Home Metabolism Glucosylceramide Synthase inhibitor Eliglustat For research use only.

Eliglustat

Synonyms: GENZ-112638

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 Chemical Structure

Eliglustat Chemical Structure

CAS No. 491833-29-5

Purity & Quality Control

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

Eliglustat Related Products

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

Chemical Information & Solubility

Molecular Weight 404.54 Formula

C23H36N2O4
CAS No. 491833-29-5 SDF Download Eliglustat SDF
Smiles CCCCCCCC(=O)NC(CN1CCCC1)C(C2=CC3=C(C=C2)OCCO3)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 80 mg/mL ( (197.75 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 80 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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