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

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.

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VULM 1457 Chemical Structure

VULM 1457 Chemical Structure

CAS No. : 228544-65-8

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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 143 In-stock
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10 mM * 1 mL in DMSO USD 143 In-stock
Solid
1 mg USD 61 In-stock
5 mg USD 130 In-stock
10 mg USD 200 In-stock
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Based on 1 publication(s) in Google Scholar

VULM 1457 Related Antibodies

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ACAT1 ACAT2 MGAT2 ACAT

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Description

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

 

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].

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

VULM 1457 Related Antibodies
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].

MedChemExpress (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.
Molecular Weight

449.57

Formula

C25H27N3O3S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CC=C(SC2=CC=C([N+]([O-])=O)C=C2)C=C1)NC3=C(C=CC=C3C(C)C)C(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (556.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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VULM 1457 Related Classifications

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  • 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.

Keywords:

VULM 1457228544-65-8VULM1457VULM-1457AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferasecholesterol acyltransferaseacyl-CoAhypolipidaemicdiabetes mellitushypercholesterolaemiamyocardialischaemia-reperfusionInhibitorinhibitorinhibit

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