Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fanotaprim 是二氢叶酸还原酶的有效抑制剂,抑制 tgDHFR (Toxoplasma gondiiDHFR) 和 hDHFR (human DHFR)的 IC50分别为 1.57 和 308 nM。Fanotaprim 在研究弓形虫病方面具有价值。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 818 | 现货 | ||
5 mg | ¥ 1,990 | 现货 | ||
10 mg | ¥ 3,160 | 现货 | ||
25 mg | ¥ 5,220 | 现货 | ||
50 mg | ¥ 7,380 | 现货 | ||
100 mg | ¥ 9,930 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,990 | 现货 |
产品描述 | Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor. Fanotaprim inhibits the growth of T. gondii strains with a TgDHFR IC50 of 1.57 ± 0.11 nM and a hDHFR IC50 of 308 ± 71 nM and a hDHFR to TgDHFR selectivity ratio of 196. |
靶点活性 | DHFR (human):308 ± 71 nM(human), TgDHFR:1.57 ± 0.11 nM(Toxoplasma gondii) |
体外活性 | Fanotaprim had a parasiticidal EC50 of 13 nM against the type I RH strain of T. gondii. In human MCF-7 cells, Fanotaprim had an EC50 value of 7300 nM. The selectivity of Fanotaprim in the cell-based assays is in line with its DHFR selectivity profiles of 200-fold[1]. |
体内活性 | Fanotaprim had moderate mouse liver microsome (MLM) intrinsic clearance (Clint) of 56.3 mL min–1 kg–1, which is 63% of mouse liver blood flow (LBF). Fanotaprim has low to moderate clearance of 10.6 mL min–1 kg–1, a volume of distribution of 1.14 L/kg, and a half-life of 3.9 h after a 1.0 mg/kg, iv dose. Oral bioavailability after a 0.83 mg/kg po dose was 47.3% with a Cmax of 178 ng/mL 30 min after dosing. The unbound fraction (%) in mouse plasma is 8.7 ± 0.2 and in brain homogenate 2.4 ± 0.3, determined using an equilibrium dialysis method. Fanotaprim was freely permeable into the mouse CNS at 0.5 h after a 10 mg/kg oral dose; the concentration in brain was 2560 ± 240 ng/g and in blood 1610 ± 580 ng/mL, giving a brain to blood ratio of 1.7 ± 0.6[1]. |
分子量 | 378.43 |
分子式 | C19H22N8O |
CAS No. | 2120282-75-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25 mg/mL (66.06 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6425 mL | 13.2125 mL | 26.425 mL | 66.0624 mL |
5 mM | 0.5285 mL | 2.6425 mL | 5.285 mL | 13.2125 mL | |
10 mM | 0.2642 mL | 1.3212 mL | 2.6425 mL | 6.6062 mL | |
20 mM | 0.1321 mL | 0.6606 mL | 1.3212 mL | 3.3031 mL | |
50 mM | 0.0528 mL | 0.2642 mL | 0.5285 mL | 1.3212 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。
Fanotaprim 2120282-75-7 Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism DHFR CD-1 Inhibitor mice VYR 006 VYR-006 inhibit Antifolate dhydrofolate reductase survival toxoplasmosis VYR006 inhibitor