CAY10449 |
カタログ番号GC43156 |
最近、比較的単純な化合物のシリーズが、人間のIP(プロスタサイクリン)受容体に対して高親和性のリガンドであり機能的な拮抗剤であることが発見されました。
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Sample solution is provided at 25 µL, 10mM.
Recently, a series of relatively simple compounds were found to be high-affinity ligands and functional antagonists for the human IP (prostacyclin) receptor. CAY10449 is one of the more potent of these. CAY10449 antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, it inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki value of about 3 nM. Although CAY10449 was not tested in rats, the related compound CAY10441 shows significant analgesic activity in standard antinociceptive assays.
Average Rating: 5
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