| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| P408962-1ml |
1ml |
现货  |
|
| 英文别名 | 3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | PH-797804 |
| 生化机理 | PH-797804 是一种新型吡啶酮 p38α 抑制剂，在无细胞试验中的 IC50 值为 26 nM；其选择性是 p38β 的 4 倍，并且不抑制 JNK2。第 2 阶段。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | MAP 激酶 p38 alpha 抑制剂 |
| 产品介绍 |
Information PH-797804 is a novel pyridinone inhibitor ofp38αwithIC50of 26 nM in a cell-free assay; 4-fold more selective versus p38β and does not inhibit JNK2. Phase 2. PH-797804 blocks LPS-induced TNF-α production and p38 kinase activity in the human monocytic U937 cell line, with comparable IC50 of 5.9 nM and 1.1 nM. PH-797804 has no inhibitory effect on either the JNK pathway (c-Jun phosphorylation) or ERK pathway (ERK phosphorylation) in U937 cells at concentrations up to 1 μM. PH-797804 inhibits RANKL- and M-CSF-induced osteoclast formation in a concentration-dependent manner, with IC50 of 3 nM in primary rat bone marrow cells. IC50 values for PH-797804 against the following targets have been determined to be greater than 200 μM (unless specified): CDK2, ERK2, IKK1, IKK2, IKKi, MAPKAP2, MAPKAP3, MKK7 (>100 μM), MNK, MSK (>164 μM), PRAK, RSK2, and TBK1, which means the activity of PH-797804 is specific. In vivo Orally dosing of PH-797804 effectively inhibits acute inflammatory responses induced by systemically administered endotoxin in both rat and cynomolgus monkeys. PH-797804 treatment for 10 days demonstrates robust anti-inflammatory activity in chronic disease models, significantly reducing both joint inflammation and associated bone loss in streptococcal cell wall-induced arthritis in rats and mouse collagen-induced arthritis. Dose-response analysis resulted in ED50 values of 0.07 mg/kg and 0.095 mg/kg in rat and cynomolgus monkeys, respectively. PH-797804 inhibits LPS-induced TNF-α, IL-6, and MK-2 activity in a dose- and concentration-dependent manner in a human endotoxin challenge model. cell lines： Concentrations：-- Incubation Time：-- Powder Purity:≥99% |
| IC50 | p38α, IC50: 26 nM |
|---|
| Canonical SMILES | CNC(=O)C1=CC(=C(C)C=C1)N2C(=CC(=C(Br)C2=O)OCC3=CC=C(F)C=C3F)C |
|---|---|
| 分子量 | 477.3 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 71 mg/mL (198.66 mM); Ethanol: 3 mg/mL warmed with 50ºC Water: bath (8.39 mM); Water: Insoluble; |
|---|
| concentration | 9.0-11.0（mmol/L） |
|---|---|
| NMR Spectrum 1H | Conforms to Structure |
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