基本信息
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产品编号：R10220 |
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产品名称：RD3-0028 |
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CAS: |
3886-39-3 |
储存条件 |
粉末 |
-20℃ |
三年 |
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分子式： |
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分子量 |
168.28 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
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Ethanol |
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Water |
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体内 |
现配现用 |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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生物活性
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产品描述 |
一种有效的，口服生物可利用的Akt抑制剂，对Akt1，Akt2，和 Akt3 的Ki分别为 0.08nM，2nM，和 2.6nM。Phase 2。 |
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靶点/IC50 |
RSV EC50: 4.5μM |
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体外研究 |
RD3-0028 has a 50% effective concentration of 4.5μM and a 50% cytotoxic concentration of 271.0μM which is superior to that of ribavirin. RD3-0028 inhibits different RSV strains at a low concentration (4.5-11.0μM) using the MTT method. Using the MTT method, EC50 values of RD3-0028 against tested strains are lower than those of ribavirin. RD3-0028 does not inhibit the replication of measles virus, influenza A virus, herpes simplex virus types 1 and 2, or human cytomegalovirus. |
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体内研究 |
Aerosols generated from reservoirs containing RD3-0028 (7mg/mL) administered for 2 h twice daily for 3 days significantly reduces the pulmonary titer of RSV-infected mice. It is clear that the minimal effective dose of RD3-0028 for RSV-infected mice is significantly less than that of ribavirin, the only compound currently available for use against RSV disease.Furthermore, the RD3-0028 aerosol administration protect the lungs of infected, CYP-treated mice against tissue damage, as evidenced by the preservation of the lung architecture and a reduction in pulmonary inflammatory infiltrates. RD3-0028 aerosol is not toxic for mice at the therapeutic dose. The plasma concentration of RD3-0028 is maintained at the same level from 5 min to 1 h, and decreases with a half-life of 2.2 h for 1±8 h. The excretion of radioactivity in the urine and faeces at 24 h after aerosol treatment is 89.3 and 4.5%, respectively, indicating that almost all the radioactivity is rapidly excreted in the urine. The excretion of total radioactivity is 98.9% within 168h. |
推荐实验方法(仅供参考)
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细胞实验: |
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Cell Assay |
50mL of HeLa cell suspensions (30000 cells/well) and the Long strain of RSV(25 TCID50/well) in MEM supplemented with 0.1% bovine serum albumin and antibiotics are added to each well in a 96-well round-bottomed microtiter plate that is filled with 50mL of MM in the presence or absence of several concentrations of RD3-0028. The anti-RSV assay is performed primarily with the MTT method. |
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动物实验: |
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Animal Administration |
Mouse: Aerosols are generated from reservoirs containing 0.3 to 7.0mg of RD3-0028 per mL. Solutions of ribavirin are prepared in saline containing 2.5 to 60mg/mL. Mice are treated intraperitoneally with 100mg of cyclophosphamide per kg of body weight 5 days before virus inoculation. The mice are weighed, anesthetized with sodium pentobarbital (50mg/kg),and inoculated intranasally with approximately 105 PFU of RSV A2 in 50mL (day 0). From day 1 through day 3, the mice are exposed to the RD3-0028 or ribavirin aerosol. Placebo consisted of 10% DMSO-saline containing 1% Tween 80. On day 4, the day on which untreated mice had the maximum RSV pulmonary titer, all animals are killed and the lungs of each mouse are removed and for virus quantification. Rat: 14C-RD3-0028 is dissolved in 10% dimethyl sulphoxide (DMSO)/saline containing 1% Tween 80 for administration by the aerosol route. The aerosol is generated using a head-exposure chamber, mono-position, with a mist generator. The mass median aerodynamic diameter of the aerosol particle is 2.1mm. Rats are exposed to the 14C-RD3-0028 aerosol for 15min and killed at indicated times after the end of exposure. Because the aerosol treatment with 14C-RD3-0028 exposed the rat to 8.8 mg (91.5kBq)/animal, the solution of this compound is orally administered at a dose of 8.8 mg/body. |
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 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
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 )
