicle-treated animals. Administration of CGS 21680 did not significantly affect +dP/dt when compared to occluded vehicle-treated animals. 5. The results from the present investigation indicate that occlusion of the coronary artery in rats results in a state of heart failure characterized by reduced arterial pressure and cardiac output, and increased venous resistance, Pmcf and left ventricular end-diastolic pressure. Administration of CGS 21680 to animals with acute heart failure resulted in increased cardiac output which was due to reduced venous resistance, as well as increased heart rate.

The selective adenosine A2 receptor agonist, CGS 21680, is a potent depressant of cerebral cortical neuronal activity.[Pubmed:2322828]

Brain Res. 1990 Feb 19;509(2):328-30.

The A2 selective adenosine receptor agonist 2-p-(2-carboxyethyl)phenethylamino-5'-N-ethylcarboxamidoadenosine (CGS 21680) depressed the spontaneous, acetylcholine- and glutamate-evoked firing of rat cerebral sensorimotor cortical neurons. Iontophoretically applied CGS 21680 was equipotent with adenosine as a depressant and its actions were antagonized by 8-p-sulphophenyltheophylline applied from another barrel of the multibarrelled micropipette. The observation of a potent depressant action of a selective A2 receptor agonist suggests that A2 receptors are involved in the modulation of cerebral cortical neuronal firing by adenosine.

Description

CGS 21680 Hydrochloride is a selective adenosine A2A receptor agonist with a Ki of 27 nM.

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