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

Ilaprazole sodium (Synonyms: IY-81149 sodium)

目录号: HY-B2145 纯度: 98.50%
产品使用指南

Ilaprazole (IY-81149) sodium,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 sodium 用于胃溃疡的研究。Ilaprazole sodium 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 sodium Chemical Structure

Ilaprazole sodium Chemical Structure

CAS No. : 172152-50-0

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Description

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

In Vitro

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

In Vivo

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

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.
Molecular Weight

388.42

Formula

C₁₉H₁₇N₄NaO₂S

CAS No.

172152-50-0

SMILES

O=S(C1=NC2=CC=C(N3C=CC=C3)C=C2[N-]1)CC4=NC=CC(OC)=C4C.[Na+]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

References
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Keywords:

IlaprazoleIY-81149IY81149IY 81149Proton PumpTOPKT-LAK cell-originated protein kinaseoralpumpgastriculcersacidcancerInhibitorinhibitorinhibit

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Ilaprazole sodium
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HY-B2145
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