niclosamide

Niclosamide (Niclocide) 是一种口服生物可利用的氯化水杨酰苯胺。它通过抑制 DNA 复制，具有驱虫和潜在的抗肿瘤活性。

Niclosamide olamine (Niclosamide Ethanolamine salt) 是一种驱虫剂，可破坏寄生虫和动物模型中的线粒体代谢。它可逆地抑制雷帕霉素复合物的哺乳动物靶标，从而抑制STAT3(IC50为 0.25 μM) 并刺激自噬反应。

Niclosamide Monohydrate is used for the treatment of most tapeworm infections by inhibiting DNA replication.

Niclosamide (BAY2353) sodium 为用于研究寄生虫感染的口服抗蠕虫化合物，同时是STAT3抑制剂，在HeLa细胞中IC50为0.25μM。此化合物显示抗癌生物活性，并可抑制Vero E6细胞DNA复制。

SARS-CoV-2-IN-14 是一种有效的、可口服的 SARS-CoV-2 抑制剂（IC50 ：0.39 μM），是一种氯硝柳胺类似物。SARS-CoV-2-IN-14在人血浆和肝 S9 酶测定中比氯硝柳胺稳定性更强。SARS-CoV-2-IN-14以口服的方式给药可以提高其生物利用度和半衰期。

TFM is a piscicide.1It is toxic to sea lamprey (P. marinus) with LC50values ranging from 1.97 to 2.11 and 2.05 to 2.21 mg/L for sac and swim-up fry, respectively, 1.6 to 2.45 mg/L for juveniles, and 1.6 to 1.63 mg/L for adults. It is also toxic to juvenile lake sturgeon (A. fulvescens) less than 100 mm in size but not to a variety of other fish species. TFM (50 μM) uncouples oxidative phosphorylation by 22 and 28% in isolated sea lamprey and rainbow trout (O. mykiss) liver, respectively.2Formulations containing TFM have been used as lampricides in the control of larval sea lamprey populations. 1.Boogaard, M.A., Bills, T.D., and Johnson, D.A.Acute toxicity of TFM and a TFM/niclosamide mixture to selected species of fish, including lake sturgeon (Acipenser fulvescens) and mudpuppies (Necturus maculosus), in laboratory and field exposuresJ. Great Lakes Res.29(Suppl 1)529-541(2003) 2.Birceanu, O., McClelland, G.B., Wang, Y.S., et al.The lampricide 3-trifluoromethyl-4-nitrophenol (TFM) uncouples mitochondrial oxidative phosphorylation in both sea lamprey (Petromyzon marinus) and TFM-tolerant rainbow trout (Oncorhynchus mykiss)Comp. Biochem. Physiol. C. Toxicol. Pharmacol.153(3)342-349(2011)

SARS-CoV-2-IN-15 (compound 11) 是一种氯硝柳胺类似物，其在人血浆和肝 S9 酶测定中比氯硝柳胺具有更高的稳定性。当口服给药时，它可以提高生物利用度和半衰期。SARS-CoV-2-IN-15 是SARS-CoV-2的有效抑制剂，IC50值为 0.49 μM。

SARS-CoV-2-IN-13 (compound 6) 是氯硝柳胺的类似物。在人血浆和肝S9酶测定中，SARS-CoV-2-IN-13 比氯硝柳胺更稳定。SARS-CoV-2-IN-13 口服给药时可以提高生物利用度和半衰期。SARS-CoV-2-IN-13 是SARS-CoV-2的有效抑制剂，IC50值为 0.057 μM。

JMX0312 is a salicylamide derivative used as a potent inhibitor of HAdV infection. JMX0312 showed significantly improved anti-HAdV activities with nanomolar to submicromolar IC50 values and high selectivity indexes (SI > 100), indicating better safety windows, compared to those of the lead compound niclosamide.