228544-65-8
228544-65-8 structure
- Name: VULM 1457
- Chemical Name: 1-[2,6-di(propan-2-yl)phenyl]-3-[4-(4-nitrophenyl)sulfanylphenyl]urea
- CAS Number: 228544-65-8
- Molecular Formula: C25H27N3O3S
- Molecular Weight: 449.56500
- Catalog: Research Areas Cardiovascular Disease
- Create Date: 2017-01-12 22:01:31
- Modify Date: 2024-01-14 10:49:08
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VULM 1457 is a potent inhibitor of cholesterol acyltransferase (acyl-CoA). VULM1457 significantly reduces production and secretion of adrenomedullin (AM) and down-regulates AM receptors on human hepatoblastic cells. VULM 1457 has remarkable hypolipidaemic activity and improves the overall myocardial ischaemia-reperfusion injury outcomes. VULM 1457 has the potential for the research of diabetes mellitus and hypercholesterolaemia[1][2].
| Name | 1-[2,6-di(propan-2-yl)phenyl]-3-[4-(4-nitrophenyl)sulfanylphenyl]urea |
|---|---|
| Synonyms | Amthamine dihydrobromide |
| Description | VULM 1457 is a potent inhibitor of cholesterol acyltransferase (acyl-CoA). VULM1457 significantly reduces production and secretion of adrenomedullin (AM) and down-regulates AM receptors on human hepatoblastic cells. VULM 1457 has remarkable hypolipidaemic activity and improves the overall myocardial ischaemia-reperfusion injury outcomes. VULM 1457 has the potential for the research of diabetes mellitus and hypercholesterolaemia[1][2]. |
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| Related Catalog | |
| Target |
ACAT |
| In Vitro | VULM1457 (0.03 and 0.1 µM) significantly down-regulates specific AM receptors on HepG2 cells, reduced AM secretion of HepG2 cells exposed to hypoxia[1].VULM1457 negatively regulates cell proliferation induced by AM[1]. Preincubation of HepG2 cells with VULM1457 (0.1 µM) significantly reduces the total number of specific [125I]AM binding identified on cells at untouched affinity. Preincubation of HepG2 cells with high concentrations of VULM1457 (1.0 and 10.0 µM) significantly modifies the characteristics of binding of AM, i.e[1]. Preincubation of HepG2 cells with VULM1457 (0.1 µM) significantly reduces the specific [125I]AM binding on hypoxic cells with BmaxHypox being 127±10 and KD 0.06±0.11 nM. Preincubation of cells with VULM1457 (0.1 µM) significantly enhances the number of cells (24.2±6 %) and higher concentrations of VULM1457 (1.0 and 10.0 µM) reduces the total number of cells. With the high concentrations of VULM1457 (1.0 and 10.0 µM), the reductions in [125I]AM specific binding on HepG2 cells is markedly attenuated[1]. |
| In Vivo | VULM 1457 significantly reduces atherogenic activity in animal experimental atherosclerosis[1]. VULM 1457 protect the hearts of diabetic–hypercholesterolaemic rats against ischaemia/reperfusion injury in vivo[2]. VULM 1457 (50 mg/kg/day; administered as an admixture to the fat-cholesterol diet for 5 days) significantly decreases plasma total cholesterol levels (1.7±0.1 mM vs. 2.9±0.5 mM in diabetic–hypercholesterolaemic animals). The hypolipidaemic effect of VULM 1457 is also observed in the liver of DM-HCH rats (3.9±0.2 mg/g vs. 7.4±1.0 mg/g)[2]. Animal Model: Male Wistar rats (250-300 g body weight), fed a standard diet and tap water ad libitum[2] Dosage: 50 mg/kg/day Administration: Administered as an admixture to the fat-cholesterol diet for 5 days Result: Improved the overall myocardial ischaemia-reperfusion injury outcomes in the diabetic-hypercholesterolaemic rats by suppressing arrhythmogenesis as well as by reducing myocardial necrosis, aside from remarkable hypolipidaemic activity. |
| References |
| Molecular Formula | C25H27N3O3S |
|---|---|
| Molecular Weight | 449.56500 |
| Exact Mass | 449.17700 |
| PSA | 112.25000 |
| LogP | 8.30600 |