VULM 1457
Based on 1 Customer Validation
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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- Pureté: 99.71%
- CAS No.: 228544-65-8
- Formule: C25H27N3O3S
- Masse moléculaire:449.57
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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ACAT |
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 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.
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Animal Model:Male Wistar rats (250-300 g body weight), fed a standard diet and tap water ad libitum[2]
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Dosage:50 mg/kg/day
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Administration:Administered as an admixture to the fat-cholesterol diet for 5 days
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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.
Chemical Information
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CAS No. 228544-65-8
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Appearance Solid
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Masse moléculaire 449.57
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Formule C25H27N3O3S
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Color Light yellow to yellow
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 125 mg/mL (278.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[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 [Content Brief]
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 |
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| 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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