A glucosylceramide synthase inhibitor (IC50 = 40 nM for inhibition of glucosylceramide production in K562 cells); selective for glucosylceramide synthase over α-glucosidase I and II

Eliglustat (hemitartrate) – 10 mg

Brand:
Cayman
CAS:
928659-70-5
Storage:
-20
UN-No:
Non-Hazardous - /

Eliglustat is an inhibitor of glucosylceramide synthase (IC50 = 40 nM for inhibition of glucosylceramide production in K562 cells).{41053} It is selective for glucosylceramide synthase over α-glucosidase I and II, α-1,6-glucosidase, lysosomal glucocerebrosidase, non-lysosomal glucosylceramidase, sucrase, and maltase (IC50s = >10 µM for all). It decreases cell surface levels of the gangliosides GM1 and GM3 in K562 and B16/F10 cells with IC50 values of 24 and 29 nM, respectively. Eliglustat (150 mg/kg per day) decreases glucosylceramide levels in the liver and lungs of D409V/null mice, a model of Gaucher disease. Formulations containing eliglustat have been used in the treatment of type 1 Gaucher disease.  

 

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Description

A glucosylceramide synthase inhibitor (IC50 = 40 nM for inhibition of glucosylceramide production in K562 cells); selective for glucosylceramide synthase over α-glucosidase I and II, α-1,6-glucosidase, lysosomal glucocerebrosidase, non-lysosomal glucosylceramidase, sucrase, and maltase (IC50s = >10 µM for all); decreases GM1 and GM3 cell surface levels in K562 and B16/F10 cells (IC50s = 24 and 29 nM, respectively); decreases glucosylceramide levels in the liver and lungs of D409V/null mice,,

Formal name: N-[(1R,2R)-2-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-hydroxy-1-(1-pyrrolidinylmethyl)ethyl]-octanamide, 2R,3R-dihydroxybutanedioate (2:1)

Synonyms:  Genz-112638

Molecular weight: 479.6

CAS: 928659-70-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Sphingolipid Turnover||Research Area|Endocrinology & Metabolism|Inborn Errors of Metabolism||Research Area|Lipid Biochemistry|Sphingolipids||Research Area|Neuroscience

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