10mM in DMSO para flujos de trabajo cromatográficos y analíticos sensibles que requieren una interferencia mínima de la línea base.
Store at -80°C Envío Dry ice packs + Cold packs. Consulte el COA específico del lote para conocer las especificaciones exactas.
SDS, COA, ficha técnica y hoja de especificaciones disponibles para descargar. COA específico del lote accesible mediante búsqueda por número de lote.
Citado en 1 publicaciones revisadas por pares sobre cromatografía, síntesis orgánica y reacciones de acoplamiento cruzado.
Information
A922500 A922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets.
In vitro
A 922500 inhibits the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 296 μM. A 922500 potently inhibits huDGAT-1 and mseDGAT-1.
In vivo
Zucker fatty rats and diet-induced dyslipidemic hamsters are dosed orally with A 922500 (0.03, 0.3, and 3 mg/kg) for 14 days. Serum triglycerides ae significantly reduced by the 3 mg/kg dose of A 922500 in both the Zucker fatty rat (39%) and hyperlipidemic hamster (53%). These serum triglyceride changes are accompanied by significant reductions in free fatty acid levels by 32% in the Zucker fatty rat and 55% in the hyperlipidemic hamster. In addition, high-density lipoprotein-cholesterol is significantly increases (25%) in the Zucker fatty rat by A 922500 administered at 3 mg/kg. A 922500 confers weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depletes serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice. A 922500 (0.03, 0.3 and 3 mg/kg, p.o.) dose-dependently attenuates the maximal postprandial rise in serum triglyceride concentrations.
Cell Data
cell lines：HUVECs
Concentrations：
Incubation Time：
Powder Purity:≥99%
Documento completo sobre peligros, manipulación, almacenamiento y cumplimiento normativo.
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Ver hoja de especificaciones →| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Solubilidad | Solubility (25°C) In vitro DMSO: 15 mg/mL (18.96 mM); Water: Insoluble; Ethanol: Insoluble; |
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