AAT-008 |
| カタログ番号GC42666 |
AAT-008 は、組換えヒト EP4 および組換えラット EP4 に対してそれぞれ 0.97 nM および 6.1 nM の Kis を持つ強力で選択的な経口活性プロスタグランジン EP4 受容体アンタゴニストです 。
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Cas No.: 847727-81-5
Sample solution is provided at 25 µL, 10mM.
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AAT-008 is an orally bioavailable and potent antagonist of the prostaglandin E2 (PGE2) receptor subtype 4 (EP4; IC50 = 16.3 nM in a human EP4 functional assay). It is selective for EP4 with IC50 values of 2.4, 1,890, >20,000, and >20,000 nM for binding to human recombinant EP4, EP2, EP1, and EP3, respectively. AAT-008 has potent binding affinity for human, rat, and dog EP4 (Kis = 0.97, 6.1, and 38 nM, respectively) and suppresses PGE2-induced elevation of intracellular cAMP with an antagonistic potency (pA2) of 1.1 nM in vitro. Oral administration of AAT-008 reduces carrageenan-induced mechanical hyperalgesia in rats in a dose-dependent manner.
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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