Cyclofenil is a selective estrogen receptor modulator and an ovulation-inducing agent. Cyclofenil shows an inhibitory effect on dengue virus replication in Vero cells with an EC 50 of 1.62 μM. Cyclofenil has anti-dengue-virus activity.
性状
Solid
IC50 & Target[1][2]
Estrogen receptor; Dengue virus
体外研究(In Vitro)
Cyclofenil shows an inhibitory effect on dengue virus (DENV) replication in mammalian cells but not in mosquito cells. Cyclofenil also inhibits the replication of Zika virus. A time-of-addition assay suggested that Cyclofenil may interfere with two stages of the Dengue virus (DENV) life cycle: the translation-RNA synthesis and assembly-maturation stages. The level of intracellular infectious particles decreased more drastically after treatment with Cyclofenil than the viral RNA level do, indicating that the assembly-maturation stage might be the main target of Cyclofenil. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
The number of estrogen receptors α (ERα) and β (ERβ)-immunoreactive (-ir) cells is determined of each stage of the estrous cycle in intact rats. Additionally, the effects of blocking ERα and ERβ on ovulation rate on diestrus-2 or proestrus day through the microinjection of methyl-piperidino-pyrazole (MPP) or Cyclofenil in either side of preoptic-anterior hypothalamic area (POA-AHA) are evaluated. The number of ERα-ir and ERβ-ir cells in POA-AHA varied in each phase of estrous cycle. Either MPP or Cyclofenil in the right side of POA-AHA on diestrus-2 day reduced the ovulation rate, while at proestrus day it was decreased in rats treated in either side with MPP, and in those treated with Cyclofenil in the left side. MPP or Cyclofenil produced a decrease in the surge of luteinizing hormone levels (LH) and an increase in progesterone and follicle stimulating hormone (FSH).
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Tohma D, et al. An estrogen antagonist, cyclofenil, has anti-dengue-virus activity. Arch Virol. 2019 Jan;164(1):225-234.[2]. Arrieta-Cruz I, et al. Estrogen Receptors Alpha and Beta in POA-AHA Region Regulate Asymmetrically Ovulation. Cell Mol Neurobiol. 2019 Nov;39(8):1139-1149.
溶解度数据
In Vitro: DMSO : 100 mg/mL (274.39 mM; Need ultrasonic)配制储备液