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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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E413855-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $116.90 | |
E413855-10mg | 10mg | In stock | $155.90 | |
E413855-25mg | 25mg | In stock | $234.90 | |
E413855-50mg | 50mg | In stock | $312.90 | |
E413855-100mg | 100mg | In stock | $574.90 |
Glucosylceramide Synthase Inhibitors
Synonyms | EN300-259910 | Genz 99067 | s7852 | 1000191-50-3 | CCG-101413 | CHEBI:82752 | Genz-99067 | Z825742124 | GLXC-90436 | AC-35323 | F53213 | DB09039 | N-((1R,2R)-1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-1-hydroxy-3-(pyrrolidin-1-yl)propan-2-yl)octanamide | STL |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Eliglustat (GENZ-112638) inhibits glucosylceramide synthase(GCS) (IC50=20 nM in intact MDCK cells), thus reducing the load of glucosylceramide influx into the lysosome. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Product Description | Information Eliglustat Eliglustat (GENZ-112638) inhibits glucosylceramide synthase(GCS) (IC50=20 nM in intact MDCK cells), thus reducing the load of glucosylceramide influx into the lysosome. Targets glucosylceramide synthase (In intact MDCK cells) 20 nM In vitro Eliglustat tartrate is designed and developed to inhibit glucosylceramide synthase, the enzyme that catalyzes the formation of glucosylceramide from UDP-glucose and ceramide.The inhibition of glucosylceramide synthase by eliglustat tartrate is highly specific. Eliglustat tartrate displays limited or no activity against a variety of glycosidases. Additionally, no inhibition of sucrase or maltase is observed at drug concentrations up to 10 μM. In vivo Preclinical studies in normal mice, rats and dogs with i.v. and oral administration demonstrates significant dose-related decreases in spleen, kidney and liver glucosylceramide content, consistent with prior observations with the palmitoyl homologue.In rodents, Genz-112638 is rapidly metabolized with a half-life of 15–45 minutes. |
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IUPAC Name | N-[(1R,2R)-1-(2,3-dihydro-1,4-benzodioxin-6-yl)-1-hydroxy-3-pyrrolidin-1-ylpropan-2-yl]octanamide |
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INCHI | 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 | FJZZPCZKBUKGGU-AUSIDOKSSA-N |
Canonical SMILES | CCCCCCCC(=O)NC(CN1CCCC1)C(C2=CC3=C(C=C2)OCCO3)O |
Isomeric SMILES | CCCCCCCC(=O)N[C@H](CN1CCCC1)[C@@H](C2=CC3=C(C=C2)OCCO3)O |
PubChem CID | 23652731 |
Molecular Weight | 404.54 |
PubChem CID | 23652731 |
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CAS Registry No. | 491833-29-5 |
ChEMBL Ligand | CHEMBL2110588 |
Wikipedia | Eliglustat |
DrugCentral Ligand | 4834 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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H2229230 | Certificate of Analysis | Jun 21, 2022 | E413855 |
H2229231 | Certificate of Analysis | Jun 21, 2022 | E413855 |
H2229232 | Certificate of Analysis | Jun 21, 2022 | E413855 |
H2229234 | Certificate of Analysis | Jun 21, 2022 | E413855 |
Solubility | Solubility (25°C) In vitro DMSO: 80 mg/mL (197.75 mM); Ethanol: 80 mg/mL (197.75 mM); Water: Insoluble; |
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1. Lukina E, Watman N, Arreguin EA, Dragosky M, Iastrebner M, Rosenbaum H, Phillips M, Pastores GM, Kamath RS, Rosenthal DI et al.. (2010) Improvement in hematological, visceral, and skeletal manifestations of Gaucher disease type 1 with oral eliglustat tartrate (Genz-112638) treatment: 2-year results of a phase 2 study.. Blood, 116 (20): (4095-8). [PMID:20713962] |
2. Larsen SD, Wilson MW, Abe A, Shu L, George CH, Kirchhoff P, Showalter HD, Xiang J, Keep RF, Shayman JA. (2012) Property-based design of a glucosylceramide synthase inhibitor that reduces glucosylceramide in the brain.. J Lipid Res, 53 (2): (282-91). [PMID:22058426] |
3. Lukina E, Watman N, Dragosky M, Pastores GM, Arreguin EA, Rosenbaum H, Zimran A, Angell J, Ross L, Puga AC et al.. (2014) Eliglustat, an investigational oral therapy for Gaucher disease type 1: Phase 2 trial results after 4 years of treatment.. Blood Cells Mol Dis, 53 (4): (274-6). [PMID:24835462] |