产品
编 号：F522413
分子式：C11H18N4O4
分子量：270.29
分子式：C11H18N4O4
分子量：270.29
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
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5mg
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10mg
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结构图
CAS No: 92478-27-8
产品详情
生物活性：
Morinidazole is an orally active and 5-nitroimidazole antimicrobial agent that undergoes extensive metabolism in humans via N+-glucuronidation and sulfation. Morinidazole can be used for bacterial infections research including appendicitis and pelvic inflammatory disease (PID) caused by anaerobic bacteria.
体内研究：
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.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.Pharmacokinetic parameters of Morinidazole in control and 5/6 nephrectomized (Nx) ratsGroupCmax (μg/mL)Tmax (h)T1/2 (h)AUC0-t (μg·h/mL)AUC0-∞ (μg·h/mL)CL (mL/h/kg)Vss (mL/kg)MRT (h)
Control rats48.20.081.1687.287.35828051.39
5/6 Nx rats53.20.081.3291.291.35528911.62
Intravenous injection; 50 mg/kg Morinidazole; Blood samples were collected from retro-orbital venous plexus before the dose (0 hours), at 5, 15, and 30 minutes, and at 1, 2, 4, 6, 8, and 12 hours after the dose.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.
体外研究：
Morinidazole can be metabolized to N+-glucuronide of S-morinidazole [M8-1] and N+-glucuronide of R-morinidazole [M8-2] via N+-glucuronidation, and sulfate conjugate of 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.Morinidazole shows activity against Trichomonas vaginalis and Entamoeba histolytica in vitro, with MIC values of 2 μg/mL and 3 μg/mL, respectively.
Morinidazole is an orally active and 5-nitroimidazole antimicrobial agent that undergoes extensive metabolism in humans via N+-glucuronidation and sulfation. Morinidazole can be used for bacterial infections research including appendicitis and pelvic inflammatory disease (PID) caused by anaerobic bacteria.
体内研究：
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.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.Pharmacokinetic parameters of Morinidazole in control and 5/6 nephrectomized (Nx) ratsGroupCmax (μg/mL)Tmax (h)T1/2 (h)AUC0-t (μg·h/mL)AUC0-∞ (μg·h/mL)CL (mL/h/kg)Vss (mL/kg)MRT (h)
Control rats48.20.081.1687.287.35828051.39
5/6 Nx rats53.20.081.3291.291.35528911.62
Intravenous injection; 50 mg/kg Morinidazole; Blood samples were collected from retro-orbital venous plexus before the dose (0 hours), at 5, 15, and 30 minutes, and at 1, 2, 4, 6, 8, and 12 hours after the dose.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.
体外研究：
Morinidazole can be metabolized to N+-glucuronide of S-morinidazole [M8-1] and N+-glucuronide of R-morinidazole [M8-2] via N+-glucuronidation, and sulfate conjugate of 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.Morinidazole shows activity against Trichomonas vaginalis and Entamoeba histolytica in vitro, with MIC values of 2 μg/mL and 3 μg/mL, respectively.
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