76081-98-6
76081-98-6 結構式
基本信息
SCH 28080
Schering compound 28080
imidazo-(1-2-a)pyrine-3-acetonitrile
2-Methyl-8-(phenylmethoxy)imidazo-(1-2-A)pyrine-3-acetonitrile
2-METHYL-8-(PHENYLMETHOXY)IMIDAZO[1,2-A]PYRIDINE-3-ACETONITRILE
Imidazo(1,2-A)pyridine-3-acetonitrile, 2-methyl-8-(phenylmethoxy)-
3-(CYANOMETHYL)-2-METHYL-8-(PHENYLMETHOXY)IMIDAZO[1,2-ALPHA]PYRIDINE
物理化學性質
常見問題列表
Ki: 0.12 μM ((H + /K + )-ATPase)
SCH28080 competitively inhibits the K
+
-stimulated hydrolysis of ATP, with a K
i
of 0.12 μM .
SCH28080 inhibits histamine-induced
[14C]
aminopyrine uptake into isolated rabbit parietal cells with an IC
50
of 0.029 μM.
SCH28080 causes a dose-dependent reduction in cell viability with IC
50
values of 22.9 μM and 15.3 μM after 2 h and 24 h treatments, respectively, and cell viability was below 10% at 100 μM already after 2 h treatment.
SCH28080 induces apoptosis and is cytotoxic at higher doses.
SCH28080 inhibits insulin secretion by activation of IK ATP and inhibition of L-type voltage-gated Ca
2+
channels, reduces cell viability and dose-dependently induces apoptosis/necrosis.
Cell Viability Assay
| Cell Line: | INS-1E cell |
| Concentration: | 3.1 μM, 6.25 μM, 12.5 μM, 25 μM, 50 μM, 100 μM |
| Incubation Time: | 2 hours, 24 hours |
| Result: | Caused a dose-dependent reduction in cell viability. |
SCH28080 (20 mg/kg; i.p.) inhibits gastric ulcers induced by pylorusligation in rats.
| Animal Model: | Male Wistar rat (280-350 g), the Shay rat model |
| Dosage: | 20 mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Showed 91% inhibition on gastric ulcers induced by pylorusligation in rats. |