Tilorone dihydrochloride
中文名称：盐酸替洛隆
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。
Tilorone dihydrochloride Chemical Structure
CAS: 27591-69-1
产品质控
Tilorone dihydrochloride相关产品
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| 相关化合物库 | 激酶抑制剂库 FDA药物库 天然产物库 已知活性药物库-I 生物活性库Ⅱ | 点击展开 |
IFN抑制剂选择性比较
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。 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 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]. | |||
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| 细胞实验 | 细胞系 | PC3 prostate cancer cell lines | ||
| 浓度 | 0-20 μM | |||
| 孵育时间 | 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. |
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| 体内研究(In Vivo) | ||
| 体内研究活性 | 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]. | |
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| 动物实验 | Animal Models | Sprague-Dawley rats |
| Dosages | 6.25-70 mg/kg | |
| Administration | i.p. | |
化学信息&溶解度
| 分子量 | 483.47 | 分子式 | C25H34N2O3.2HCl |
| CAS号 | 27591-69-1 | SDF | -- |
| Smiles | CCN(CC)CCOC1=CC2=C(C=C1)C3=C(C2=O)C=C(C=C3)OCCN(CC)CC.Cl.Cl | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
Water : 96 mg/mL Ethanol : 96 mg/mL DMSO : 43 mg/mL ( (88.94 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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