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Eliglustat hemitartrate Glucosylceramide Synthase inhibitor

Name: Eliglustat hemitartrate
Brand: Selleck Chemicals
SKU: S4433
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S4433

Eliglustat hemitartrate (Genz-112638, Eliglustat tartrate) is a potent, specific and orally active inhibitor of glucosylceramide synthase with IC50 of 24 nM.

Chemical Structure

Molecular Weight: 959.17

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

Quality Control

Batch: Purity: 99.89%

99.89

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite Casein Kinase Serine/threonin kinase Lipoxygenase LPL Receptor Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Amino Acids and Derivatives Fatty Acid Synthase Glucokinase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO
Related Products	Ibiglustat succinate

Chemical Information, Storage & Stability

Molecular Weight	959.17	Formula	C₅₀H₇₈N₄O₁₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	928659-70-5	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Genz-112638, Eliglustat tartrate, Cerdelga			Smiles	CCCCCCCC(=O)NC(CN1CCCC1)C(O)C2=CC3=C(OCCO3)C=C2.CCCCCCCC(=O)NC(CN4CCCC4)C(O)C5=CC6=C(OCCO6)C=C5.OC(C(O)C(O)=O)C(O)=O

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (104.25 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

Ethanol : 10 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (5.21mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.710mg/ml (0.74mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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

Calculation results:

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.

Mechanism of Action

Targets/IC₅₀/Ki	Glucosylceramide Synthase ^[1] (Cell-free assay) 24 nM
In vitro	When treated gaucher disease neuronal progenitor cells (NPCs) with the GlcCer synthase inhibitors Eliglustat and the brain‐penetrant Ibiglustat, there are significant reductions in both, GlcCer and GlcSph levels in the mutant NPCs.^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/17509920/ [2] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8235124/

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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