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PF 4693627
- PF 04693627
- Optical Purity: >98% d.e.
- Soluble in DMSO
- MF: C26H29Cl2N3O3
- MW: 502.43
Description
PF 4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with reported IC50 values of 3 nM in enzyme assays and 109 nM in whole-blood assays.
mPGES-1 catalyzes inducible PGE2 formation downstream of COX-derived PGH2 and is a target for anti-inflammatory pharmacology. PF 4693627 is useful for studying selective suppression of PGE2 production without directly inhibiting COX enzymes.
Key Features
- Potent mPGES-1 inhibitor
- Reported IC50: 3 nM enzyme assay; 109 nM whole-blood assay
- Selective over COX-2 and other eicosanoid pathway enzymes in reported profiling
- Orally bioavailable anti-inflammatory pharmacology
Applications
- mPGES-1 enzyme assays
- PGE2 biosynthesis studies
- Inflammation model research
- Eicosanoid pathway inhibitor profiling
More Information
| Parent CAS No. | 1312815-93-2 |
|---|---|
| Chemical Name | 1-(5-chloro-6-(4-chlorophenyl)benzo[d]oxazol-2-yl)-N-((1S,3S)-3-(hydroxymethyl)cyclohexyl)piperidine-4-carboxamide |
| extra_info | . |
| SMILES | N1(C2=NC3=CC(Cl)=C(C4=CC=C(Cl)C=C4)C=C3O2)CCC(C(N[C@H]2CCC[C@H](CO)C2)=O)CC1 |&1:23,27,r| |
| MFCD | N.A. |
| InChi | 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 |
| InChiKey | CPDNPVKDQXLYHO-JXFKEZNVSA-N |
| CID | 53252516 |
| Short Description | mPGES-1 inhibitor |
References
- G.B. Arhancet 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. 2013, 23, 1114-1119.
- D.P. Walker et al. Synthesis and biological evaluation of substituted benzoxazoles as inhibitors of mPGES-1: use of a conformation-based hypothesis to facilitate compound design. Bioorg. Med. Chem. Lett. 2013, 23, 1120-1126.
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