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Merck
CN

S4443

SCH-28080

≥98% (HPLC), gastric H+ and K+-ATPase inhibitor, solid

别名:

2-methyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine-3-acetonitrile

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关于此项目

经验公式(希尔记法):
C17H15N3O
化学文摘社编号:
分子量:
277.32
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
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产品名称

SCH-28080, ≥98% (HPLC), solid

SMILES string

Cc1nc2c(OCc3ccccc3)cccn2c1CC#N

InChI key

PYKJFEPAUKAXNN-UHFFFAOYSA-N

InChI

1S/C17H15N3O/c1-13-15(9-10-18)20-11-5-8-16(17(20)19-13)21-12-14-6-3-2-4-7-14/h2-8,11H,9,12H2,1H3

assay

≥98% (HPLC)

form

solid

color

white to light tan

solubility

DMSO: soluble >10 mg/mL, H2O: insoluble

compatibility

for use with ABI 7700

storage temp.

−20°C

Quality Level

Application

SCH-28080 was used to treat zebrafish embryos to study the role of H+/K+-ATPase in establishment of left-right axis during development.

Biochem/physiol Actions

SCH-28080 is a potent inhibitor of gastric H+ and K+-ATPase. The novel antiulcer agents, SCH-28080 and SCH-32651 were examined for their ability to inhibit the H+K+ ATPase enzyme activity in a preparation of microsomal membranes from rabbit fundic mucosa. SCH- 28080 inhibited the isolated enzyme activity with a potency similar to omeprazole, IC50s of 2.5 and 4.0 μM respectively. SCH 32651 was less potent exhibiting an IC50 of 200.0 μM. Both compounds may therefore exert their antisecretory activity via a direct inhibition of the parietal cell H+K+ ATPase.
SCH-28080 is a potent inhibitor of gastric H+ and K+-ATPase.

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Jiahong Shao et al.
Biochimica et biophysica acta, 1800(9), 906-911 (2010-07-03)
The H,K-ATPase, consisting of α and ß subunits, belongs to the P-type ATPase family. There are two isoforms of the α subunit, HKα₁ and HKα₂ encoded by different genes. The ouabain-resistant gastric HKα₁-H,K-ATPase is Sch28080-sensitive. However, the colonic HKα₂-H,K-ATPase from
Aydan Yenişehirli et al.
Pharmacological research, 54(6), 397-405 (2006-09-05)
The effect of H(+)/K(+)-ATPase inhibitors on rat vas deferens contractility was investigated in vitro. Omeprazole (100-300microM), lansoprazole (100-300microM) and SCH 28080 (10-100microM) (2-methyl-8-(phenylmethoxy)-imidazo[1,2-a]pyridine-3-acetonitrile) decreased contractile responses of vas deferens to electrical field stimulation, high K(+) (80mM) and phenylephrine in a
W A Simon et al.
The Journal of pharmacology and experimental therapeutics, 321(3), 866-874 (2007-03-21)
After treatment of millions of patients suffering from gastroesophageal reflux disease (GERD) and other acid-related ailments with proton pump inhibitors, there are still unmet medical needs such as rapid and reliable pain relief, especially for nocturnal acid breakthrough. In this
P Kirchhoff et al.
American journal of physiology. Gastrointestinal and liver physiology, 291(5), G838-G843 (2006-06-27)
The gastric H+,K+-ATPase of the parietal cell is responsible for acid secretion in the stomach and is the main target in the pharmacological treatment of acid-related diseases. Omeprazole and other benzimidazole drugs, although having delayed efficacy if taken orally, have
C K Scott et al.
European journal of pharmacology, 112(2), 268-270 (1985-06-07)
The novel antiulcer agents, SCH 28080 and SCH 32651 were examined for their ability to inhibit the H+K+ ATPase enzyme activity in a preparation of microsomal membranes from rabbit fundic mucosa. SCH 28080 inhibited the isolated enzyme activity with a

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