基本信息
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产品编号：O10184 |
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产品名称：Osalmid |
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CAS: |
526-18-1 |
储存条件 |
粉末 |
2-8℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
229.23 |
-20℃ |
一个月 |
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化学名： |
1-METHYL-3,4-DIHYDROSPIRO[CHROMENE-2,4-PIPERIDIN]-4-AMINEHYDROCHLORIDE |
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Solubility (25°C) |
体外 |
DMSO |
≥100mg/mL (436.24mM) |
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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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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
4.3624mL |
21.8122mL |
43.6243mL |
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5mM |
0.8725mL |
4.3624mL |
8.7249mL |
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10mM |
0.4362mL |
2.1812mL |
4.3624mL |
生物活性
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产品描述 |
核糖核苷酸还原酶小亚基M2的靶向化合物；抑制核糖核苷酸还原酶活性的IC50值为8.23 μM。 |
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靶点/IC50 |
(ribonucleotide reductase) IC50: 8.23μM |
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体外研究 |
Osalmid is identified as a potential ribonucleotide reductase small subunit M2 (RRM2) compound. Osalmid is 10-fold more active in inhibiting ribonucleotide reductase (RR) activity than hydroxyurea, and significantly inhibits HBV DNA and cccDNA synthesis in HepG2.2.15 cells in a time- and dose-dependent manner. After treatment for 8 days with Osalmid, the EC50 for HBV DNA inhibition are 11.1μM for culture supernatant and 16.5μM for cells. Osalmid suppresses RR activity in a concentration-dependent manner, with an IC50 of 8.23μM. Osalmid is shown to possess potent activity against a 3TCresistant HBV strain, suggesting utility in treating drug-resistant HBV infections. |
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体内研究 |
Osalmid reduces RR activity and HBV replication in HBV-transgenic mice and shows a synergistic efficacy with 3TC without significant toxicity. Oral dosing of osalmid at 400mg/kg/d results in a time-dependent inhibition of HBV DNA replication. After treatment for 4 weeks, osalmid suppresses HBV DNA replication by about 40-45% as compared to the control in mouse sera and liver tissues. |
推荐实验方法(仅供参考)
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细胞实验: |
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Cell Assay |
HepG2.2.15 cells are cultured in the presence of 200μg/mL G418. Cell viability is determined using a Cell Counting Kit-8 in 96-well plates treated with Osalmid for designated times. For long term assays, the culture supernatants are replaced with fresh media containing Osalmid every two days. The control wells contained equivalent amounts of DMSO. The CC50 is calculated as the concentration of a compound that reduced the cell viability to 50% compared to the control. |
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动物实验: |
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Animal Administration |
Mice: The HBV-transgenic mouse lineage is initially produced on a BALB/c background. Osalmid or 3TC is suspended in 0.05% CMC-Na and administered once a day by gavage at 400 and 100mg/kg, respectively, for 28 days. For the combination group, mice are intragastrically administered with a mixture of osalmid and 3TC. 0.05% CMC-Na solution is used as control.The mouse sera are collected and assayed for HBV DNA levels and AST/ALT activity. Mice are then sacrificed after the 28-day drug treatment and the livers are excised for analysis. |
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 )
