A2AR-agonist-1

An agonist of adenosine A2A receptor and inhibitor of ENT1

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库存: 现货

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5mg

￥3737.00

2990.00

- +
10mg

￥5350.00

4280.00

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50mg

￥15887.00

12710.00

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100mg

￥22250.00

17800.00

- +

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Background

A_2AR agonist-1 is an agonist of the adenosine A_2A receptor and an inhibitor of equilibrative nucleoside transporter 1 (ENT1; K_is = 4.39 and 3.47 ?M 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 ?M 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 A_2AR agonist-1 (0.11 mg/kg) also rescues motor performance and increases survival in a transgenic mouse model of Huntington’s disease.

1.Chen, J.-B., Liu, E.M., Chern, T.-R., et al.Design and synthesis of novel dual-action compounds targeting the adenosine A(2A) receptor and adenosine transporter for neuroprotectionChem. Med. Chem.6(8)1390-1400(2011) 2.Kao, Y.H., Lin, M.S., Chen, C.M., et al.Targeting ENT1 and adenosine tone for the treatment of Huntington's diseaseHum. Mol. Genet.26(3)467-478(2017)