Nizatidine(Synonyms: 尼扎替丁)

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Nizatidine (Synonyms: 尼扎替丁) 纯度: 99.19%

Nizatidine 是一种口服有效的组胺 H2 受体 (histamine H2 receptor) 拮抗剂,可用于胃溃疡的研究。在动物实验中,Nizatidine 的作用是减少胃酸的含量,并防止溃疡愈合后的复发。

Nizatidine(Synonyms: 尼扎替丁)

Nizatidine Chemical Structure

CAS No. : 76963-41-2

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10 mM * 1 mL in DMSO ¥500 In-stock
100 mg ¥350 In-stock
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生物活性

Nizatidine is a potent and orally active histamine H2 receptor antagonist, can be used for the research of stomach and intestines ulcers. Nizatidine works by decreasing the secretion of gastric acid the stomach makes and prevent ulcers from coming back after they have healed in animal models[1].

IC50 & Target[2]

H2 Receptor

 

体内研究
(In Vivo)

Nizatidine (oral gavage; 27 mg/kg; once daily; at 12 weeks of age and were sacrificed at 30 weeks after development of HCC in the setting of nonalcoholic steatohepatitis (NASH)) results in a 35% reduction of tumor nodules relative to controls. Nizatidine results in a 60% reduction in tumor nodules, reduces collagen proportional area and expression of profibrotic markers in DEN-injured rats[2].
Nizatidine (oral gavage; 27 mg/kg; once daily; 4 weeks) decreases the incidence of gastric ulceration, and significantly decreases the mean ulcer score and ulcer index in male albino rats[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male albino rats[3]
Dosage: 27 mg/kg
Administration: Oral gavage; 27 mg/kg; once daily; 4 weeks
Result: Was effective in the management of NSAIDs induced peptic ulcer in rats.

Clinical Trial

分子量

331.46

Formula

C12H21N5O2S2

CAS 号

76963-41-2

中文名称

尼扎替丁;尼沙替丁; 尼扎替定

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
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (150.85 mM)

H2O : 20 mg/mL (60.34 mM; Need ultrasonic)

* “≥” 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 3.0170 mL 15.0848 mL 30.1696 mL
5 mM 0.6034 mL 3.0170 mL 6.0339 mL
10 mM 0.3017 mL 1.5085 mL 3.0170 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: PBS

    Solubility: 50 mg/mL (150.85 mM); Clear solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 3.5 mg/mL (10.56 mM); Clear solution

    此方案可获得 ≥ 3.5 mg/mL (10.56 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 35.0 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

  • 3.

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

    Solubility: ≥ 3.5 mg/mL (10.56 mM); Clear solution

    此方案可获得 ≥ 3.5 mg/mL (10.56 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 35.0 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
  • 4.

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

    Solubility: ≥ 3.5 mg/mL (10.56 mM); Clear solution

    此方案可获得 ≥ 3.5 mg/mL (10.56 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 35.0 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. T M Lin, et al. Actions of nizatidine, a selective histamine H2-receptor antagonist, on gastric acid secretion in dogs, rats and frogs. J Pharmacol Exp Ther. 1986 Nov;239(2):406-10.

    [2]. Shen Li, et al. Abstract 4004: The H2 receptor antagonist nizatidine inhibits carcinogenesis in two rodent models of hepatocellular carcinoma. Tumor Biology. Cancer research.

    [3]. Ahmed S. Alazzouni, et al. Comparative histological and histochemical studies between ranitidine and nizatidine in treatment of peptic ulcer with evaluation of their adverse effects on male sex hormones. The Journal of Basic and Applied Zoology volume

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