CGS 21680 120225-54-9 GlpBio

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Product Data Sheet

Product Name:Cat. No.:

CGS 21680GC10172

Chemical Properties

Cas No.ChemicalNameCanonicalSMILESFormulaSolubilityGeneraltipsShippingCondition

120225-54-9

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

CCNC(=O)C1C(C(C(O1)N2C=NC3=C2N=C(N=C3N)NCCC4=CC=C(C=C4)CCC(=O)O)O)OC23H29N7O6

≥19.25mg/mL in DMSO

M.WtStorage

499.52Store at -20°C

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in theultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.Evaluation sample solution : ship with blue ice All other available size: ship with RT , orblue ice upon request.

Structure

Caution: Producthasnot been fully validated for medical applications. For research use only.

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Address: 10292 Central Ave. #205, Montclair, CA, USA

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Product Data Sheet

实验参考方法

Vitro experiment [1,2]:SamplesHippocampal and striatal slices

The solubility of this compound in DMSO is > 19.3 mg/mL. General tips for

obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes

Preparation method

and/or shake it in the ultrasonic bath for a while. Stock solution can be storedbelow -20℃ for several months.

Reacting conditionEC50: 110 nM

In hippocampal slices, CGS 21680 appeared to be a weak agonist on pre- andpostsynaptic measures of electrophysiological activity (putative A1 receptormediated events) and was ine?ective at stimulating the formation of cAMP (aputative A2b mediated response). In striatal slices, CGS 21680 potently

stimulated the formation of cAMP with an EC50 of 110 nM but was ine?ective at

Applicationsinhibiting electrically stimulated dopamine release. CGS21680 (10 nM) showed

only small survival activity, but the activity was signi?cantly enhanced by theaddition of a phosphodiesterase inhibitor, IBMX. The survival activity ofCGS21680 on cultured motoneurons was exerted by mixed e?ects of the

adenylate cyclase-cAMP-PKA pathway and the transactivation of neurotrophinreceptors.

Animal experiment [3,4]:Animal modelsFemale Lewis ratsDosage formIntraperitoneal injection, 1 mg/kg, every two days

In female Lewis rats, CGS21680 (1 mg/kg/i.p.) intervention promoted thedevelopment of EAN. CGS21680 intervention promoted in?ammatory cell

in?ltration and demyelination of sciatic nerves. CGS21680 intervention elevatedthe levels of P0 peptide-speci?c antibodies in serum. CGS21680 interventionsuppressed Th1 and Th17 cytokines, and powerfully inhibited lymphocyte

proliferation and IL-2 secretion. CGS21680 intervention reduced the proportionsCD4+Foxp3+ Treg cells while increased CD4+CXCR5+ Tfh cells, B cells and

Applicationdendritic cells in draining lymph nodes. CGS21680 intervention increased the

expressions of MHC class II and CD86. CGS21680 (0.1 mg/kg, i.p.) transientlyincreased heart frequency. Following transient MCAo, CGS21680 at both dosesprotected from neurological de?cit from the ?rst day up to 7 days thereafter.

CGS21680 reduced microgliosis, astrogliosis and improved myelin organization inthe striatum and cytoarchitecture of the ischemic cortex and striatum. Two daysafter transient MCAo, CGS21680 reduced the number of in?ltrated granulocytesinto the ischemic tissue.

Please test the solubility of all compounds indoor, and the actual solubility may

Other notesslightly di?er with the theoretical value. This is caused by an experimental

system error and it is normal.

Caution: Producthasnot been fully validated for medical applications. For research use only.

Tel: (626) 353-8530 Fax: (626) 353-8530 E-mail: tech@glpbio.com

Address: 10292 Central Ave. #205, Montclair, CA, USA

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Product Data Sheet

References:

[1]. Lupica C R, Cass W A, Zahniser N R, et al. E?ects of the selective adenosine A2 receptor agonistCGS 21680 on in vitro electrophysiology, cAMP formation and dopamine release in rat hippocampusand striatum[J]. Journal of Pharmacology and Experimental Therapeutics, 1990, 252(3): 1134-1141.[2]. Komaki S, Ishikawa K, Arakawa Y. Trk and cAMP-dependent survival activity of adenosine A 2Aagonist CGS21680 on rat motoneurons in culture[J]. Neuroscience letters, 2012, 522(1): 21-24.

[3]. Zhang M, Li X L, Li H, et al. Activation of the adenosine A 2A receptor exacerbates experimentalautoimmune neuritis in Lewis rats in association with enhanced humoral immunity[J]. Journal ofneuroimmunology, 2016, 293: 129-136.

[4]. Melani A, Corti F, Cellai L, et al. Low doses of the selective adenosine A 2A receptor agonist

CGS21680 are protective in a rat model of transient cerebral ischemia[J]. Brain research, 2014, 1551:59-72.

Background

CGS 21680 is a selective agonists of A2 adenosine receptor with IC50 value of 22nM [1].

CGS 21680 is found to be potent and selective adenosine A2 receptor agonists. In a radioligandbinding in vitro assay, CGS 21680 binds A2 receptor with IC50 value of 22nM and the A1/A2 ratio is141, In the perfused rat heart model, CGS 21680 can increase coronary ?ow with greater EC25 valuethan 1000nM. It shows a good separation between its ability to induce vasorelaxation and

bradycardia. CGS 21680 also has potent e?ect on blood pressure in vivo with EC25 value of 9μg/kgand it can induce an increase in heart rate [1].

It is reported that CGS 21680 also has the potency of anti-in?ammatory. It can reduce the

development of acute lung in?ammation in a mouse model of carrageenan-induced pleurisy. In bothprior and post-treatment, CGS 21680 can reduce the number of in?ammatory cells and the degree oflung injury [2].

References:

[1] Alan J. Hutchison, Randy L. Webb, Howard H. Oei, Geetha R. Ghai, Mark B. Zimmerman andMichael Williams. CGS 21680C, an A2 Selective Adenosine Receptor Agonist with PreferentialHypotensive Activity. The Journal of Pharmacology and Experimental Therapeutics. 1989, 25 (1):47-55.

[2] Daniela Impellizzeri, Rosanna Di Paola, Emanuela Esposito, Emanuela Mazzon, Irene Paterniti,Alessia Melani, Placido Bramanti, Felicita Pedata, Salvatore Cuzzocrea. CGS 21680, an agonist of theadenosine (A2A) receptor, decreases acute lung in?ammation. European Journal of Pharmacology.2011, 68: 305-316.

Caution: Producthasnot been fully validated for medical applications. For research use only.

Tel: (626) 353-8530 Fax: (626) 353-8530 E-mail: tech@glpbio.com

Address: 10292 Central Ave. #205, Montclair, CA, USA

3www.glpbio.com