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Submit ReviewPF 8380
说明： Potent autotaxin inhibitor
化学名： 3,5-Dichlorobenzyl-[4-[3-oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]]piperazine-1-carboxylate
纯度： ≥97% (HPLC)
生物活性 for PF 8380
PF 8380 is a potent autotaxin inhibitor (IC50 = 2.8 nM in isolated enzyme assay; 101 nM in human whole blood). Modulates lysophosphatidic acid (LPA) levels in vivo and in vitro by directly inhibiting autotaxin; reduces LPA levels both in plasma and at site of inflammation. Decreases leptin-induced MMP13 expression, in vitro. Orally available.
技术数据 for PF 8380
| 分子量 | 478.33 |
| 公式 | C22H21Cl2N3O5 |
| 储存 | Store at -20°C |
| 纯度 | ≥97% (HPLC) |
| CAS Number | 1144035-53-9 |
| PubChem ID | 25265312 |
| InChI Key | JMSUDQYHPSNBSN-UHFFFAOYSA-N |
| Smiles | O=C(C2=CC(OC(N4)=O)=C4C=C2)CCN1CCN(C(OCC3=CC(Cl)=CC(Cl)=C3)=O)CC1 |
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 PF 8380
参考文献 for PF 8380
参考文献是支持产品生物活性的出版物。
Gierse et al (2010) A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation. J.Pharmacol.Exp.Ther. 334 310 PMID: 20392816
Jankowski (2011) Autotaxin: its role in biology of melanoma cells and as a pharmacological target. Enzyme Res. 194857 PMID: 21423677
Poulami et al (2017) High-fat diet-induced acceleration of osteoarthritis is associated with a distinct and sustained plasma metabolite signature. Sci.Rep. 7 8205 PMID: 28811491
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关键词: PF 8380, PF 8380 supplier, PF8380, pfizer, autotaxin, lysophospholipase, d, inhibitors, lysophosphatidic, acid, LPA, inhibits, potent, Autotaxin, 4078, Tocris Bioscience
PF 8380 的评论
平均评分: 5 (基于 2 条评论。)
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The effect of ATX inhibition on LPS induced pro-inflammatory phenotype in microglia..
By
lisha joshi on 06/10/2019
分析类型： In Vitro
种属： Mouse
细胞系/组织： BV2 microglia cells
PF8380 was used to inhibit autotaxin in BV2 microglia cells in order to study the effect of ATX-LPA axis on microglia proinflammatory phenotype. Cells were treated with LPS (20ng/mi) in the absence or presence of the inhibitor (10µM) for 24 hours and then collected for RNA isolation and subsequent analysis of iNOS and TNFa expression with qPCR.
PF 8380 decreases the levels of lysophosphatidic acid in mouse brain.
By
Joanna Plastira on 10/10/2018
分析类型： In Vivo
种属： Mouse
细胞系/组织： Brain
During preliminary studies we investigated whether the ATX inhibitor PF-8380 crosses the BBB and impacts LPA levels in the brain. After oral gavage of 3mg/kg PF-8380 per mouse (PF-8380 was dissolved in hydroxyl methyl cellulose), mice were anesthetized and perfused with PBS at different time points and the whole brains were dissected and immediately snap frozen in liquid nitrogen. Lipids were extracted using the Bligh & Dyer HCl method and the levels of LPA and PF-8380 were quantitated by LC-MS/MS.
