Discontinued Product

C3 (Cat. No. 5957) has been withdrawn from sale for commercial reasons.
Description: Selective microsomal prostaglandin E synthase 1 (mPGES-1) inhibitor
Chemical Name: N-Cyclopentyl-1-[5,6-dimethyl-1-(1-methylethyl)-1H-benzimidazol-2-yl]-4-piperidinecarboxamide
Purity: ≥98% (HPLC)
Reviews (1)

Biological Activity for C3

C3 is a selective microsomal prostaglandin E synthase 1 (mPGES-1) inhibitor (IC50 values are 90 and 900 nM for rat and human mPGES-1, respectively). Displays selectivity for mPGES-1 over COX-1, COX-2, PGIS, hPGDS and iPGDS (% inhibition values are 15, 18, 0, 0 and 60 % inhibition at 50 μM, respectively). Reduces PGE2 production in vitro and in a localized inflammation animal model. Elevates CD80 expression by tumor associated phagocytes in vitro. Also decreases vascular contractility, in ex vivo human vessels.

Technical Data for C3

M. Wt 382.54
Formula C23H34N4O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1268709-57-4
PubChem ID 67033699
Smiles CC(N1C2=CC(C)=C(C=C2N=C1N3CCC(C(NC4CCCC4)=O)CC3)C)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

References for C3

References are publications that support the biological activity of the product.

Leclerc et al (2013) Characterization of a human and murine mPGES-1 inhibitor and comparison to mPGES-1 genetic deletion in mouse models of inflammation. Prostaglandins Other Lipid Mediat. 107 26 PMID: 24045148

Ozen et al (2017) Inhibition of microsomal PGE synthase-1 reduces human vascular tone by increasing PGI2: a safer alternative to COX-2 inhibition. Br.J.Pharmacol. 174 4087 PMID: 28675448

Olesch et al (2015) MPGES-1-derived PGE2 suppresses CD80 expression on tumor-associated phagocytes to inhibit anti-tumor immune responses in breast cancer. Oncotarget 6 10284 PMID: 25871398

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Keywords: C3, C3 supplier, compound, 3, selective, microsomal, prostaglandin, E, synthase, 1, inhibitors, inhibits, mPGES-1, PGES, PGE2, Other, Synthases/Synthetases, 5957, Tocris Bioscience

Citations for C3

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Currently there are no citations for C3.

Reviews for C3

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C3 inhibits LPA induced COX-2 expression in osteosarcoma cells.
By Christopher Trummer on 10/23/2018
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Osteosarcoma

MG-63 cells were treated with LPA (10 µM) alone or in combination with C3 (20 µM), PTX (Pertussis Toxin, 400 ng/ml) or H2L 5765834 (20 µM) for 3 h to follow COX-2 expression using Western blot. C3 inhibited COX-2 expression induced by LPA.

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