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说明： Selective microsomal prostaglandin E synthase 1 (mPGES-1) inhibitor
化学名： N-Cyclopentyl-1-[5,6-dimethyl-1-(1-methylethyl)-1H-benzimidazol-2-yl]-4-piperidinecarboxamide
纯度： ≥98% (HPLC)
生物活性 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.
技术数据 for C3
| 分子量 | 382.54 |
| 公式 | C23H34N4O |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for C3
参考文献 for C3
参考文献是支持产品生物活性的出版物。
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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关键词: C3, C3 supplier, compound, 3, selective, microsomal, prostaglandin, E, synthase, 1, inhibitors, inhibits, mPGES-1, PGES, PGE2, Other, Synthases/Synthetases, 5957, Tocris Bioscience
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平均评分: 5 (Based on 1 Review.)
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C3 inhibits LPA induced COX-2 expression in osteosarcoma cells.
By
Christopher Trummer on 10/23/2018
分析类型： In Vitro
种属： Human
细胞系/组织： 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.
