| Bioactivity | 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[1]. | ||||||||||||
| Target | organic anion transporter | ||||||||||||
| Invitro | 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[1].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[1].Morinidazole shows activity against Trichomonas vaginalis and Entamoeba histolytica in vitro, with MIC values of 2 μg/mL and 3 μg/mL, respectively[2]. | ||||||||||||
| In Vivo | 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[2].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[3].Pharmacokinetic parameters of Morinidazole in control and 5/6 nephrectomized (Nx) rats[3]Group | ||||||||||||
| Name | Morinidazole | ||||||||||||
| CAS | 92478-27-8 | ||||||||||||
| Formula | C11H18N4O4 | ||||||||||||
| Molar Mass | 270.29 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
Morinidazole
CAS: 92478-27-8 F: C11H18N4O4 W: 270.29
Morinidazole is an orally active and 5-nitroimidazole antimicrobial agent that undergoes extensive metabolism in humans
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