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.

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. VULM1457 negatively regulates cell proliferation induced by AM.
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.
Preincubation of HepG2 cells with VULM1457 (0.1 µM) significantly reduces the specific [¹²⁵I]AM binding on hypoxic cells with B_maxHypox being 127±10 and K_D 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

VULM 1457 significantly reduces atherogenic activity in animal experimental atherosclerosis.
VULM 1457 protect the hearts of diabetic–hypercholesterolaemic rats against ischaemia/reperfusion injury in vivo.
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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

VULM 1457 significantly reduces atherogenic activity in animal experimental atherosclerosis.
VULM 1457 protect the hearts of diabetic–hypercholesterolaemic rats against ischaemia/reperfusion injury in vivo.
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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . J Drímal, et al. The ACAT inhibitor VULM1457 significantly reduced production and secretion of adrenomedullin (AM) and down-regulated AM receptors on human hepatoblastic cells. Gen Physiol Biophys. 2005 Dec;24(4):397-409.  [Content Brief]

  . Adameová A, et al. The myocardial infarct size-limiting and antiarrhythmic effects of acyl-CoA:cholesterol acyltransferase inhibitor VULM 1457 protect the hearts of diabetic-hypercholesterolaemic rats against ischaemia/reperfusion injury both in vitro and  [Content Brief]