An orally bioavailable mPGES-1 inhibitor
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PF-4693627

Item No. 22768

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[5-chloro-6-(4-chlorophenyl)-2-benzoxazolyl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-4-piperidinecarboxamide
CAS Number
1312815-93-2
Molecular Formula
C26H29Cl2N3O3
Formula Weight
502.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/mlEthanol: 5 mg/ml
λmax
300 nm
SMILES
ClC1=CC=C(C2=CC(OC(N3CCC(C(N[C@@H]4C[C@@H](CO)CCC4)=O)CC3)=N5)=C5C=C2Cl)C=C1
InChi Code
InChI=1S/C26H29Cl2N3O3/c27-19-6-4-17(5-7-19)21-13-24-23(14-22(21)28)30-26(34-24)31-10-8-18(9-11-31)25(33)29-20-3-1-2-16(12-20)15-32/h4-7,13-14,16,18,20,32H,1-3,8-12,15H2,(H,29,33)/t16-,20-/m0/s1
InChi Key
CPDNPVKDQXLYHO-JXFKEZNVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $41

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    1 mg

    $75

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    5 mg

    $351

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    10 mg

    $659

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    Product Description

    PF-4693627 is an orally bioavailable inhibitor of microsomal prostaglandin E (PGE) synthase-1 (mPGES-1; IC50 = 3 nM).1 It is selective for mPGES-1 over PGDS, TXAS, and 5-LO in HWB-1483 cells, which have IC50 values greater than 50 μM, as well as COX-2 in fetal fibroblasts (IC50 = >10 μM). PF-4693627 inhibits LPS-stimulated synthesis of PGE2 in human whole blood (IC50 = 109 nM). In vivo, PF-4693627 (10 mg/kg) inhibits PGE2 production in a guinea pig model of carrageenan-induced air pouch inflammation.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Arhancet, G.B., Walker, D.P., Metz, S., et al. Discovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation. Bioorg. Med. Chem. Lett. 23(4), 1114-1119 (2013).