Morinidazole 吗啉硝唑,98.05%

产品编号:Bellancom-15781| CAS NO:92478-27-8| 分子式:C11H18N4O4| 分子量:270.29

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-15781
3500.00 杭州 北京(现货)
Bellancom-15781
5000.00 杭州 北京(现货)

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Morinidazole 吗啉硝唑

产品介绍 Morinidazole 是一种口服有效的 5-硝基咪唑抗菌剂,在人体中通过 N+-葡萄糖醛酸化和磺化进行代谢。Morinidazole 可用于用于研究细菌感染,包括厌氧菌引起的阑尾炎、盆腔炎 (PID) 等。
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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) rats

Group Cmax (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 rats 48.2 0.08 1.16 87.2 87.3 582 805 1.39
5/6 Nx rats 53.2 0.08 1.32 91.2 91.3 552 891 1.62
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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) rats

Group Cmax (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 rats 48.2 0.08 1.16 87.2 87.3 582 805 1.39
5/6 Nx rats 53.2 0.08 1.32 91.2 91.3 552 891 1.62
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
性状Solid
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (369.97 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6997 mL 18.4986 mL 36.9973 mL
5 mM 0.7399 mL 3.6997 mL 7.3995 mL
10 mM 0.3700 mL 1.8499 mL 3.6997 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (10.17 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (10.17 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.75 mg/mL (10.17 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (10.17 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.75 mg/mL (10.17 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (10.17 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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