5.33371
Acid Ceramidase Inhibitor IV, BOC
Sinónimos:
Acid Ceramidase Inhibitor IV, BOC, AC Inhibitor IV
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About This Item
Fórmula empírica (notación de Hill):
C24H21FN2O3
Número de CAS:
Peso molecular:
404.43
Número MDL:
Código UNSPSC:
12352106
NACRES:
NA.77
Productos recomendados
Ensayo
≥98% (HPLC)
Nivel de calidad
Formulario
solid
fabricante / nombre comercial
Calbiochem®
condiciones de almacenamiento
OK to freeze
protect from light
color
off-white
solubilidad
DMSO: 40 mg/mL
temp. de almacenamiento
2-8°C
Descripción general
A cell-permeable, chemically and metabolically stable (t1/2 >5 h in aqueous buffers at pH 4.5 and 7.4; t1/2 >2 h in murine plasma at 37 °C) benzoxazolone carboxamide (BOC) compound that inhibits acid ceramidase (AC) activity in a potent (IC50 = 79 nM against HEK293 lysosomal lysate AC activity) and selective manner via covalent modification of the active site Cys143, exhibiting little or no potency toward a panel of 15 enzymes, including proteases, lipoxygenases, cyclooxygenases, sPLA2, and monoacylglycerol lipase (67% inhibition of cathepsin D and ≤17.1% inhibition of the rest at 10 µM). Culture treatment results in long-lasting (>6 h) suppression of cellular AC activity in murine macrophage-like Raw 264.7 and human colon adenocarcinoma SW403 cells (IC50 with 3 h treatment = 400 and 825 nM, respectively), as well as built-ups of cellular AC substrates Cer(d18:0/16:0) & Cer(d18:1/16:0) in a dose-dependent manner. Intraperitoneal injection (10 mg/kg) effectively inhibits tissue AC activity in multiple organs, including lung, heart, kidney, brain hippocampus, and liver (by 70%, 60%, 44%, 40%, 35%, respectively), with good pharmacokinetic properties (Tmax = 30 min, Cmax = 1.768 µg/mL, t1/2 = 458 min, AUC0-8 h = 0.31 mg·min/mL; 10 mg/kg i.p.).
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Acid Ceramidase Inhibitor, BOC, CAS 1644158-57-5, is a cell-permeable, potent inhibitor of acid ceramidase (IC₅₀ = 79 nM against HEK293 lysosomal lysate AC activity).
Acciones bioquímicas o fisiológicas
Cell permeable: yes
Primary Target
Acid ceramidase
Acid ceramidase
Reversible: no
Target IC50: 79 nM against HEK293 lysosomal lysate AC activity
Advertencia
Toxicity: Standard Handling (A)
Reconstitución
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Otras notas
Pizzirani, D., et al. 2015. Angew. Chem. Int. Ed. Engl.54, 485.
Información legal
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Código de clase de almacenamiento
11 - Combustible Solids
Clase de riesgo para el agua (WGK)
WGK 3
Punto de inflamabilidad (°F)
Not applicable
Punto de inflamabilidad (°C)
Not applicable
Certificados de análisis (COA)
Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»
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