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

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Quality Control

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

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

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

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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

Mechanism of Action

Targets/IC50/Ki
glucosylceramide synthase
(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.
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.In rodents, this compound is rapidly metabolized with a half-life of 15–45 minutes.
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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