Description
Eliglustat hemitartrate is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM.
Product information
CAS Number: 928659-70-5
Molecular Weight: 959.17
Formula: C50H78N4O14
Chemical Name: (2R,3R)-2,3-dihydroxybutanedioic acid; bis(N-[(1R,2R)-1-(2,3-dihydro-1,4-benzodioxin-6-yl)-1-hydroxy-3-(pyrrolidin-1-yl)propan-2-yl]octanamide)
Smiles: CCCCCCCC(=O)N[C@H](CN1CCCC1)[C@H](O)C1=CC2OCCOC=2C=C1.CCCCCCCC(=O)N[C@H](CN1CCCC1)[C@H](O)C1=CC2OCCOC=2C=C1.OC(=O)[C@H](O)[C@@H](O)C(O)=O
InChiKey: KUBARPMUNHKBIQ-VTHUDJRQSA-N
InChi: InChI=1S/2C23H36N2O4.C4H6O6/c2*1-2-3-4-5-6-9-22(26)24-19(17-25-12-7-8-13-25)23(27)18-10-11-20-21(16-18)29-15-14-28-20;5-1(3(7)8)2(6)4(9)10/h2*10-11,16,19,23,27H,2-9,12-15,17H2,1H3,(H,24,26);1-2,5-6H,(H,7,8)(H,9,10)/t2*19-,23-;1-,2-/m111/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 110 mg/mL (114.68 mM; Need ultrasonic). H2O : ≥ 50 mg/mL (52.13 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Eliglustat tartrate shows good potency with an IC50 of 24 nM and specificity against the target enzyme.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).
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.
Products are for research use only. Not for human use.
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