Eliglustat

For research use only.

Catalog No.S7852 Synonyms: GENZ-112638

2 publications

Eliglustat Chemical Structure

CAS No. 491833-29-5

Eliglustat (GENZ-112638) inhibits glucosylceramide synthase(GCS) (IC50=20 nM in intact MDCK cells), thus reducing the load of glucosylceramide influx into the lysosome.

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Selleck's Eliglustat has been cited by 2 publications

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Choose Selective Glucosylceramide Synthase Inhibitors

Biological Activity

Description Eliglustat (GENZ-112638) inhibits glucosylceramide synthase(GCS) (IC50=20 nM in intact MDCK cells), thus reducing the load of glucosylceramide influx into the lysosome.
Targets
glucosylceramide synthase [1]
(In intact MDCK cells)
20 nM
In vitro

Eliglustat tartrate is designed and developed to inhibit glucosylceramide synthase, the enzyme that catalyzes the formation of glucosylceramide from UDP-glucose and ceramide.The inhibition of glucosylceramide synthase by eliglustat tartrate is highly specific. Eliglustat tartrate displays limited or no activity against a variety of glycosidases. Additionally, no inhibition of sucrase or maltase is observed at drug concentrations up to 10 μM[1].

In vivo Preclinical studies in normal mice, rats and dogs with i.v. and oral administration demonstrates significant dose-related decreases in spleen, kidney and liver glucosylceramide content, consistent with prior observations with the palmitoyl homologue[1].In rodents, Genz-112638 is rapidly metabolized with a half-life of 15–45 minutes[2].

Protocol

Solubility (25°C)

In vitro DMSO 80 mg/mL (197.75 mM)
Water Insoluble
Ethanol ''''80 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 404.54
Formula

C23H36N2O4

CAS No. 491833-29-5
Storage powder
in solvent
Synonyms GENZ-112638
Smiles CCCCCCCC(=O)NC(CN1CCCC1)C(C2=CC3=C(C=C2)OCCO3)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00891202 Completed Drug: Eliglustat tartrate|Drug: Placebo Gaucher Disease Type 1 Genzyme a Sanofi Company|Sanofi November 2009 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID