AAT-008 |
| Catalog No.GC42666 |
AAT-008 est un antagoniste des récepteurs de la prostaglandine EP4 puissant, sélectif et actif par voie orale avec Kis de 0,97 et 6,1 nM pour l'EP4 humain recombinant et l'EP4 de rat recombinant, respectivement .
Products are for research use only. Not for human use. We do not sell to patients.
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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