An orally bioavailable, potent, and selective EP4 receptor antagonist
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AAT-008

Item No. 21810

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(1S)-1-[[[5-chloro-2-(3-fluorophenoxy)-3-pyridinyl]carbonyl]amino]ethyl]-benzoic acid
CAS Number
847727-81-5
Molecular Formula
C21H16ClFN2O4
Formula Weight
414.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 0.5 mg/ml
λmax
234, 293 nm
SMILES
C[C@H](NC(C1=CC(Cl)=CN=C1OC2=CC=CC(F)=C2)=O)C3=CC=C(C(O)=O)C=C3
InChi Code
InChI=1S/C21H16ClFN2O4/c1-12(13-5-7-14(8-6-13)21(27)28)25-19(26)18-9-15(22)11-24-20(18)29-17-4-2-3-16(23)10-17/h2-12H,1H3,(H,25,26)(H,27,28)/t12-/m0/s1
InChi Key
FKXDPPYCCKCVCW-LBPRGKRZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $268

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    25 mg

    $587

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    Product Description

    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).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Okumura, Y., Yamagishi, T., Nukui, S., et al. Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist. Bioorg. Med. Chem. Lett. 27(5), 1186-1192 (2017).