[CAS NO. 172152-50-0] Ilaprazole sodium
PRODUCTS SPECIFICATIONS [172152-50-0]
DESCRIPTION [172152-50-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 388.42 |
| Molecular Formula | C19H17N4NaO2S |
| SMILES | O=S(C1=NC2=CC=C(N3C=CC=C3)C=C2[N-]1)CC4=NC=CC(OC)=C4C.[Na+] |
Summary
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 IC 50 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 IC 50 of Ilaprazole (IY-81149) sodium is 9 nM [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 ED
50
of Ilaprazole sodium and Omeprazole is 1.2 and 1.4 mg/kg and in the case of i.d. administration, the ED
50
of Ilaprazole sodium and omeprazole is 3.9 and 4.1 mg/kg, respectively. Ilaprazole sodium also significantly inhibits pentagastrin-stimulated gastric secretion. Its ED
50
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 ED
50
of Ilaprazole sodium 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
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02860624 | Livzon Pharmaceutical Group Inc. |
Gastroesophageal Reflux Disease
|
December 2011 | Phase 3 |
| NCT05558150 | Il-Yang Pharm. Co., Ltd. |
Drug Interaction Potentiation
|
November 11, 2022 | Phase 1 |
| NCT01820143 | Il-Yang Pharm. Co., Ltd. |
Healthy|Pharmacokinetics|Pharmacodynamics|Ilaprazole
|
February 2005 | Phase 1 |
| NCT02084420 | Il-Yang Pharm. Co., Ltd. |
Peptic Ulcer
|
December 2012 | Phase 3 |
| NCT00471094 | Takeda |
Esophagitis
|
May 2007 | Phase 2 |
| NCT01107938 | Livzon Pharmaceutical Group Inc. |
Gastroesophageal Reflux Disease
|
May 2010 | Phase 2 |
| NCT05237297 | Il-Yang Pharm. Co., Ltd. |
Drug Interaction Potentiation
|
February 17, 2022 | Phase 1 |
| NCT00952978 | Livzon Pharmaceutical Group Inc. |
Duodenal Ulcer
|
September 2005 | Phase 3 |
| NCT02835560 | Livzon Pharmaceutical Group Inc.|Fifth Affiliated Hospital, Sun Yat-Sen University |
Helicobacter Pylori Eradication Antibiotic
|
June 2013 | Phase 4 |
| NCT02401477 | Il-Yang Pharm. Co., Ltd. |
Helicobacter Infections
|
December 2014 | Phase 4 |
| NCT03362281 | Livzon Pharmaceutical Group Inc. |
Peptic Ulcer Hemorrhage
|
October 2014 | Phase 3 |
| NCT03342456 | The Third Xiangya Hospital of Central South University|Livzon Pharmaceutical Group Inc.|Yung Shin Pharm. Ind. Co., Ltd. |
Duodenal Ulcer Due to Helicobacter Pylori
|
December 13, 2017 | Phase 4 |
| NCT02648659 | Kyungpook National University Hospital |
Peptic Ulcer
|
March 2, 2016 | Phase 4 |
| NCT00953381 | Livzon Pharmaceutical Group Inc. |
Duodenal Ulcer
|
October 2004 | Phase 2 |
| NCT03139253 | Yanqing Li|Shandong University |
Antimicrobial Susceptibility Testing|Triple Therapy
|
May 30, 2017 | Phase 4 |
| NCT02873065 | Livzon Pharmaceutical Group Inc. |
Helicobacter Pylori Eradication
|
September 2014 | Phase 4 |
| NCT02666976 | Yonsei University |
Gastrointestinal Subepithelial Tumors
|
July 2014 | Phase 4 |
| NCT02998437 | Il-Yang Pharm. Co., Ltd.|Severance Hospital |
Drug Interaction Potentiation
|
December 2016 | Phase 1 |
| NCT01509261 | Il-Yang Pharm. Co., Ltd. |
Erosive Esophagitis|GERD
|
July 2010 | Phase 3 |
| NCT02847455 | Livzon Pharmaceutical Group Inc. |
Duodenal Ulcer
|
August 2008 | Phase 2|Phase 3 |
| NCT02638584 | Il-Yang Pharm. Co., Ltd. |
Gastric Cancer
|
December 2015 | Phase 4 |
| NCT01688544 | Inje University |
Healthy
|
January 2009 | Phase 1 |
| NCT03362268 | Livzon Pharmaceutical Group Inc. |
Peptic Ulcer Hemorrhage
|
February 2014 | Phase 2 |
| NCT03444883 | Il-Yang Pharm. Co., Ltd. |
Non-erosive Reflux Disease
|
October 31, 2018 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 41.67 mg/mL ( 107.28 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5745 mL | 12.8727 mL | 25.7453 mL |
| 5 mM | 0.5149 mL | 2.5745 mL | 5.1491 mL |
| 10 mM | 0.2575 mL | 1.2873 mL | 2.5745 mL |
References
- [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):204-213.
- [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.