Home Metabolism Glucosylceramide Synthase inhibitor Eliglustat

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Eliglustat Glucosylceramide Synthase inhibitor

Cat.No.S7852

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

Chemical Structure

Molecular Weight: 404.54

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: S785201 DMSO]80 mg/mL]false]Ethanol]80 mg/mL]false]Water]Insoluble]false Purity: 99.8%
99.8

Chemical Information, Storage & Stability

Molecular Weight 404.54 Formula

C23H36N2O4

 Storage (From the date of receipt)
CAS No. 491833-29-5 Download SDF Storage of Stock Solutions

Synonyms GENZ-112638 Smiles CCCCCCCC(=O)NC(CN1CCCC1)C(C2=CC3=C(C=C2)OCCO3)O

Solubility

In vitro
Batch:

DMSO : 80 mg/mL (197.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 80 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
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 this compound is highly specific. It 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 of this compound demonstrates significant dose-related decreases in spleen, kidney and liver glucosylceramide content, consistent with prior observations with the palmitoyl homologue[1].In rodents, this compound is rapidly metabolized with a half-life of 15–45 minutes[2].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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