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LCL521

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Catalog No. T11835Cas No. 1226851-11-1

LCL521 inhibits lysosomal acid sphingomyelinase (ASMase).LCL521 is an acid ceramidase (ACDase) inhibitor.

LCL521

LCL521

😃Good
Catalog No. T11835Cas No. 1226851-11-1
LCL521 inhibits lysosomal acid sphingomyelinase (ASMase).LCL521 is an acid ceramidase (ACDase) inhibitor.
Pack SizePriceAvailabilityQuantity
25 mg$9876-8 weeks
50 mg$1,3606-8 weeks
100 mg$2,1906-8 weeks
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Product Introduction

Bioactivity
Description
LCL521 inhibits lysosomal acid sphingomyelinase (ASMase).LCL521 is an acid ceramidase (ACDase) inhibitor.
In vitro
LCL521 (1 µM) effectively inhibited ACDase in MCF7 cells, but the effects were transient. LCL521 (10 µM) caused a profound decrease of sphingosine and an increase of ceramide, but additionally affected the processing and regeneration of the ACDase protein, with biphasic and reversible effects on the expression of ACDase, which paralleled the long-term changes of cellular sphingosine and ceramide. The higher concentrations of LCL521 also inhibited Dihydroceramide desaturase (DES-1). In summary, LCL521 exhibits significant effects on ACDase in a dose and time-dependent manner.[2]
In vivo
When PDT-treated SCCVII cells are used to vaccinate SCCVII tumor-bearing mice, adjuvant LCL521 treatment (75 mg/kg; i.p.) resulted in marked retardation of tumor growth. This effect can be attributed to the capacity of LCL521 to effectively restrict the activity of two main immunoregulatory cell populations (Tregs and myeloid-derived suppressor cells, MDSCs) that are known to hinder the efficacy of PDT vaccines. The interaction of LCL521 with PDT-based antitumor mechanisms is dominated by immune system contribution that includes overriding the effects of immunoregulatory cells but could also include a tacit contribution from boosting direct tumor cell kill.[3]
Chemical Properties
Molecular Weight592.77
FormulaC31H52N4O7
Cas No.1226851-11-1
Smiles[C@@H]([C@H](NC(CCCCCCCCCCCCC)=O)COC(CN(C)C)=O)(OC(CN(C)C)=O)C1=CC=C(N(=O)=O)C=C1
Relative Density.1.093 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 148.5 mg/mL (250.5 mM), Sonication is recommended.
Ethanol: 90.0 mg/mL (151.8 mM), Sonication is recommended.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.6870 mL8.4350 mL16.8699 mL84.3497 mL
5 mM0.3374 mL1.6870 mL3.3740 mL16.8699 mL
10 mM0.1687 mL0.8435 mL1.6870 mL8.4350 mL
20 mM0.0843 mL0.4217 mL0.8435 mL4.2175 mL
50 mM0.0337 mL0.1687 mL0.3374 mL1.6870 mL
100 mM0.0169 mL0.0843 mL0.1687 mL0.8435 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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