Tilorone dihydrochloride

目录号：S5020 批次号：S502001

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化学数据

化学结构式 别名 N/A 储存条件
(自收到货起)		 3年 / -20°C / 粉状
1年 / -80°C / 溶于溶剂
化学式

C25H34N2O3.2HCl
分子量 483.47 CAS号 27591-69-1
Solubility (25°C)* 体外 Water 96 mg/mL (198.56 mM)
Ethanol 96 mg/mL (198.56 mM)
DMSO 43 mg/mL (88.94 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

产品描述 Tilorone dihydrochloride是一种广谱的、具有口服活性的抗病毒试剂，可激活干扰素的生成。它具有抗肿瘤和抗炎活性。
体外研究 Tilorone hydrochloride has cytotoxic activity in vitro against Walker carcinosarcoma 256, leukemia L5178Y, and the Novikoff hepatoma[1]. The antiviral activity of tilorone has been reported against a broad-spectrum array of viruses, including herpes simplex virus, influenza A and B virus, Venezuelan equine encephalitis virus, Mengo virus, Semliki Forest virus, vesicular stomatitis virus, and West Nile virus. Tilorone has been shown to possess a broad array of other biological activities, including cell growth inhibition in PC3 CDK5dn prostate cancer cells (IC50, 8 to 12 μM) and inhibition of primase DnaG from Bacillus anthracis (IC50,7.1 μM), and in a mouse model of pulmonary fibrosis it decreased lung hydroxyproline content and the expression of collagen genes. Other biologically important activities include α7 nicotinic receptor (nAChR) agonist activity (Ki, 56 nM) and activated human alpha7 nAChR with an EC50 of 2.5 μM, which is a target for various central nervous system diseases. Tilorone was also shown to have radioprotective activity, potent modulation of HIF-mediated gene expression in neurons with neuroprotective properties, induction of the accumulation of glycosaminoglycans, delayed infectious prion clearance, and prolonged prion disease incubation time[2]. Tilorone treatment resulted in decreased PC3 cell growth and invasion. It selectively targets PC3 cells with low CDK5 activity[3].
体内研究 Tilorone dihydrochloride has antitumor activity against Walker carcinosarcoma 256 and the reticulum cell sarcoma A-RCS in rodents. Tilorone hydrochloride was inactive when tested in several other rodent tumors including leukemias L 1210 and P388[1]. A series of in vitro ADMET (absorption, distribution, metabolism, excretion, toxicity) assays demonstrated the drug has excellent solubility, high Caco-2 permeability, was not a P-glycoprotein substrate, and had no inhibitory activity against five human CYP450 enzymes (3A4, 2D6, 2C19, 2C9, and 1A2). Tilorone was shown to have 52% human plasma protein binding with excellent plasma stability and a mouse liver microsome half-life of 48 min. Dose range-finding studies in mice demonstrated a maximum tolerated single dose of 100 mg/kg of body weight. A pharmacokinetics study in mice at 2- and 10-mg/kg dose levels showed that the drug is rapidly absorbed, has dose-dependent increases in maximum concentration of unbound drug in plasma and areas under the concentration-time curve, and has a half-life of approximately 18 h in both males and females, although the exposure was ∼2.5-fold higher in male mice[2].

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验 细胞系 PC3 prostate cancer cell lines
浓度 0-20 μM
处理时间 72 h
方法

One thousand PC3 cells were plated in 96-well plates containing 100 μl complete RPMI media. At circa 50% confluence, tilorone dihydrochloride was administered. For experiments the compound was diluted in complete RPMI media to obtain the desired final concentration. After treatment for 72 h (tilorone monotherapy), MTS reagent was added and absorption at 490 nm was determined.
动物实验 动物模型 Sprague-Dawley rats
剂量 6.25-70 mg/kg
给药处理 i.p.

特定的存储和包装每个产品的信息在产品说明书上都有注明。大多数Selleck产品，在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同，大多数建议储存在-20°C，抑制剂属于化学试剂，可在常温下运输储存两周左右。即使如此，我们保证产品的出货量将保持产品质量的条件下，一般都会放入冰袋。望阁下收到产品后，请按照产品数据表建议适当存储。

如果需要长期保存，请于零下二十度低温保存。禁止用于人体及治疗！

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