Eliglustat (GENZ-112638, Genz 99067, Cerdelga)

Cat No.:V6861 Purity: ≥98%
Eliglustat (GENZ-112638, Genz-99067, GENZ112638, Genz99067,Cerdelga) is a novel, potent, specific and orally bioactive glucocerebroside synthase inhibitor (IC50= 24 nM) approved by FDA in 2014 for the treatment for Gauchers disease.
Eliglustat (GENZ-112638, Genz 99067, Cerdelga) Chemical Structure CAS No.: 491833-29-5
Product category: Glucosylceramide Synthase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
500mg
Other Sizes

Other Forms of Eliglustat (GENZ-112638, Genz 99067, Cerdelga):

  • Eliglustat tartrate
  • Eliglustat-d15 tartrate (Genz 99067-d15 (tartrate))
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Eliglustat (GENZ-112638, Genz-99067, GENZ112638, Genz99067, Cerdelga) is a novel, potent, specific and orally bioactive glucocerebroside synthase inhibitor (IC50 = 24 nM) approved by FDA in 2014 for the treatment for Gaucher's disease.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Eliglustat tartrate has the ability to inhibit target enzymes and has good potency, with an IC50 of 24 nM [1]. The addition of Genz-112638 (0.6-1000 nM) to K562 or B16/F10 cells over a period of 72 hours led in a delayed suppression of GM1 and GM3 cell surfaces, with an average IC50 of 24 nM (range 14-1000 nM) in K562 cells. 34 nM), with an average IC50 value for GM3 inhibition in B16/F10 cells of 29 nM (range 12-34 nM). 48 nanometers)[1].
ln Vivo
In comparison to age-matched control animals, mice with a significant accumulation of substrate prior to therapy had lower levels of step ceramide and fewer Gaucher cells in their spleen, lung, and heart [1].
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
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H36N2O4
Molecular Weight
404.551
Exact Mass
404.2675
CAS #
491833-29-5
SMILES
InChI=1S/C23H36N2O4/c1-2-3-4-5-6-9-22(26)24-19(17-25-12-7-8-13-25)23(27)18-10-11-20-21(16-18)29-15-14-28-20/h10-11,16,19,23,27H,2-9,12-15,17H2,1H3,(H,24,26)/t19-,23-/m1/s1
InChi Key
N-((1R,2R)-1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-1-hydroxy-3-(pyrrolidin-1-yl)propan-2-yl)octanamide
InChi Code
FJZZPCZKBUKGGU-AUSIDOKSSA-N
Chemical Name
Genz-99067 GENZ-112638Cerdelga Genz99067 UNIIN0493335P3GENZ 112638Genz 99067 GENZ112638 Eliglustat tartrate eliglustat hemitartrate Eliglustat trade name Cerdelga.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~247.19 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4719 mL 12.3594 mL 24.7188 mL
5 mM 0.4944 mL 2.4719 mL 4.9438 mL
10 mM 0.2472 mL 1.2359 mL 2.4719 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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