[CAS NO. 172152-36-2] Ilaprazole

Name: Ilaprazole
Brand: Arctom Scientific
SKU: SLK-S3666

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PRODUCTS SPECIFICATIONS [172152-36-2]

Store

Catalog

SLK-S3666

Brand

Selleck

CAS

172152-36-2

DESCRIPTION [172152-36-2]

Overview

MDL	MFCD00942538
Molecular Weight	366.44
Molecular Formula	C19H18N4O2S
SMILES	S(CC1=C(C)C(OC)=CC=N1)(=O)C=2NC=3C(N2)=CC=C(C3)N4C=CC=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

Ilaprazole (IY-81149) is a new used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD) and duodenal ulcer. It inhibits with an IC50 of 6.0 μM.

Targets

Proton pump ^[2]	H+/K+-ATPase ^[2] (Cell-free assay)	TOPK ^[1]
	6 μM	111 μM(Kd)

In vitro

Ilaprazole inhibited TOPK activities with high affinity and selectivity. In vitro studies showed that ilaprazole inhibited TOPK activities in HCT116, ES-2, A549, SW1990 cancer cells. Ilaprazole was also found to induce the cleavage of poly-(ADP-ribose) polymerase (PARP), a DNA repair regulatory protein. In rabbit parietal cell preparation, IY-81149 irreversibly inhibited H+/K+-ATPase in dose-dependent manner with an IC50 of pump inhibitory activity of 6.0×10

In vivo

Ilaprazole could suppress tumor growth by inhibiting TOPK activities in vivo. The phosphorylations of histone H3 (Ser10) were significantly inhibited in ilaprazole-treated tumor tissues. The toxicological data showed that the LD50 of ilaprazole was more than 5000 mg/kg in rats. In pylorus-ligated rats, IY-81149 had a strong and long-lasting antisecretory activity despite of its instability in acidic solution. IY-81149 strongly inhibited secretagogues stimulated gastric acid secretion in rats and dogs.

References

[1] Zheng M, et al. Oncotarget. 2017, 8(24):39143-39153.
[2] Kwon D, et al. Arzneimittelforschung. 2001, 51(3):204-13.

Synonyms

1H-Benzimidazole, 2-[[(4-methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-6-(1H-pyrrol-1-yl)-

1H-Benzimidazole, 2-[[(4-methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-5-(1H-pyrrol-1-yl)-

2-[[(4-Methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-6-(1H-pyrrol-1-yl)-1H-benzimidazole

IY 81149

Ilaprazole

RS-ilaprazole

2-[(4-Methoxy-3-methylpyridin-2-yl)methylsulfinyl]-6-pyrrol-1-yl-1H-benzimidazole