Product overview

Name CGS 21680 hydrochloride
Purity >98%
Description Prototypic, selective A2A receptor agonist
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Biological Data

Biological description

Prototypic, selective A2A receptor agonist that also shows some affinity at A1 and A3 receptors (Ki values are 25, 289 and 69 nM at A2A, A1 and A3, EC50 = 89 µM at A2B receptors respectively).

Can be used to distinguish A2A- and A2B- mediated effects.

The crystal structure of hA2AR thermostabilized in an active-like confirmation with CGS21680 has been described.

Additionally shows hypotensive, anti-inflammatory and neuroprotective effects. Active in vivo.

Solubility & Handling

Storage instructions -20°C (desiccate)
Solubility overview Soluble in DMSO (100 mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

Calculators

Molarity

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Dilution

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Chemical Data

Purity >98%
Chemical name 4-[2-[[6-Amino-9-(N-ethyl-β-D-ribofu ranuronamidosyl)-9H-purin-2-yl]amino]ethyl]benzene propanoic acid hydrochloride
Molecular Weight 535.99
Chemical structure CGS 21680 hydrochloride [124431-80-7] Chemical Structure
Molecular Formula C23H29N7O6.HCl
CAS Number 124431-80-7
PubChem identifier 44134621
SMILES CCNC(=O)C1C(C(C(O1)N2C=NC3=C2N=C(N=C3N)NCCC4=CC=C(C=C4)CCC(=O)O)O)O.Cl
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
InChiKey QPHVMNOEKKJYJO-UHFFFAOYSA-N
MDL number MFCD11045878
Appearance White solid

References for CGS 21680 hydrochloride

References are publications that support the biological activity of the product
  • Molecular Determinants of CGS21680 Binding to the Human Adenosine A2A Receptor

    Lebon et al (2015) Mol Pharmacol. 87(6) : 907-15
  • Effects of CGS 21680, a selective A2A adenosine receptor agonist, on cardiac output and vascular resistance in acute heart failure in the anaesthetized rat

    Nekooeian and Tabrizchi (1998) Br J Pharmacol. 123(8) : 1666-72
  • The selective adenosine A2 receptor agonist, CGS 21680, is a potent depressant of cerebral cortical neuronal activity

    Phillis JW (1990) Brain Res. 509(2) : 328-30

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