An agonist of adenosine A2A receptor and inhibitor of ENT1
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A2AR Agonist-1

Item No. 28414

Technical Information
Formal Name
N-[2-(1H-indol-3-yl)ethyl]-adenosine
CAS Number
41552-95-8
Synonyms
  • JMF 1907
Molecular Formula
C20H22N6O4
Formula Weight
Purity
≥98%
Formulation
A solid
λmax
272, 364 nm
SMILES
[H][C@]1(O[C@H](CO)[C@@H](O)[C@H]1O)N2C=NC3=C(NCCC4=CNC5=C4C=CC=C5)N=CN=C32
InChi Code
InChI=1S/C20H22N6O4/c27-8-14-16(28)17(29)20(30-14)26-10-25-15-18(23-9-24-19(15)26)21-6-5-11-7-22-13-4-2-1-3-12(11)13/h1-4,7,9-10,14,16-17,20,22,27-29H,5-6,8H2,(H,21,23,24)/t14-,16-,17-,20-/m1/s1
InChi Key
QGCNEMXXKWZPHR-WVSUBDOOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    A2AR agonist-1 is an agonist of the adenosine A2A receptor and an inhibitor of equilibrative nucleoside transporter 1 (ENT1; Kis = 4.39 and 3.47 µM for the human receptor and guinea pig transporter, respectively).1 It decreases adenosine uptake by 80% in PC12 cells when used at a concentration of 61 µM and increases brain levels of adenosine in a transgenic mouse model of Huntington’s disease when administered at a dose of 20 mg/kg.2 A2AR agonist-1 (0.11 mg/kg) also rescues motor performance and increases survival in a transgenic mouse model of Huntington’s disease.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chen, J.-B., Liu, E.M., Chern, T.-R., et alDesign and synthesis of novel dual-action compounds targeting the adenosine A(2A) receptor and adenosine transporter for neuroprotection. Chem. Med. Chem. 6(8), 1390-1400 (2011).

    2. Kao, Y.H., Lin, M.S., Chen, C.M., et alTargeting ENT1 and adenosine tone for the treatment of Huntington’s disease. Hum. Mol. Genet. 26(3), 467-478 (2017).