Tilorone dihydrochloride

For research use only. Not for use in humans.

目录号:S5020 中文名称:盐酸替洛隆

Tilorone dihydrochloride Chemical Structure

CAS No. 27591-69-1

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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产品安全说明书

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。
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:

[3]

- 合并
  • Cell lines: PC3 prostate cancer cell lines
  • Concentrations: 0-20 μM
  • Incubation Time: 72 h
  • Method:

    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.


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: Sprague-Dawley rats
  • Dosages: 6.25-70 mg/kg
  • Administration: i.p.
    (Only for Reference)

溶解度 (25°C)

体外 Water 96 mg/mL (198.56 mM)
DMSO 43 mg/mL (88.94 mM)
Ethanol '96 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 483.47
化学式

C25H34N2O3.2HCl

CAS号 27591-69-1
储存条件 粉状
溶于溶剂
别名 N/A

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID