Ilaprazole (IY-81149) is an orally activeproton pumpinhibitor. Ilaprazole irreversibly inhibitsH⁺/K⁺-ATPasein a dose-dependent manner with anIC₅₀of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potentTOPK(T-lymphokine-activated killer cell-originated protein kinase) inhibitor^[1][2].

IC50: 6.0 μM (H⁺/K⁺-ATPase)^[1]

On cumulation of 14C-aminopyrine in histamine stimulated parietal cells, the IC₅₀of Ilaprazole (IY-81149) sodium is 9 nM^[1].

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 ED₅₀of Ilaprazole and omeprazole is 1.2 and 1.4 mg/kg and in the case of i.d. administration, the ED₅₀of Ilaprazole and omeprazole is 3.9 and 4.1 mg/kg, respectively. Ilaprazole also significantly inhibits pentagastrin-stimulated gastric secretion. Its ED₅₀is 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 ED₅₀of Ilaprazole administered intraduodenally is 0.43 mg/kg and that of Omeprazole is 0.68 mg/kg^[1].

366.44

Solid

C₁₉H₁₈N₄O₂S

172152-36-2

艾普拉唑

Room temperature in continental US; may vary elsewhere.

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。

DMSO : ≥ 35 mg/mL(95.51 mM)

Ethanol : 12.5 mg/mL(34.11 mM;Need ultrasonic)

*"≥" means soluble, but saturation unknown.

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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

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-CDin 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 μL20% 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。