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Eliglustat  (Synonyms: Genz 99067)

Cat. No.: HY-14885 Purity: 99.95%
COA Handling Instructions

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

Eliglustat Chemical Structure

CAS No. : 491833-29-5

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 106 In-stock
Solution
10 mM * 1 mL in DMSO USD 106 In-stock
Solid
1 mg USD 66 In-stock
5 mg USD 119 In-stock
10 mg USD 158 In-stock
50 mg USD 317 In-stock
100 mg USD 581 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Eliglustat:

Eliglustat Related Antibodies

Top Publications Citing Use of Products

    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.

    • 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.

    Eliglustat Related Antibodies
    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

    Appearance

    Solid

    Formula

    C23H36N2O4
    CAS No.
    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)

    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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

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

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

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.95%

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

    Handling Instructions (2659 KB)
    References
    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
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    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.

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    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
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    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    Eliglustat491833-29-5Genz 99067Genz99067Genz-99067OthersInhibitorinhibitorinhibit

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