Biological Activity
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.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc
Technical Data
| M. Wt | 477.3 |
| Formula | C22H19BrF2N2O3 |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 23.86 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 477.3. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 2.1 mL | 10.48 mL | 20.95 mL |
| 5 mM | 0.42 mL | 2.1 mL | 4.19 mL |
| 10 mM | 0.21 mL | 1.05 mL | 2.1 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: PH 797804, supplier, PH797804, potent, selective, p38a, p38alpha, p38b, p38beta, p38α, p38β, inhibitors, inhibits, anti-inflammatory, p38, p38, Tocris Bioscience
