An orally bioavailable

AAT-008 – 25 mg

Brand:
Cayman
CAS:
847727-81-5
Storage:
-20
UN-No:
Non-Hazardous - /

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).{33448} 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.  

 

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Description

An orally bioavailable, potent, and selective EP4 receptor antagonist (IC50 = 16.3 nM in a human EP4 functional assay); selective for EP4, with IC50 values of 2.4, 1,890, >20,000, and >20,000 nM for binding to human EP4, EP2, EP1, and EP3, respectively; has potent binding affinity for human, rat, and dog EP4 (Kis = 0.97, 6.1, and 38 nM, respectively; suppresses PGE2-induced elevation of intracellular cAMP in vitro (pA2 = 1.1 nM); reduces carrageenan-induced mechanical hyperalgesia in rats in a dose-dependent manner,

Formal name: 4-[(1S)-1-[[[5-chloro-2-(3-fluorophenoxy)-3-pyridinyl]carbonyl]amino]ethyl]-benzoic acid

Synonyms: 

Molecular weight: 414.8

CAS: 847727-81-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway

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