Eliglustat (Synonyms: Genz 99067)

Name: Eliglustat
Brand: MedChemExpress
SKU: HY-14885
Rating: 5.0 (11 reviews)

Cat. No.: HY-14885 Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

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

For research use only. We do not sell to patients.

Eliglustat Chemical Structure

CAS No. : 491833-29-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 106	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 106	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 119	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 158	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 317	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 581	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Eliglustat:

10 Publications Citing Use of MCE Eliglustat

: Eliglustat purchased from MedChemExpress. Usage Cited in: EMBO J. 2022 Dec 12;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.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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.

Clinical Trial

Molecular Weight

404.54

Formula

C₂₃H₃₆N₂O₄

CAS No.

491833-29-5

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (245 KB) HNMR (193 KB) LCMS (454 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

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

Eliglustat Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Eliglustat491833-29-5Genz 99067Genz99067Genz-99067OthersInhibitorinhibitorinhibit

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Eliglustat (Synonyms: Genz 99067)

Customer Review

Other Forms of Eliglustat:

Eliglustat Related Antibodies

10 Publications Citing Use of MCE Eliglustat

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•Related Screening Libraries:

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Eliglustat Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Eliglustat Related Classifications

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