Art. -Nr.: HY-14885

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Eliglustat

(Synonyms: Genz 99067)

13 Cited Publications

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Based on 13 publication(s) in Google Scholar

Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC₅₀ of 24 nM.

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Reinheit: 99.74%
CAS. Nr.: 491833-29-5
Formel: C₂₃H₃₆N₂O₄
Molecular Weight:404.54

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Eliglustat Chemical Structure

CAS. Nr.: 491833-29-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC₅₀ of 24 nM.

IC₅₀ & Target

IC50: 24 nM (glucocerebroside synthase)^[1]

In Vitro

Eliglustat tartrate shows good potency with an IC₅₀ of 24 nM and specificity against the target enzyme^[1].Incubating K562 or B16/F10 cells for 72 h with increasing amounts of Genz-112638 (0.6-1000 nM) results in a dose-dependent reduction of cell surface levels of both GM1 and GM3. The mean IC₅₀ value for inhibiting the cell surface presentation of GM1 in K562 cells was 24 nM (range 14-34 nM) and that for GM3 in B16/F10 cells was 29 nM (range 12-48 nM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Mice that received drug prior to significant accumulation of substrate (10 weeks of age) showed reduced levels of glucosylceramide and number of Gaucher cells in the spleen, lung and liver when compared to age-matched control animals^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 491833-29-5
Appearance Solid
Molecular Weight 404.54
Formel C₂₃H₃₆N₂O₄
Color White to off-white
SMILES

CCCCCCCC(N[C@H](CN1CCCC1)[C@@H](C2=CC=C(OCCO3)C3=C2)O)=O
Synonyms

Genz 99067
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (13)

All Cell Proliferation/Viability AssayCell Imaging/StainingWBIHCIn Vivo Imaging

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Journal Impact Factor

Immunity

The SPPL3-Defined Glycosphingolipid Repertoire Orchestrates HLA Class I-Mediated Immune Responses. [Abstract]

2021 Jan 12;54(1):132-150.e9. PMID: 33271119
Cancer Discov

Targeting UGCG overcomes resistance to lysosomal autophagy inhibition. [Abstract]

2023 Feb 6;13(2):454-473. PMID: 36331284
Nat Commun

Inhibition of glycosphingolipid synthesis with eliglustat in combination with immune checkpoint inhibitors in advanced cancers: preclinical evidence and phase I clinical trial. [Abstract]

2024 Aug 14;15(1):6970. PMID: 39138212
Nat Commun

Caveolin-1-mediated sphingolipid oncometabolism underlies a metabolic vulnerability of prostate cancer. [Abstract]

2020 Aug 27;11(1):4279. PMID: 32855410

Eliglustat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Aug 27;11(1):4279. [Abstract]

Viability curves for RM-9 and PC-3M cells following 48 h treatment with vehicle (ethanol), Eliglustat (128 μM), PDMP or PPMP.

Eliglustat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Aug 27;11(1):4279. [Abstract]

Treatment with Eliglustat (128 μM) indicated loss of the branched, fused-like-mitochondrial architecture, and accumulation of punctate mitochondria co-localized with the lysosome.

Eliglustat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Aug 27;11(1):4279. [Abstract]

Treatment of PC-3M cells with Eliglustat (128 μM) increased protein expression of the mitophagy-associated markers LC3B-II.

Eliglustat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Aug 27;11(1):4279. [Abstract]

Representative immunohistochemistry staining for Cav-1, BrdU-TUNEL, PCNA, HMGB1, and LC3B in RM-9 tumors following treatment with either saline or Eliglustat (60 mg/kg, i.p.).

Eliglustat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Aug 27;11(1):4279. [Abstract]

Representative IVIS images following treatment with saline or Eliglustat (60 mg/kg, i.p.).
Sci Adv

Tumor-derived RAC1A159V mutation promotes an immunosuppressive microenvironment that represses response to immune checkpoint inhibitor. [Abstract]

2025 Oct 31;11(44):eaea1212. PMID: 41160695
Cell Death Dis

ECHS1, an interacting protein of LASP1, induces sphingolipid-metabolism imbalance to promote colorectal cancer progression by regulating ceramide glycosylation. [Abstract]

2021 Oct 6;12(10):911. PMID: 34615856
Int J Biol Macromol

Inhibiting UGCG prevents PRV infection by decreasing lysosome-associated autophage. [Abstract]

2024 Dec 2:285:138303. PMID: 39631580
EMBO J

ST3GAL5-catalyzed gangliosides inhibit TGF-β-induced epithelial-mesenchymal transition via TβRI degradation. [Abstract]

2023 Jan 16;42(2):e110553. PMID: 36504224

Eliglustat purchased from MedChemExpress. Usage Cited in: EMBO J. 2023 Jan 16;42(2):e110553. [Abstract]

Eliglustat (1, 2 μM; 6 days) strongly promotes TGF-β-induced SMAD2 phosphorylation in A549-VIM-RFP cells. Eliglustat incubate for 4 days and then treat with TGF-β or vehicle control for another 2 days.
PLoS Biol

The mTORC2 subunit RICTOR drives breast cancer progression by promoting ganglioside biosynthesis through transcriptional and epigenetic mechanisms. [Abstract]

2025 Sep 11;23(9):e3003362. PMID: 40934285
Stem Cells Transl Med

Elevated glucosylsphingosine in Gaucher disease induced pluripotent stem cell neurons deregulates lysosomal compartment through mammalian target of rapamycin complex 1. [Abstract]

2021 Jul;10(7):1081-1094. PMID: 33656802
PLoS One

Cellular and biochemical response to chaperone versus substrate reduction therapies in neuropathic Gaucher disease. [Abstract]

2021 Oct 25;16(10):e0247211. PMID: 34695170
Leiden University

2022 Jun 15.
bioRxiv

2021 Feb 2.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (247.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4719 mL

12.3597 mL

24.7194 mL

5 mM

0.4944 mL

2.4719 mL

4.9439 mL

10 mM

0.2472 mL

1.2360 mL

2.4719 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (6.18 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[1]

The inhibitory activity of Genz-112638 is determined indirectly by measuring its effect on the cell surface levels of the gangliosides GM1 and GM3 on either K562 or B16/F10 cells. GM1 levels on the K562 cells are determined by incubating the cells with increasing amounts of Genz-112638 (0.6-1000 nM) for 72 h after which the cells are harvested and stained using 10 μg of recombinant cholera toxin-FITC in 100 μL phosphate buffered saline (PBS) containing 0.5% bovine serum albumin (BSA) for 30 min on ice. Cells are ished, resuspended in PBS containing 0.5% BSA and the fluorescence quantitated^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice: Eliglustat hemitartrate is dissolved in water for injection and administered in a dose escalation from 75 mg/kg/day to 150 mg/kg/day over the course of nine days, with three days at each dose and increments of 25 mg/kg/day. Mice are weighed three times per week to monitor the potential impact of the drug on their overall health. Animals are killed by carbon dioxide inhalation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. McEachern KA, et al. A specific and potent inhibitor of glucosylceramide synthase for substrate inhibition therapy ofGaucher disease. Mol Genet Metab. 2007 Jul;91(3):259-68. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4719 mL	12.3597 mL	24.7194 mL	61.7986 mL
	5 mM	0.4944 mL	2.4719 mL	4.9439 mL	12.3597 mL
	10 mM	0.2472 mL	1.2360 mL	2.4719 mL	6.1799 mL
	15 mM	0.1648 mL	0.8240 mL	1.6480 mL	4.1199 mL
	20 mM	0.1236 mL	0.6180 mL	1.2360 mL	3.0899 mL
	25 mM	0.0989 mL	0.4944 mL	0.9888 mL	2.4719 mL
	30 mM	0.0824 mL	0.4120 mL	0.8240 mL	2.0600 mL
	40 mM	0.0618 mL	0.3090 mL	0.6180 mL	1.5450 mL
	50 mM	0.0494 mL	0.2472 mL	0.4944 mL	1.2360 mL
	60 mM	0.0412 mL	0.2060 mL	0.4120 mL	1.0300 mL
	80 mM	0.0309 mL	0.1545 mL	0.3090 mL	0.7725 mL
	100 mM	0.0247 mL	0.1236 mL	0.2472 mL	0.6180 mL

Keywords

Eliglustat

13 Cited Publications

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Eliglustat

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Publications Citing Use of MedChemExpress (MCE) Eliglustat

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Eliglustat

Anti-Infection Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Targeted Diversity Library

Rare Diseases Drug Library

Pediatric Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Cardiotoxic Compound Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Eliglustat

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Eliglustat Related Classifications

HY-14885 Related Classifications