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• 产品描述： (R)-Morinidazole is an orally active and 5-nitroimidazole antimicrobial agent that undergoes extensive metabolism in humans via N+-glucuronidation and sulfation. (R)-Morinidazole can be used for bacterial infections research including appendicitis and pelvic inflammatory disease (PID) caused by anaerobic bacteria

• 靶点： organic anion transporter

• 体外研究：
  (R)-Morinidazole can be metabolized to N+-glucuronide of S-Morinidazole R enantiomer [M8-1] and N+-glucuronide of (R)-Morinidazole [M8-2] via N+-glucuronidation, and sulfate conjugate of (R)-Morinidazole [M7] via sulfation. M7 is a substrate for organic anion transporter 1 (OAT1) and OAT3 (Km=28.6 and 54.0 μM, respectively), M8-1 and M8-2 are the substrates for OAT3. (R)-Morinidazole shows activity against Trichomonas vaginalis and Entamoeba histolytica in vitro, with MIC values of 2 μg/mL and 3 μg/mL, respectively

• 体内研究：
  (R)-Morinidazole (20 mg/kg or 25 mg/kg; p.o.; single dose) inhibits Trichomonas vaginalis and Entamoeba histolytica in vivo in rats with EC50s of 20 mg/kg and 25 mg/kg, respectively. (R)-Morinidazole (50 mg/kg; i.v.; 0.25, 0.75, 1.5 h) shows a different concentration in tissues after intravenous injection, with a higher concentration in liver, kidney, plasma than lung, heart, and spleen in mice Animal Model: Renal failure model in SD rats (180-220 g) Dosage: 50 mg/kg Administration: Intravenous injection; sacrificed rats at 0.25, 0.75, and 1.50 hours after dose administration Result: Increased plasma exposures slightly compared with control.

• 参考文献：
  1. Zhong K, et al. Effects of renal impairment on the pharmacokinetics of morinidazole: uptake transporter-mediated renal clearanceof the conjugated metabolites. Antimicrob Agents Chemother. 2014 Jul;58(7):4153-61. 2. Kong F, et al. Increased Plasma Exposures of Conjugated Metabolites of Morinidazole in Renal Failure Patients: A Critical Role of Uremic Toxins. Drug Metab Dispos. 2017 Jun;45(6):593-603. 3. Lu Aifeng, et al. Application of α-(morpholine-1-yl)methyl-2-methyl-nitroimidazole-1-ethanol as anti-trichomonal agent and amebacide: China, CN1981764[P]. 2007-06-20.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.7 ml	18.499 ml	36.998 ml
  5 mM	0.74 ml	3.7 ml	7.4 ml
  10 mM	0.37 ml	1.85 ml	3.7 ml
  50 mM	0.074 ml	0.37 ml	0.74 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 *