Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 397 | 现货 | ||
2 mg | ¥ 595 | 现货 | ||
5 mg | ¥ 995 | 现货 | ||
10 mg | ¥ 1,570 | 现货 | ||
25 mg | ¥ 3,290 | 现货 | ||
50 mg | ¥ 4,790 | 现货 | ||
100 mg | ¥ 6,850 | 现货 | ||
500 mg | ¥ 13,700 | 6-8周 |
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]. |
分子量 | 449.57 |
分子式 | C25H27N3O3S |
CAS No. | 228544-65-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: < 44.96 mg/mL
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
VULM 1457 228544-65-8 Metabolism Acyltransferase acyl-CoA:cholesterol acyltransferase hypercholesterolaemia Diacylglycerol acyltransferase ischaemia-reperfusion myocardial Diglyceride acyltransferase mono- acylglycerol acyltransferase Inhibitor acyl-CoA VULM-1457 cholesterol acyltransferase VULM1457 hypolipidaemic inhibit diabetes mellitus inhibitor