产品
编 号:F427846
分子式:C17H20Cl2N2S
分子量:355.33
产品类型
结构图
CAS No: 69-09-0
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产品详情
生物活性:
Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis.
体内研究:
Chlorpromazine hydrochloride (20 mg/kg;腹腔注射;每日一次,持续 7 天) 抑制裸鼠体内的异种移植肿瘤生长。Animal Model:5- to 6-week-old athymic nude mice bearing intracranial U-87MG xenograft tumors.
Dosage:20 mg/kg
Administration:Injected intraperitoneally; single daily for 7 days
Result:Inhibited tumor growth on day 17.
体外研究:
Chlorpromazine hydrochloride (0,10,20,40 μM;0,24,48 h) 以剂量和时间依赖的方式抑制 U-87MG 神经胶质瘤细胞的生长。Chlorpromazine hydrochloride (20 μM;0、12、24、48 小时) 降低 U-87MG 神经胶质瘤细胞中细胞周期蛋白 A 和细胞周期蛋白 B1 的水平,12 小时后。 Chlorpromazine hydrochloride (20 μM) 抑制细胞周期进程。 Chlorpromazine hydrochloride (10 μM;1 h) 显著抑制 sEV 内化并显著减少经 sEV 处理的骨骼中的 MDSCs骨髓细胞 (MDSCs可显著抑制免疫细胞反应,引起癌细胞免疫抑制)。Chlorpromazine hydrochloride (3,10,20,40,60 μM) 阻断hNa v1.7 电流呈浓度依赖性。Chlorpromazine hydrochloride 阻断 HERG 钾通道,IC50 值为21.6 μM,希尔系数为 1.11。