An agonist of the adenosine A2A receptor and an inhibitor of ENT1 (Kis = 4.39 and 3.47 µM

A2AR Agonist-1 – 5 mg

Brand:
Cayman
CAS:
41552-95-8
Storage:
-20
UN-No:
Non-Hazardous - /

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).{50081} 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.{47653} A2AR agonist-1 (0.11 mg/kg) also rescues motor performance and increases survival in a transgenic mouse model of Huntington’s disease.  

 

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Description

An agonist of the adenosine A2A receptor and an inhibitor of ENT1 (Kis = 4.39 and 3.47 µM, for the human receptor and guinea pig transporter, respectively); decreases adenosine uptake by 80% in PC12 cells at 61 µM and increases brain levels of adenosine in a transgenic mouse model of Huntington’s disease at 20 mg/kg; rescues motor performance and increases survival in a transgenic mouse model of Huntington’s disease at 0.11 mg/kg

Formal name: N-[2-(1H-indol-3-yl)ethyl]-adenosine

Synonyms:  JMF 1907

Molecular weight: 410.4

CAS: 41552-95-8

Purity: ≥98%

Formulation: A solid

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