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VULM 1457

CAS No. : 228544-65-8

MCE 站：VULM 1457

产品活性：VULM 1457 是一种有效的胆固醇酰基转移酶 (acyl-CoA) 抑制剂。VULM1457 显着降低肾上腺髓质素 (AM) 的产生和分泌，并下调人肝母细胞上的 AM 受体。VULM 1457 具有显着的降血脂活性，并改善了整体心肌缺血再灌注损伤结果。VULM 1457 具有研究糖尿病和高胆固醇血症的潜力。

研究领域：Metabolic Enzyme/Protease

作用靶点：Acyltransferase

In Vitro: VULM1457 (0.03 ａnd 0.1 M) 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 M) 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 M) significantly modifies the characteristics of binding of AM, i.e.
Preincubation of HepG2 cells with VULM1457 (0.1 M) 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 M) significantly enhances the number of cells (24.2±6 %) ａnd higher concentrations of VULM1457 (1.0 ａnd 10.0 M) reduces the total number of cells. With the high concentrations of VULM1457 (1.0 ａnd 10.0 M), the reductions in [¹²⁵I]AM specific binding on HepG2 cells is markedly attenuated.

In Vivo: VULM 1457 significantly reduces atherogenic activity in animal experimental atherosclerosis.
VULM 1457 protect the hearts of diabetichypercholesterolaemic 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 diabetichypercholesterolaemic 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).

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