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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)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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。
生物活性

VULM 1457 is a potent inhibitor of cholesterolacyltransferase(acyl-CoA). VULM1457 significantly reduces production and secretion ofadrenomedullin(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].

IC50& Target[1]

ACAT

 

体外研究
(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 BmaxHypoxbeing 127±10 and KD0.06±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].

体内研究
(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 waterad 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.
分子量

449.57

性状

Solid

Formula

C25H27N3O3S

CAS 号

228544-65-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL(556.09 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.2243 mL11.1217 mL22.2435 mL
5 mM0.4449 mL2.2243 mL4.4487 mL
10 mM0.2224 mL1.1122 mL2.2243 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。