Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GS-9191是一种DNA 聚合酶α和ß 的强效抑制剂 ,是一种新型核苷类似物9-(2-膦酰甲氧基乙基)鸟嘌呤(PMEG)的原药 ,可渗透皮肤并在上皮层代谢为活性核苷三磷酸类似物。GS-9191具有抗增殖活性,以剂量相关的方式减少乳头瘤的大小。GS-9191可能对治疗HPV 引起的病变有作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,260 | 现货 | ||
5 mg | ¥ 3,120 | 现货 | ||
10 mg | ¥ 4,570 | 现货 | ||
25 mg | ¥ 7,270 | 现货 | ||
50 mg | ¥ 9,780 | 现货 | ||
100 mg | ¥ 13,200 | 现货 | ||
500 mg | ¥ 26,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 4,420 | 现货 |
产品描述 | GS-9191 is a potent inhibitor of DNA polymerase alpha and ß , a prodrug of the novel nucleoside analogue 9-(2-phosphonomethoxyethyl)guanine (PMEG) , which penetrates the skin and is metabolized in the epithelium to an active nucleoside triphosphate analogue.GS-9191 has antiproliferative activity and reduces the size of papillomas in a dose-related manner.GS-9191 may be useful in the treatment of HPV-induced lesions. |
靶点活性 | HPV-positive cell lines:0.03 nM(EC50), Non-HPV-infected cells:1-15 nM(EC50) |
体外活性 |
GS-9191 was markedly more potent than PMEG or cPrPMEDAP in a series of human papillomavirus (HPV)-positive cell lines, with effective concentrations to inhibit 50% cell growth (EC(50)) as low as 0.03, 207, and 284 nM, respectively. In contrast, GS-9191 was generally less potent in non-HPV-infected cells and primary cells (EC(50)s between 1 and 15 nM). DNA synthesis was inhibited by GS-9191 within 24 h of treatment; cells were observed to be arrested in S phase by 48 h and to subsequently undergo apoptosis (between 3 and 7 days).[2] In an animal model (cottontail rabbit papillomavirus), topical GS-9191 was shown to decrease the size of papillomas in a dose-related manner. At the highest dose (0.1%), cures were evident at the end of 5 weeks, and lesions did not recur in a 30-day follow-up period. These data suggest that GS-9191 may have utility in the treatment of HPV-induced lesions.[2] |
别名 | GS 9191 |
分子量 | 734.82 |
分子式 | C37H51N8O6P |
CAS No. | 859209-84-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 7.35 mg/mL (10 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.3609 mL | 6.8044 mL | 13.6088 mL | 34.0219 mL |
5 mM | 0.2722 mL | 1.3609 mL | 2.7218 mL | 6.8044 mL | |
10 mM | 0.1361 mL | 0.6804 mL | 1.3609 mL | 3.4022 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GS-9191 859209-84-0 Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis GS 9191 GS9191 Inhibitor inhibitor inhibit