C3

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Cat.No. 5957 - C3 | C23H34N4O | CAS No. 1268709-57-4
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)
Datasheet
Citations
Reviews (1)
Literature

Biological Activity

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

M. Wt 382.54
Formula C23H34N4O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1268709-57-4
PubChem ID 67033699
InChI Key FPPVJOTXZIRXTF-UHFFFAOYSA-N
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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 19.13 50
ethanol 38.25 100

Preparing Stock Solutions

The following data is based on the product molecular weight 382.54. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.61 mL 13.07 mL 26.14 mL
5 mM 0.52 mL 2.61 mL 5.23 mL
10 mM 0.26 mL 1.31 mL 2.61 mL
50 mM 0.05 mL 0.26 mL 0.52 mL

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References

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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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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Cancer

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A collection of over 750 products for cancer research, the guide includes research tools for the study of:

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  • Angiogenesis
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