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Submit ReviewPH 797804
说明： Potent and selective p38α/β inhibitor
化学名： (-)-3-[3-Bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxo-1(2H)-pyridinyl]-N,4-dimethylbenzamide
纯度： ≥98% (HPLC)
生物活性 for PH 797804
PH 797804 is a potent and selective p38α/β inhibitor (IC50 values are 26 and 102 nM, respectively). Exhibits >100-fold selectivity for p38α/β over 71 other kinases, enzymes and GPCRs, including p38γ, p38δ, JNK and ERK2. Inhibits LPS-induced TNFα production in U937 monocytes in vitro. Suppresses acute and chronic inflammatory responses in rat models of arthritis. Orally active.
PH 797804 is the (-)-atropisomer, which is 100-fold more potent than its (+)-atropisomer.
许可信息
Sold for research purposes under agreement from Pfizer Inc
化合物库 for PH 797804
PH 797804 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
技术数据 for PH 797804
| 分子量 | 477.3 |
| 公式 | C22H19BrF2N2O3 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1358027-80-1 |
| PubChem ID | 22049997 |
| InChI Key | KCAJXIDMCNPGHZ-UHFFFAOYSA-N |
| Smiles | FC1=CC=C(COC2=C(Br)C(N(C3=CC(C(NC)=O)=CC=C3C)C(C)=C2)=O)C(F)=C1 |
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.
溶解性数据 for PH 797804
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 23.86 | 50 |
制备储备液 for PH 797804
以下数据基于产品分子量 477.3。 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.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.19 mL | 20.95 mL | 41.9 mL |
| 2.5 mM | 0.84 mL | 4.19 mL | 8.38 mL |
| 5 mM | 0.42 mL | 2.1 mL | 4.19 mL |
| 25 mM | 0.08 mL | 0.42 mL | 0.84 mL |
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产品说明书 for PH 797804
参考文献 for PH 797804
参考文献是支持产品生物活性的出版物。
Hope et al (2009) Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation. J.Pharmacol.Exp.Ther. 331 882 PMID: 19720877
Selness et al (2011) Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase. Bioorg.Med.Chem.Lett. 21 4066 PMID: 21641211
If you know of a relevant reference for PH 797804, please let us know.
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关键词: PH 797804, PH 797804 supplier, PH797804, potent, selective, p38a, p38alpha, p38b, p38beta, p38α, p38β, inhibitors, inhibits, anti-inflammatory, p38, 5866, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.
Pathways for PH 797804
