| 生物活性: |
靶点:Parasite 通路:Anti-infection 背景说明:是一种抗蠕虫化合物。 生物活性:Pyrvinium pamoate 是一种抗蠕虫药,可抑制 WNT 通路信号传导。[1-2] In Vitro:扑蛲灵可抑制不同亚型乳腺癌细胞(管腔型、MCF-7、claudin-l-L-1、MCF-7、MCF-7、claudin-l-1、MCF-7、MCF-7)的增殖,扑蛲灵能抑制乳腺癌干细胞(BCSCs)的自我更新,降低乳腺癌细胞系中 CD44+CD24-/low 和 ALDH 阳性 BCSCs 的含量。[1]对于 WNT 信号突变的结肠癌细胞,扑蛲灵以剂量依赖的方式阻止结肠癌细胞在体外生长,其抑制浓度(IC(50))差异很大,从 0.6 × 10(-6)到 65 × 10(-6)mol/L。[2]PyrPam 并不是 CK1 的真正激活剂,它对细胞信号通路的扰动是通过 Akt 磷酸化的下降启动的,进而促进了 GSK3 磷酸化和激活的降低。[3]扑蛲灵能抑制心脏成纤维细胞在葡萄糖缺乏条件下的存活。[5] In Vivo:在裸鼠体内注射 HCT116 细胞后扑蛲灵治疗降低肿瘤的生长。[2]在心肌梗塞小鼠模型中,扑蛲灵能减少疤痕形成,改善心脏收缩力。[5] 数据来源文献:[1]. Xu L,et al. WNT pathway inhibitor pyrvinium pamoate inhibits the self-renewal and metastasis of breast cancer stem cells. Int J Oncol. 2016 Mar;48(3):1175-86. [2]. Wiegering A,et al. The impact of pyrvinium pamoate on colon cancer cell viability. Int J Colorectal Dis. 2014 Oct;29(10):1189-98. [3]. Venerando A,et al. Pyrvinium pamoate does not activate protein kinase CK1,but promotes Akt/PKB down-regulation and GSK3 activation. Biochem J. 2013 May 15;452(1):131-7. [5]. Murakoshi M,et al. An anthelmintic drug,pyrvinium pamoate,thwarts fibrosis and ameliorates myocardial contractile dysfunction in a mouse model of myocardial infarction. PLoS One. 2013 Nov 4;8(11):e79374.
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| 其它标识: |
EC:EINECS 222-596-3 MDL:MFCD00010090 SMILES:CC1=CC(=C(N1C2=CC=CC=C2)C)C=CC3=[N+](C4=C(C=C3)C=C(C=C4)N(C)C)C.CC1=CC(=C(N1C2=CC=CC=C2)C)C=CC3=[N+](C4=C(C=C3)C=C(C=C4)N(C)C)C.C1=CC=C2C(=C1)C=C(C(=C2CC3=C(C(=CC4=CC=CC=C43)C(=O)O)[O-])[O-])C(=O)O InChIKey:OOPDAHSJBRZRPH-UHFFFAOYSA-L InChI:InChI=1S/2C26H28N3.C23H16O6/c2*1-19-17-21(20(2)29(19)24-9-7-6-8-10-24)11-13-23-14-12-22-18-25(27(3)4)15-16-26(22)28(23)5;24-20-16(14-7-3-1-5-12(14)9-18(20)22(26)27)11-17-15-8-4-2-6-13(15)10-19(21(17)25)23(28)29/h2*6-18H,1-5H3;1-10,24-25H,11H2,(H,26,27)(H,28,29)/q2*+1;/p-2 PubChem CID:54680693
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| 基本信息: |
CAS:3546-41-6 中文名称:扑蛲灵 英文名称:Pyrvinium pamoate 别名:Pyrvinium embonate;扑蛲灵 分子式:2C26H28N3·C23H14O6 分子量:1151.39 规格:10mg ; 50mg 溶解性:Soluble in DMSO(Need ultrasonic) 纯度:≥98% 外观(性状):Solid 储存条件:Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
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| 靶点: |
Parasite |