1. Membrane Transporter/Ion Channel
    Cell Cycle/DNA Damage
  2. Proton Pump
    TOPK
  3. Ilaprazole

Ilaprazole (Synonyms: 艾普拉唑; IY-81149)

目录号: HY-101664 纯度: ≥98.0%
产品使用指南

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。

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Ilaprazole Chemical Structure

Ilaprazole Chemical Structure

CAS No. : 172152-36-2

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10 mM * 1 mL in DMSO ¥1209 In-stock
2 mg ¥900 In-stock
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50 mg ¥8500 In-stock
100 mg ¥14000 In-stock
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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE 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].

MCE 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
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 MCE 网站选购。
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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