产品
编 号:F299793
分子式:C28H27ClF5NO
分子量:523.97
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
联系客服
产品详情
生物活性:
Penfluridol (R-16341) is a potent, long-acting, first-generation, oral diphenylbutylpiperidine antipsychotic agent by targeting D2-like dopamine receptor. Penfluridol effectively inhibits TNFα-induced NF-κB activation and alleviates the severity of arthritis and colitis in vivo. Penfluridol is a Ca2+-calmodulin inhibitor. Penfluridol induces apoptosis and autophagy. Penfluridol is used for chronic schizophrenia, acute psychosis, Tourette syndrome and autoimmune diseases. Penfluridol inhibites the growth of E. faecalis planktonic cells with the MIC of 7.81 μg/ml.

体内研究:
Penfluridol (10 mg/kg;每日灌胃给药;从第一次免疫后的第18天开始) 显着降低了胶原蛋白诱导的关节炎的严重程度。Animal Model:DBA/1J male mice aged 10–12 weeks with type II chicken collagen-induced arthritis (CIA) model
Dosage:10 mg/kg
Administration:Daily oral gavage; from the 18th day after the first immunization
Result:Inhibited inflammatory cell infiltration, suppressed pannus formation, and protected articular cartilage from damage. obviously decreased mRNA expressions of CXCL10 and MCP-1 in inflamed joints and statistically reduced production levels of inflammatory cytokines IL-1β and IL-6 in sera.

体外研究:
Penfluridol (R-16341;1.25-40 μM;24、48 小时) 会降低携带 FLT3-WT 或 FLT3-ITD 突变的人 AML 细胞的细胞活力。Penfluridol (7.5 μM;24 小时) 会导致携带 FLT3-WT 和 FLT3-ITD 突变的 AML 细胞凋亡。Penfluridol (1.25-7.5 μM;24 小时) 通过触发 LC3 周转和酸性泡状细胞器 (AVO) 形成来诱导 ROS 介导的自噬。Penfluridol (1μM;2 小时) 抑制 TNFα 诱导的 ERK,JNK 和 P38 的磷酸化水平。Penfluridol (1μM;2 小时) 抑制 TNFα 诱导的 IL-1β,IL-6,IL-17 和 NOS2 的 mRNA 表达。Penfluridol 抑制脾脏幼稚的 CD4+T 细胞对 Th1 和 Th17 的分化,并抑制 M1 巨噬细胞极化。
产品资料