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VULM 1457
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
VULM 1457图片
CAS NO:228544-65-8
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
VULM 1457 是有效的胆固醇酰基转移酶抑制剂,具有显著的降血脂活性,并改善了整体心肌缺血再灌注损伤结果。VULM 1457 显著降低肾上腺髓质素的产生和分泌,并下调人肝母细胞上的 AM 受体。VULM 1457 具有研究糖尿病和高胆固醇血症的潜力。

产品描述

VULM 1457 is a potent ACAT inhibitor. VULM 1457 has remarkable hypolipidaemic activity and improves the overall myocardial ischaemia-reperfusion injury outcomes. VULM1457 significantly reduces production and secretion of adrenomedullin (AM) and down-regulates AM receptors on human hepatoblastic cells.

体外活性

Preincubation of HepG2 cells with VULM1457 (0.1 μM) significantly reduced 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 enhanced the number of cells (24.2±6 %) and higher concentrations of VULM1457 (1.0 and 10.0 μM) reduces the total number of cells[2]. In HepG2 cell lines, VULM1457 (0.03 μM; 0.1 μM) significantly down-regulated specific AM receptors on HepG2 cells, and reduced AM secretion of HepG2 cells exposed to hypoxia. VULM1457 negatively regulates cell proliferation induced by AM[2].

体内活性

In male Wistar rats, VULM 1457 protected the hearts of diabetic–hypercholesterolaemic rats against ischemia/reperfusion injury in vivo[1]. VULM 1457 (50 mg/kg/day) 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)[1].

Cas No.

228544-65-8

分子式

C25H27N3O3S

分子量

449.57

储存和溶解度

DMSO:<44.96mg/ml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years