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Tilorone dihydrochloride
中文名稱：鹽酸替洛隆
Tilorone dihydrochloride是一種廣譜的、具有口服活性的抗病毒試劑，可激活干擾素的生成。它具有抗腫瘤和抗炎活性。
Tilorone dihydrochloride Chemical Structure
CAS: 27591-69-1
產(chǎn)品質(zhì)控
批次：
S502001
Water]96 mg/mL]false]Ethanol]96 mg/mL]false]DMSO]43 mg/mL]false
純度：
99.96%
99.96
Tilorone dihydrochloride相關(guān)產(chǎn)品
| 相關(guān)產(chǎn)品 | Aloe-emodin Anti-mouse IFNAR-1-InVivo KIN1148 | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)化合物庫 | 激酶抑制劑庫 FDA藥物庫 天然產(chǎn)物庫 已知活性藥物庫-I 高選擇性抑制劑庫 | 點(diǎn)擊展開 |
生物活性
| 產(chǎn)品描述 | Tilorone dihydrochloride是一種廣譜的、具有口服活性的抗病毒試劑，可激活干擾素的生成。它具有抗腫瘤和抗炎活性。 |
|---|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | 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]. | |||
|---|---|---|---|---|
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | PC3 prostate cancer cell lines | ||
| 濃度 | 0-20 μM | |||
| 孵育時間 | 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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| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)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]. | |
|---|---|---|
| 動物實(shí)驗(yàn) | Animal Models | Sprague-Dawley rats |
| Dosages | 6.25-70 mg/kg | |
| Administration | i.p. | |
化學(xué)信息&溶解度
| 分子量 | 483.47 | 分子式 | C25H34N2O3.2HCl |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
Water : 96 mg/mL (198.56 mM) Ethanol : 96 mg/mL (198.56 mM) DMSO : 43 mg/mL ( (88.94 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) |
摩爾濃度計算器 |
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體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實(shí)驗(yàn)計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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