Ilaprazole(Synonyms: 艾普拉唑; IY-81149)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Ilaprazole (Synonyms: 艾普拉唑; IY-81149) 纯度: ≥98.0%

Ilaprazole (IY-81149),一种具有口服活性质子泵抑制剂,以剂量依赖性方式不可逆地抑制 H+/K+-ATPase,在兔壁细胞制剂中的 IC50 为 6 μM。Ilaprazole 用于胃溃疡的研究。Ilaprazole 也是一种有效的T细胞起源蛋白激酶 (TOPK) 抑制剂。

Ilaprazole(Synonyms: 艾普拉唑; IY-81149)

Ilaprazole Chemical Structure

CAS No. : 172152-36-2

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1209 In-stock
2 mg ¥900 In-stock
5 mg ¥1500 In-stock
10 mg ¥2400 In-stock
50 mg ¥8500 In-stock
100 mg ¥14000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Ilaprazole 相关产品

相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • Membrane Transporter/Ion Channel Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • NMPA-Approved Drug Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library

生物活性

Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H+/K+-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor[1][2].

IC50 & Target

IC50: 6.0 μM (H+/K+-ATPase)[1]

体外研究
(In Vitro)

On cumulation of 14C-aminopyrine in histamine stimulated parietal cells, the IC50 of Ilaprazole (IY-81149) sodium is 9 nM[1].

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.

体内研究
(In Vivo)

Ilaprazole (3-30 mg/kg; i.d.) dose-dependently inhibits gastric acid secretion[1].
In anesthetized rats, Ilaprazole dose-dependently increased gastric pH which was lowered by histamine infusion. In the case of i.v. injection, the ED50 of Ilaprazole and omeprazole is 1.2 and 1.4 mg/kg and in the case of i.d. administration, the ED50 of Ilaprazole and omeprazole is 3.9 and 4.1 mg/kg, respectively. Ilaprazole also significantly inhibits pentagastrin-stimulated gastric secretion. Its ED50 is 2.1 mg/kg and that of Omeprazole is 3.5 mg/kg with i.d. administration. In the case of i.v. injection, Ilaprazole is equipotent to Omeprazole. Ilaprazole also inhibits gastric acid secretion strongly in fistular rats. The ED50 of Ilaprazole administered intraduodenally is 0.43 mg/kg and that of Omeprazole is 0.68 mg/kg[1].

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 SD rat (after pylorus ligation)[1]
Dosage: 3, 10, 30 mg/kg
Administration: Intraduodenally
Result: The acid output and volume significantly inhibited by about 60 % and 46 % at 3 mg/kg were s, respectively. At 30 mg/kg, it showed 93 % and 73 % inhibition on acid output and volume, respectively.

Clinical Trial

分子量

366.44

Formula

C19H18N4O2S

CAS 号

172152-36-2

中文名称

艾普拉唑

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 : ≥ 35 mg/mL (95.51 mM)

Ethanol : 12.5 mg/mL (34.11 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 2.7290 mL 13.6448 mL 27.2896 mL
5 mM 0.5458 mL 2.7290 mL 5.4579 mL
10 mM 0.2729 mL 1.3645 mL 2.7290 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% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.25 mg/mL (3.41 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (3.41 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 EtOH 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% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.25 mg/mL (3.41 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (3.41 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 EtOH 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% EtOH    90% corn oil

    Solubility: ≥ 1.25 mg/mL (3.41 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (3.41 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 12.5 mg/mL 的澄清 EtOH 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]. Kwon D, et al. Effects of IY-81149, a newly developed proton pump inhibitor, on gastric acid secretion in vitro and in vivo. Arzneimittelforschung. 2001;51(3):204-13.

    [2]. Zheng M, et al. Proton pump inhibitor ilaprazole suppresses cancer growth by targeting T-cell-originated protein kinase. Oncotarget. 2017;8(24):39143-39153.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务