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VULM 1457

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Chemical Structure| 228544-65-8 同义名 : -
CAS号 : 228544-65-8
货号 : A950228
分子式 : C25H27N3O3S
纯度 : 99%+
分子量 : 449.565
MDL号 : MFCD10687104
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 250 mg/mL(556.09 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 VULM 1457 is a potent inhibitor of cholesterol acyltransferase (acyl-CoA). VULM1457 significantly reduces adrenomedullin (AM) production and secretion and downregulates AM receptors on human hepatocytes. VULM 1457 has significant hypolipidemic activity and can improve the overall efficacy of myocardial ischemia-reperfusion injury. VULM 1457 has the potential to study diabetes and hypercholesterolemia [1][2].VULM 1457 significantly down-regulates specific AM receptors on HepG2 cells at concentrations ranging from 0.03 and 0.1 µM and reduces AM secretion in HepG2 cells exposed to hypoxia[1][2].VULM1457 negatively regulates AM-induced cell proliferation[1].Pre-incubation of HepG2 cells with VULM 1457 at a concentration of 0.1 µM significantly reduced the total number of untouched affinity-specific [125I]AM binding found on the cells. Pre-incubation of HepG2 cells with VULM 1457 at high concentrations and at concentrations of 1.0 and 10.0 µM significantly altered AM binding properties[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.12mL

2.22mL

1.11mL

22.24mL

4.45mL

2.22mL

参考文献

[1]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.

[2]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