1. Metabolic Enzyme/Protease
  2. Acyltransferase
  3. VULM 1457

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。

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VULM 1457 Chemical Structure

VULM 1457 Chemical Structure

CAS No. : 228544-65-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1430
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1 mg ¥495
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5 mg ¥1300
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10 mg ¥2000
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50 mg ¥7000
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Customer Review

查看 Acyltransferase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VULM 1457 is a potent inhibitor of cholesterol acyltransferase (acyl-CoA). VULM1457 significantly reduces production and secretion of adrenomedullin (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 BmaxHypox being 127±10 and KD 0.06±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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats (250-300 g body weight), fed a standard diet and tap water ad 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

Formula

C25H27N3O3S

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 250 mg/mL (556.09 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2243 mL 11.1217 mL 22.2435 mL
5 mM 0.4449 mL 2.2243 mL 4.4487 mL
查看完整储备液配制表

* 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°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2243 mL 11.1217 mL 22.2435 mL 55.6087 mL
5 mM 0.4449 mL 2.2243 mL 4.4487 mL 11.1217 mL
10 mM 0.2224 mL 1.1122 mL 2.2243 mL 5.5609 mL
15 mM 0.1483 mL 0.7414 mL 1.4829 mL 3.7072 mL
20 mM 0.1112 mL 0.5561 mL 1.1122 mL 2.7804 mL
25 mM 0.0890 mL 0.4449 mL 0.8897 mL 2.2243 mL
30 mM 0.0741 mL 0.3707 mL 0.7414 mL 1.8536 mL
40 mM 0.0556 mL 0.2780 mL 0.5561 mL 1.3902 mL
50 mM 0.0445 mL 0.2224 mL 0.4449 mL 1.1122 mL
60 mM 0.0371 mL 0.1854 mL 0.3707 mL 0.9268 mL
80 mM 0.0278 mL 0.1390 mL 0.2780 mL 0.6951 mL
100 mM 0.0222 mL 0.1112 mL 0.2224 mL 0.5561 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
VULM 1457
目录号:
HY-107571
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