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• 产品描述： TMC353121 is a potent respiratory syncytial virus (RSV) fusion inhibitor with pEC50 of 9.9.

• 靶点： pEC50: 9.9 (RSV)

• 体内研究：
  After i.v. bolus administration of a single dose of 10 mg/kg to Sprague-Dawley rats, the plasma drug concentration-time profile of TMC353121 exhibits multicompartmental pharmacokinetics. Mean plasma drug concentrations decrease rapidly during the first hours after dosing and then more slowly, with a half-life of about 12 h, as determined for the last part of the curve between 8 and 24 h postdose. TMC353121 is rapidly eliminated from plasma (CL=8.6 liters/h/kg) and extensively distributed (Vss=55 liters/kg). TMC353121 is administered once, i.v. at 2.5 mg/kg or at 0.25 mg/kg. Drug levels are determined in lung tissue, serum, and BAL fluid at different time points. TMC353121 followed multicompartment pharmacokinetics, with a fast decay in serum within the first hour after i.v. injection, followed by a slower decay. The drug is eliminated quickly from the blood resulting in very low blood levels after 24 h. Lung concentrations are much higher than serum concentrations and in BAL fluid the drug is just above the limit of detection at 8 h after injection. Very low drug levels can still be detected in the lung 5 days after treatment

• 参考文献：
  1. Bonfanti JF, et al. Selection of a respiratory syncytial virus fusion inhibitor clinical candidate. 2. Discovery of a morpholinopropylaminobenzimidazole derivative (TMC353121). J Med Chem. 2008 Feb 28;51(4):875-96. 2. Rouan MC, et al. Pharmacokinetics-pharmacodynamics of a respiratory syncytial virus fusion inhibitor in the cotton rat model. Antimicrob Agents Chemother. 2010 Nov;54(11):4534-9. 3. Olszewska W, et al. Antiviral and lung protective activity of a novel respiratory syncytial virus fusion inhibitor in a mouse model. Eur Respir J. 2011 Aug;38(2):401-8.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.79 ml	8.949 ml	17.898 ml
  5 mM	0.358 ml	1.79 ml	3.58 ml
  10 mM	0.179 ml	0.895 ml	1.79 ml
  50 mM	0.036 ml	0.179 ml	0.358 ml

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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 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *