VULM 1457

SKU: orb1305611

Description

VULM 1457 is a potent ACAT inhibitor with significant hypolipidemic activity. It improves outcomes in myocardial ischemia-reperfusion injury models and has been shown in vitro to reduce adrenomedullin production and receptor expression in human hepatoblastic cells, supporting research in cardiovascular and metabolic diseases.

Research Area

Metabolism Research

Key Properties

• CAS Number: 228544-65-8
• MW: 449.57
• Purity: 99.92% (May vary between batches)
• Formula: C₂₅H₂₇N₃O₃S
• SMILES: CC(C)c1cccc(C(C)C)c1NC(=O)Nc1ccc(Sc2ccc(cc2)[N+]([O-])=O)cc1
• Target: Acyltransferase
• Solubility: DMSO:60 mg/mL (133.46 mM)

Bioactivity

• In Vivo:
  In male Wistar rats, VULM 1457 protected the hearts of diabetic–hypercholesterolaemic rats against ischemia/reperfusion injury in vivo. VULM 1457 (50 mg/kg/day) 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).
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• In Vitro:
  Preincubation of HepG2 cells with VULM1457 (0.1 μM) significantly reduced 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 enhanced the number of cells (24.2±6 %) and higher concentrations of VULM1457 (1.0 and 10.0 μM) reduces the total number of cells. In HepG2 cell lines, VULM1457 (0.03 μM; 0.1 μM) significantly down-regulated specific AM receptors on HepG2 cells, and reduced AM secretion of HepG2 cells exposed to hypoxia. VULM1457 negatively regulates cell proliferation induced by AM.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

VULM 1457, VULM1457, VULM-1457, diabetes mellitus, Diacylglycerol acyltransferase, Diglyceride acyltransferase, cholesterol acyltransferase, ACAT, Acyltransferase, acyl-CoA:cholesterol acyltransferase, acyl-CoA, Inhibitor, mono- acylglycerol acyltransferase, hypolipidaemic, hypercholesterolaemia, myocardial, ischaemia-reperfusion, inhibit

Compound Identifiers

PubChem CID

9933427