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

VULM 1457 是一種有效的膽固醇?；D(zhuǎn)移酶 (acyl-CoA) 抑制劑。VULM1457 顯著降低腎上腺髓質(zhì)素 (AM) 的產(chǎn)生和分泌，并下調(diào)人肝母細胞上的 AM 受體。VULM 1457 具有顯著的降血脂活性，并改善了整體心肌缺血再灌注損傷結(jié)果。VULM 1457 具有研究糖尿病和高膽固醇血癥的潛力。

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VULM 1457 Chemical Structure

VULM 1457 Chemical Structure

CAS No. : 228544-65-8

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規(guī)格 價格 是否有貨 數(shù)量
1 mg ￥298
In-stock
5 mg ￥746
In-stock
10 mg ￥1178
In-stock
25 mg ￥2463
In-stock
50 mg ￥3588
In-stock
100 mg ￥4963
In-stock
200 mg   詢價  
500 mg   詢價  

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查看 Acyltransferase 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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

 

體外研究
(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.
體內(nèi)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 號
性狀

固體

顏色

Light yellow to yellow

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 250 mg/mL (556.09 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱：
VULM 1457
目錄號：
HY-107571
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