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Chlorpromazine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Chlorpromazine图片
CAS NO:50-53-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
氯丙嗪
产品介绍
Chlorpromazine 是一种口服有效的、可透过血脑屏障的抗精神病剂,能有效拮抗D2多巴胺受体和5-HT2A,已广泛用于精神分裂症和其他精神疾病。Chlorpromazine 可通过多种途径发挥抗癌活性,包括抗增殖、诱导自噬和周期停滞 (G2-M 期)、抑制细胞色素 c 氧化酶 (CcO)、抑制肿瘤生长和转移以及抑制肿瘤免疫逃逸等。Chlorpromazine 还能阻断 hNav1.7 通道 (IC50=25.9 μM; 浓度依赖的方式) 和 HERG 钾通道 (IC50=21.6 μM) ,其在止痛以及心律失常方面也具有较好的研究潜力。Chlorpromazine 也能抑制网格蛋白介导的内吞作用。
生物活性

Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonisesD2 dopamine receptorsand5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction ofautophagyand cycle arrest (G2-M phase), inhibition ofcytochrome c oxidase(CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine 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 also can inhibit clathrin-mediated endocytosis[1][2][3][4][5].

IC50& Target

D2 dopamine receptors; 5-HT2A[1][6].

体外研究
(In Vitro)

Chlorpromazine (0, 10, 20, 40 μM; 0, 24, 48 h) inhibits growth of U-87MG glioma cells in a dose- and time- dependent manner[2].
Chlorpromazine (20 μM; 0, 12, 24, 48 h) decreases the levels of cyclin A and cyclin B1 in U-87MG glioma cells, 12 h later[2].
Chlorpromazine (20 μM) causes inhibition of cell cycle progression[2].
Chlorpromazine (10 μM; 1 h) significantly suppresses the sEV internalization and dramatically reduces MDSCs in sEV-treated bone marrow cells (MDSCs can significantly suppress the immune cell response, causing immunosuppression in cancer cells)[3].
Chlorpromazine (3, 10, 20, 40, 60 μM) blocks the hNav1.7 current in a concentration-dependent manner[4].
Chlorpromazine blocks HERG potassium channels with an IC50value of 21.6 μM and a Hill coefficient of 1.11[5].

Cell Proliferation Assay[2]

Cell Line:U-87MG glioma cells
Concentration:0, 10, 20, 40 μM
Incubation Time:0, 24, 48 h
Result:Showed anti-proliferative activity in a dose- and time-dependent manner.

Immunofluorescence[3]

Cell Line:Bone marrow cells (sEV-treated)
Concentration:10 μM
Incubation Time:1 h
Result:Reduced MDSCs and suppressed the sEV internalization.

Western Blot Analysis[2]

Cell Line:U-87MG glioma cells
Concentration:20 μM
Incubation Time:0, 12, 24, 48 h
Result:Decreased the levels of cyclin A and cyclin B1 12 h later, whereas levels of cyclin D1, proliferating cell nuclear antigen and GAPDH remained unchanged.
体内研究
(In Vivo)

Chlorpromazine (20 mg/kg; i.p.; single daily for 7 days) inhibits xenograft tumor growth in nude mouse[2].

Animal Model:5- to 6-week-old athymic nude mice bearing intracranial U-87MG xenograft tumors[2].
Dosage:20 mg/kg
Administration:Injected intraperitoneally; single daily for 7 days
Result:Inhibited tumor growth on day 17.
分子量

318.86

Formula

C17H19ClN2S

CAS 号

50-53-3

中文名称

氯丙嗪

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.