N-[2,6-BIS(1-METHYLETHYL)PHENYL]-N'-[4-[(4-NITROPHENYL)THIO]PHENYL]UREA
N-[2,6-BIS(1-METHYLETHYL)PHENYL]-N'-[4-[(4-NITROPHENYL)THIO]PHENYL]UREA Basic information
- Product Name:
- N-[2,6-BIS(1-METHYLETHYL)PHENYL]-N'-[4-[(4-NITROPHENYL)THIO]PHENYL]UREA
- Synonyms:
-
- N-[2,6-BIS(1-METHYLETHYL)PHENYL]-N'-[4-[(4-NITROPHENYL)THIO]PHENYL]UREA
- VULM 1457
- VULM 1457,acyl-CoA:cholesterol acyltransferase,hypercholesterolaemia,Diacylglycerol acyltransferase,ischaemia-reperfusion,myocardial,Diglyceride acyltransferase,mono- acylglycerol acyltransferase,Inhibitor,VULM1457,acyl-CoA,cholesterol acyltransferase,Acyltransferase,hypolipidaemic,inhibit,VULM-1457,diabetes mellitus
- Urea, N-[2,6-bis(1-methylethyl)phenyl]-N'-[4-[(4-nitrophenyl)thio]phenyl]-
- 1-(2,6-Diisopropylphenyl)-3-(4-((4-nitrophenyl)thio)phenyl)urea
- CAS:
- 228544-65-8
- MF:
- C25H27N3O3S
- MW:
- 449.57
- Mol File:
- 228544-65-8.mol
N-[2,6-BIS(1-METHYLETHYL)PHENYL]-N'-[4-[(4-NITROPHENYL)THIO]PHENYL]UREA Chemical Properties
- Boiling point:
- 535.0±50.0 °C(Predicted)
- Density
- 1.24±0.1 g/cm3(Predicted)
- storage temp.
- Store at +4°C
- solubility
- Soluble to 100 mM in DMSO
- form
- Powder
- pka
- 13.79±0.70(Predicted)
- color
- Light yellow to yellow
N-[2,6-BIS(1-METHYLETHYL)PHENYL]-N'-[4-[(4-NITROPHENYL)THIO]PHENYL]UREA Usage And Synthesis
Uses
VULM 1457 is a cholesterol acyltransferase inhibitor.
Biological Activity
Acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor. Decreases cholesterol levels in the plasma and liver of diabetic-hypercholesterolaemic rats.
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].
| 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. |
IC 50
ACAT
N-[2,6-BIS(1-METHYLETHYL)PHENYL]-N'-[4-[(4-NITROPHENYL)THIO]PHENYL]UREASupplier
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