产品
编 号:F338695
分子式:C72H66N8O12S4
分子量:1363.6
产品类型
结构图
CAS No: 36951-72-1
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产品详情
生物活性:
TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand. TMPyP4 tosylate inhibits the interaction between G-quadruplexes and IGF-1. TMPyP4 tosylate is a telomerase inhibitor and inhibits cancer cells proliferation. TMPyP4 tosylate is also a stabilizer of nucleic acid secondary structure and an acetylcholinesterase inhibitor. Besides, TMPyP4 tosylate has antiviral activity against SARS-CoV-2.
体内研究:
TMPyP4 tosylate (10 和 20 mg/kg,i.p.,每周两次) 抑制 MX-1 肿瘤模型中的肿瘤生长。TMPyP4 tosylate (15mg/kg 或 30mg/kg,i.n.) 降低感染 SARS-CoV-2 的仓鼠的平均病毒载量。TMPyP4 tosylate (30mg/kg,i.n.,仓鼠) 在给药后 1 h 达到最高浓度,Cmax 为 17.88 μg/mL,半衰期 (T1/2) 6.36 h.Animal Model:MX-1 mammary chemoadjuvant model
Dosage:10 and 20 mg/kg
Administration:Intraperitoneal injection (i.p.), twice weekly.
Result:Inhibited tumor growth and prolonged mice survival.
Animal Model:SARS-CoV-2-infected hamster
Dosage:15?mg/kg or 30?mg/kg
Administration:i.n., starting at 1?h prior to virus inoculation and continuing until 3 days post infection
Result:Decreased the mean viral loads in the nasal wash, nasal turbinate and lung tissues.
体外研究:
TMPyP4 tosylate (50μM, 96 h) 抑制端粒酶阳性 HOS 细胞中的端粒酶活性.TMPyP4 tosylate (50μM, 48 或 96 h) 抑制 HOS 细胞的生长.TMPyP4 tosylate (50μM, 96 h) 在 HOS、Saos-2、MG-63 和 U2OS 细胞系中诱导细胞凋亡。TMPyP4 tosylate (100μM,24 或 48 h) 增加 K562 细胞中的细胞周期调节蛋白和 MAPK 含量。