Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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P127738-5mg | 5mg | In stock | $117.90 | |
P127738-10mg | 10mg | In stock | $192.90 | |
P127738-25mg | 25mg | In stock | $404.90 | |
P127738-100mg | 100mg | In stock | $1,028.90 |
Novel, potent, pyridinone-based, ATP-competitive p38α inhibitor
Synonyms | SMR004702814 | C74360 | PH-797804, >=98% (HPLC) | PH-797804, (AXIAL S)-(-)- | UNII-SI09I1V827 | 1358027-80-1 | CCG-35835 | GTPL7818 | PH797804 | PH-797804 | 3-(3-Bromo-4-((2,4-difluorobenzyl)oxy)-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide | 107 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | PH-797804 is a novel p38α inhibitor of pyridone, ic50 is 26 nM in cell-free tests, which is more than 4 times more selective than p38β and does not inhibit JNK2. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | MAP kinase p38 alpha inhibitor |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
ALogP | 4.2 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 3-[3-bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxopyridin-1-yl]-N,4-dimethylbenzamide |
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INCHI | InChI=1S/C22H19BrF2N2O3/c1-12-4-5-14(21(28)26-3)9-18(12)27-13(2)8-19(20(23)22(27)29)30-11-15-6-7-16(24)10-17(15)25/h4-10H,11H2,1-3H3,(H,26,28) |
InChi Key | KCAJXIDMCNPGHZ-UHFFFAOYSA-N |
Canonical SMILES | CC1=C(C=C(C=C1)C(=O)NC)N2C(=CC(=C(C2=O)Br)OCC3=C(C=C(C=C3)F)F)C |
Isomeric SMILES | CC1=C(C=C(C=C1)C(=O)NC)N2C(=CC(=C(C2=O)Br)OCC3=C(C=C(C=C3)F)F)C |
Alternate CAS | 1358027-80-1 |
PubChem CID | 22049997 |
Molecular Weight | 477.3 |
PubChem CID | 22049997 |
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ChEMBL Ligand | CHEMBL1088751 |
CAS Registry No. | 586379-66-0 |
RCSB PDB Ligand | I45 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
I2203376 | Certificate of Analysis | Jun 19, 2024 | P127738 |
I2203377 | Certificate of Analysis | Jun 19, 2024 | P127738 |
I2203427 | Certificate of Analysis | Jun 19, 2024 | P127738 |
I2205320 | Certificate of Analysis | Jun 19, 2024 | P127738 |
Solubility | DMSO ≥93mg/mL Water <1.2mg/mL Ethanol ≥9.5mg/mL |
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1. Selness SR, Devraj RV, Devadas B, Walker JK, Boehm TL, Durley RC, Shieh H, Xing L, Rucker PV, Jerome KD et al.. (2011) Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase.. Bioorg Med Chem Lett, 21 (13): (4066-71). [PMID:21641211] [10.1021/op500134e] |
2. MacNee W, Allan RJ, Jones I, De Salvo MC, Tan LF. (2013) Efficacy and safety of the oral p38 inhibitor PH-797804 in chronic obstructive pulmonary disease: a randomised clinical trial.. Thorax, 68 (8): (738-45). [PMID:23539534] [10.1021/op500134e] |