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Submit ReviewRoflumilast
说明： Potent and selective PDE4 inhibitor
化学名： 3-(Cyclopropylmethoxy)-N-(3,5-dichloro-4-pyridinyl)-4-(difluoromethoxy)benzamide
纯度： ≥98% (HPLC)
生物活性 for Roflumilast
Roflumilast is a potent and selective PDE4 inhibitor (IC50 values are 0.2 to 4.3 nM for various splice variants of PDE4). Exhibits > 1000-fold selectivity for PDE4 over other PDE family members. Demonstrates effects on functioning of neutrophils, CD4+ and CD8+ T-cells, endothelial, epithelial and smooth muscle cells, as well as fibroblasts, in vitro. Attenuates lung inflammation, mucociliary malfunction, lung fibrosis, oxidative stress, pulmonary vascular remodeling and pulmonary hypertension in animal models of COPD disease mechanisms.
化合物库 for Roflumilast
Roflumilast is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
技术数据 for Roflumilast
| 分子量 | 403.21 |
| 公式 | C17H14Cl2F2N2O3 |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 162401-32-3 |
| PubChem ID | 449193 |
| InChI Key | MNDBXUUTURYVHR-UHFFFAOYSA-N |
| Smiles | FC(F)OC(C=C1)=C(OCC2CC2)C=C1C(NC3=C(Cl)C=NC=C3Cl)=O |
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 Roflumilast
参考文献 for Roflumilast
参考文献是支持产品生物活性的出版物。
Hatzelmann et al (2010) The preclinical pharmacology of roflum. - a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease. Pulm.Pharmacol.Ther. 23 235 PMID: 20381629
Rabe (2011) Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease. Br.J.Pharmacol. 163 53 PMID: 21232047
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关键词: Roflumilast, Roflumilast supplier, Roflumilast, potent, selective, phosphodiesterase, 4, PDE4, inhibitors, inhibits, PDE4A, PDE4B, PDE4C, PDE4D, Phosphodiesterases, 6641, Tocris Bioscience
2 篇 Roflumilast 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Roflumilast 的部分引用包括：
Martin J et al (2020) Optical Mapping of cAMP Signaling at the Nanometer Scale. Cell 182 1519-1530.e17 PMID: 32846156
Ronald M et al (2022) FGF1 and insulin control lipolysis by convergent pathways. Cell Metab 34 171-183.e6 PMID: 34986332
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