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Esomeprazole sodium/埃索美拉唑钠 {[allProObj[0].p_purity_real_show]}

货号:A188600 同义名: (S)-Omeprazole sodium; (-)-Omeprazole sodium

Esomeprazole sodium是一种有效的质子泵抑制剂,通过抑制 H+, K+-ATPase 减少胃酸分泌,用于胃食管反流疾病研究。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
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Esomeprazole sodium/埃索美拉唑钠 化学结构 CAS号:161796-78-7
Esomeprazole sodium/埃索美拉唑钠 化学结构
CAS号:161796-78-7
Esomeprazole sodium/埃索美拉唑钠 3D分子结构
CAS号:161796-78-7
Esomeprazole sodium/埃索美拉唑钠 化学结构 CAS号:161796-78-7
Esomeprazole sodium/埃索美拉唑钠 3D分子结构 CAS号:161796-78-7
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Esomeprazole sodium/埃索美拉唑钠 纯度/质量文件 产品仅供科研

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产品名称 ATPase 其他靶点 纯度
(-)-Blebbistatin 99%+
PF 03716556 ++++

H+/K+-ATPase, pIC50: ~6.5

99%
Esomeprazole sodium 98%
BTB06584 99%
Ciclopirox 97%
CB-5083 ++++

p97 AAA ATPase, IC50: 11 nM

99%+
Ciclopirox olamine 99%
Brefeldin A +++

ATPase (HCT 116), IC50: 0.2 μM

99%+
Oligomycin A 99%
Sodium orthovanadate +++

(Na,K)-ATPase, IC50: 40 nM

25-28%V
Golgicide A 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Proton Pump 其他靶点 纯度
Zinc pyrithione 98+%
PF 03716556 ++++

H+/K+-ATPase, pIC50: ~6.5

99%
Lansoprazole 98%
Esomeprazole Magnesium 98%+
Rabeprazole 99%+
Ilaprazole TOPK 97%
Bafilomycin A1 ++++

H+-ATPase, IC50: 0.44 nM

99%
Pantoprazole sodium 98%
(R)-Lansoprazole 98%
Tenatoprazole 99%+
Omeprazole 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Esomeprazole sodium/埃索美拉唑钠 生物活性

靶点
  • ATPase

描述 Esomeprazole sodium ((S)-Omeprazole sodium) is a powerful and orally active inhibitor of the proton pump, decreasing acid production by targeting the H+, K+-ATPase in the gastric parietal cells. Furthermore, Esomeprazole sodium impedes exosome release by inhibiting V-H+-ATPases, acting as an exosome inhibitor[4]. Esomeprazole is noted for its research potential in addressing symptomatic gastroesophageal reflux disease[1].[2].[3].
体内研究

Administering Esomeprazole (30-300 mg/kg; orally via gavage; daily; for 19 or 11 days; in C57BL/6J mice) significantly curbs the advancement of fibrosis in the lungs of these animals and diminishes circulating indicators of inflammation and fibrosis[2].

体外研究

In vitro, Esomeprazole (25-100 µM; for 20 hours; MDA-MB-468 cells) administration curtails the growth of triple-negative breast cancer cells in a concentration-dependent manner, attributed to an increase in intracellular acidification[1].

Esomeprazole sodium/埃索美拉唑钠 细胞实验

Cell Line
Concentration Treated Time Description References
Jurkat cells 5 μM 72 h Inhibit H+-ATPase activity and regulate intracellular pH Immunity. 2023 Dec 12;56(12):2682-2698.e9.
Het-1A cells 30 µM 6 h To evaluate the effect of Esomeprazole on HCl-induced inflammatory responses. Results showed that Esomeprazole significantly inhibited the HCl-induced elevation of pro-inflammatory cytokines (IL-6, IL-8, IL-1β, TNF-α). Front Immunol. 2024 Dec 16;15:1410904.
Human cord blood-derived mast cells 50μM 2 h To evaluate the effect of omeprazole on human mast cell degranulation and cytokine secretion. Results showed that omeprazole significantly inhibited LAMP-1 expression and histamine release. J Allergy Clin Immunol. 2020 Oct;146(4):884-893.e5.
Bone marrow-derived mast cells 50μM 2 h To evaluate the effect of omeprazole on IgE-mediated mast cell degranulation and cytokine secretion. Results showed that omeprazole significantly inhibited LAMP-1 expression and histamine release. J Allergy Clin Immunol. 2020 Oct;146(4):884-893.e5.
IPF lung fibroblasts 100 μM 24 h To evaluate the effect of esomeprazole combined with pirfenidone on TGFβ-induced collagen production. Results showed that the combination therapy significantly suppressed collagen production. Sci Rep. 2022 Nov 30;12(1):20668.
IPF lung fibroblasts 100 μM 48 h To evaluate the effect of esomeprazole combined with pirfenidone on TGFβ-induced collagen gel contraction. Results showed that the combination therapy effectively inhibited collagen gel contraction. Sci Rep. 2022 Nov 30;12(1):20668.
IPF lung fibroblasts 100 μM 72 h To evaluate the effect of esomeprazole combined with pirfenidone on TGFβ-induced cell migration. Results showed that the combination therapy was more effective in inhibiting cell migration than monotherapy. Sci Rep. 2022 Nov 30;12(1):20668.
IPF lung fibroblasts 100 μM 24 h To evaluate the effect of esomeprazole combined with pirfenidone on TGFβ-induced cell proliferation. Results showed that esomeprazole significantly enhanced the anti-proliferative effect of pirfenidone. Sci Rep. 2022 Nov 30;12(1):20668.
Human esophageal adenocarcinoma cell line OE19 50 μM, 200 μM, 350 μM 72 h To evaluate the effect of esomeprazole on OE19 cell survival, showing dose-dependent inhibition of cell survival J Exp Clin Cancer Res. 2014 Sep 1;33(1):73.
Human esophageal squamous cell carcinoma cell line KYSE410 50 μM, 250 μM, 350 μM 72 h To evaluate the effect of esomeprazole on KYSE410 cell survival, showing dose-dependent inhibition of cell survival J Exp Clin Cancer Res. 2014 Sep 1;33(1):73.

Esomeprazole sodium/埃索美拉唑钠 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Intragastric administration model Intragastric administration 50 pellets Single dose, lasting 2 hours Observe the structural changes of esomeprazole magnesium enteric-coated pellets in the stomach. Results showed that the retention rate of pellets in the stomach after 2 hours was 38.97%, and the sphericity, pellet volume, pore volume, and porosity were 0.47, 1.55×10^8 mm3, 0.44×10^8 mm3, and 27.6%, respectively. Acta Pharm Sin B. 2022 Jan;12(1):326-338
BALB/c mice Whole-brain irradiation injury model Intraperitoneal injection 10 mg/kg Once daily for 8 weeks Inhibited AEP’s enzymatic activity and alleviated radiation-induced brain injury iScience. 2024 Apr 9;27(5):109698
Mice Radiation-induced brain injury model Intraperitoneal injection 10 mg/kg Once daily for 8 weeks Inhibited the enzymatic activity of AEP and alleviated radiation-induced brain injury iScience. 2024 Apr 9;27(5):109698
BALB/c mice Passive systemic anaphylaxis model Intraperitoneal injection 1.6mg/0.2mL 4 consecutive days To evaluate the effect of esomeprazole on IgE-mediated systemic anaphylaxis. Results showed that esomeprazole significantly reduced the drop in core body temperature and release of MCPT-1 and histamine. J Allergy Clin Immunol. 2020 Oct;146(4):884-893.e5.
C57BL/6J mice TGFβ-induced lung fibrosis model Oral gavage 30 mg/kg Daily administration for 28 days To evaluate the effect of esomeprazole combined with pirfenidone on TGFβ-induced lung fibrosis. Results showed that the combination therapy was more effective in suppressing lung fibrosis and αSMA expression than monotherapy. Sci Rep. 2022 Nov 30;12(1):20668.
Mice Clostridioides difficile infection model Oral gavage 40 mg/kg Five times per 12 h interval Used to induce Clostridioides difficile infection model, results showed Esomeprazole pretreatment increased infection risk. Bioeng Transl Med. 2023 Sep 5;8(6):e10593
Mice B16-F10 melanoma model Intraperitoneal injection 12.5 mg/kg Every other day for a total of 6 injections Neutralize tumor microenvironment acidic pH and improve T cell function Immunity. 2023 Dec 12;56(12):2682-2698.e9.
Mice Autism spectrum disorder model Oral 50 mg/kg 4 weeks To investigate the effects of p-Cresol on ASD-like behaviors in mice, results showed p-Cresol induced social behavior deficits and stereotypies Microbiome. 2021 Jul 8;9(1):157

Esomeprazole sodium/埃索美拉唑钠 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03383003 Helicobacter Pylori Infection Not Applicable Completed - Taiwan ... 展开 >> Wei-Chen Tai Kaohsiung, Taiwan, 833 收起 <<
NCT02711176 Helicobacter Infection Phase 4 Completed - Iran, Islamic Republic of ... 展开 >> Ilam University of Medical Scienvc Ilam, Iran, Islamic Republic of, 6939177143 收起 <<
NCT03444402 GERD Phase 1 Completed - Korea, Republic of ... 展开 >> Seoul University Hospital Seoul, Korea, Republic of 收起 <<

Esomeprazole sodium/埃索美拉唑钠 参考文献

[1]Wayne Goh, et al. Use of proton pump inhibitors as adjunct treatment for triple-negative breast cancers. An introductory study. J Pharm Pharm Sci. 2014;17(3):439-46.

[2]Christina Nelson, et al. Therapeutic Efficacy of Esomeprazole in Cotton Smoke-Induced Lung Injury Model. Front Pharmacol. 2017 Jan 26;8:16.

[3]Thomas J Johnson, et al. Esomeprazole: a clinical review. Am J Health Syst Pharm. 2002 Jul 15;59(14):1333-9.

[4]Huarui Zhang, et al. Advances in the discovery of exosome inhibitors in cancer. J Enzyme Inhib Med Chem. 2020 Dec;35(1):1322-1330.

Esomeprazole sodium/埃索美拉唑钠 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.72mL

0.54mL

0.27mL

13.61mL

2.72mL

1.36mL

27.22mL

5.44mL

2.72mL

Esomeprazole sodium/埃索美拉唑钠 技术信息

CAS号161796-78-7
分子式C17H18N3NaO3S
分子量 367.4
SMILES Code O=[S@](C1=NC2=CC=C(OC)C=C2[N-]1)CC3=NC=C(C)C(OC)=C3C.[Na+]
MDL No. MFCD07802816
别名 (S)-Omeprazole sodium; (-)-Omeprazole sodium; Esomeprazole(sodium)
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, room temperature

溶解方案

DMSO: 105 mg/mL(285.79 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(272.18 mM),配合低频超声助溶

无水乙醇: 50 mg/mL(136.09 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
方案 三
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