PH797804
更新时间：2024-11-03 16:22:59
| 常用名 | 3-溴-4-(2,4-二氟苄氧基)-1-[5-[(甲基氨基)羰基]-2-甲基苯基]-6-甲基吡啶-2(1H)-酮 | CAS号 | 586379-66-0 |
|---|---|---|---|
| 价格 | ￥需询单/1kg ￥需询单/1g ￥需询单/1mg | 纯度 | 98.0% |
| 备货期 | 需询单 | 库存 | 询单 |
| 产品详情（用途，包装等）
用途： PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM; 4-fold more selective versus p38β and does not inhibit JNK2.IC50 value: 26 nM [1]Target: p38αMAPKin vitro: 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 [1]. 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 [2]. 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 [1]. 物理化学性质： CAS号：586379-66-0 常用中文名：3-溴-4-(2,4-二氟苄氧基)-1-[5-[(甲基氨基)羰基]-2-甲基苯基]-6-甲基吡啶-2(1H)-酮 常用英文名：PH-797804 分子式：C22H19BrF2N2O3 分子量：477.299 密度：1.5±0.1 g/cm3 沸点：593.2±50.0 °C at 760 mmHg 熔点：N/A 闪点：312.6±30.1 °C 储存条件：-20℃ |
- 上海阿拉丁生化科技股份有限公司
- 上海市 上海市 浦东新区
- 产品名：PH-797804
- 价格： ￥1281.9/10mg ￥823.9/5mg ￥959.9/1ml ￥6179.9/100mg
- 纯度：99.0%
- 备货期：1天
- 联系人：阿拉丁
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3-溴-4-(2,4-二氟苄氧基)-1-[5-[(甲基氨基)羰基]-2-甲基苯基]-6-甲基吡啶-2(1H)-酮生产厂家
参考价格：￥3510/25mg