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Eliglustat tartrate

Cat. No. M9733
Eliglustat tartrate Structure
Synonym:

Genz-112638; Eliglustat hemitartrate

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 110  USD110 In stock
10mg USD 150  USD150 In stock
25mg USD 220  USD220 In stock
50mg USD 310  USD310 In stock
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Quality Control & Documentation
Biological Activity

Eliglustat tartrate is a potent and selective glucosylceramide synthase inhibitor with IC50 of 24 nM. 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.

Chemical Information
Molecular Weight 959.17
Formula C50H78N4O14
CAS Number 928659-70-5
Solubility (25°C) Water ≥ 48 mg/mL
DMSO ≥ 48 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Annalisa Sechi, et al. Ther Clin Risk Manag. Profile of eliglustat tartrate in the management of Gaucher disease

[2] Kerry Anne McEachern, et al. Mol Genet Metab. A specific and potent inhibitor of glucosylceramide synthase for substrate inhibition therapy of Gaucher disease

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Keywords: Eliglustat tartrate, Genz-112638; Eliglustat hemitartrate supplier, inhibitors, activators


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