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PH-797804,586379-66-0

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  • ¥350 - 5000
  • MedChemExpress(MCE)已认证
  • 美国
  • HY-10403
  • 2025年12月05日
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    • 详细信息
    • 文献和实验
    • 技术资料
    • 保存条件

      Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

    • 库存

      货期:1-2天

    • 供应商

      MedChemExpress LLC

    • CAS号

      586379-66-0

    • 规格

      10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg

    规格:10 mM * 1 mL产品价格:¥1050.0
    规格:1 mg产品价格:¥350.0
    规格:5 mg产品价格:¥1000.0
    规格:10 mg产品价格:¥1700.0
    规格:25 mg产品价格:¥3400.0
    规格:50 mg产品价格:¥5000.0

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    PH-797804

    CAS No. : 586379-66-0

    MCE 国际站:PH-797804

    产品活性:PH-797804 是一种 ATP 竞争性的,选择性的 p38α/p38β 抑制剂,对 p38α 的 IC50 为 26 nM,Ki 值为 5.8 nM;对 p38β 的 Ki 值为 40 nM,对 JNK2 没有抑制作用.

    研究领域:MAPK/ERK Pathway  |  Autophagy

    作用靶点:p38 MAPK  |  Autophagy

    In 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.
    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.

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      无菌过滤高压灭菌(8磅10min)。 (6)磷酸缓冲液:pH7.4。 磷酸氢二钠28.8g(H2O)、磷酸二氢钾2.67g(无水),溶于1000ml双蒸水中,加肝素,终浓度为100u/ml。 (7)Giemsa染色液: Giemsa粉剂           1g 甘油              66ml 在研钵中,加入少量甘油油仔细研磨然后放甘油全部加磨,60℃温箱中保温2h,冷却后加入甲醇66ml。装入有色瓶中混合待用。染色时用pH

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