A potent

SCH 442416 – 1 mg

Brand:
Cayman
CAS:
316173-57-6
Storage:
-20
UN-No:
Non-Hazardous - /

SCH 442416 is a potent, brain-permeable, and selective adenosine A2A receptor (A2AR) antagonist.{40048} It is selective for A2AR with a Ki value of 0.048 nM compared to 1,111, >10,000, and >10,000 nM for A1R, A2BR, and A3R, respectively, using human recombinant protein in a radioligand binding assay. It is also selective for A2AR (Ki = 0.50 nM) in rat cerebral membranes over A1R and A3R (Kis = 1,815 and >10,000, respectively). Biodistribution in rats demonstrates preferential uptake by liver, adrenal gland, kidney, and lungs, and by the striatum in the brain. SCH 442416 (10 μM) attenuates adenosine-mediated and A2AR agonist-induced arteriole dilation.{40049}  

 

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Description

A potent, brain-permeable, and selective A2AR antagonist; selective for A2AR over A1R, A2BR, and A3R (Kis = 0.048, 1,111, >10,000, and >10,000 nM, respectively) using human recombinant receptors; selective for A2AR over A1R and A3R in rat cerebral membranes (Kis = 0.50, 1,815, and >10,000 nM, respectively); is taken up preferentially by liver, adrenal gland, kidney, and lungs, and by the striatum in the brain; attenuates adenosine-mediated and A2AR agonist-induced arteriole dilation at a concentration of 10 μM

Formal name: 2-(2-furanyl)-7-[3-(4-methoxyphenyl)propyl]-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine

Synonyms: 

Molecular weight: 389.4

CAS: 316173-57-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Cardiovascular System|Vasculature|Vasoconstriction||Research Area|Neuroscience

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