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Formula | C23H36N2O4 |
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Molecular Weight | 404.54 | CAS No. | 491833-29-5 | ||||
Solubility (25°C)* | In vitro | DMSO | 80 mg/mL (197.75 mM) | ||||
Ethanol | 80 mg/mL (197.75 mM) | ||||||
Water | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Eliglustat (GENZ-112638) inhibits glucosylceramide synthase(GCS) (IC50=20 nM in intact MDCK cells), thus reducing the load of glucosylceramide influx into the lysosome. | ||
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Targets |
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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[1]. | ||
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[1].In rodents, Genz-112638 is rapidly metabolized with a half-life of 15–45 minutes[2]. |
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Eliglustat exerts anti-fibrotic effects by activating SREBP2 in TGF-β1-treated myofibroblasts derived from patients with idiopathic pulmonary fibrosis [ Eur J Pharmacol, 2024, 966:176366] | PubMed: 38296153 |
Glucose-dependent glycosphingolipid biosynthesis fuels CD8+ T cell function and tumor control [ bioRxiv, 2024, 2024.10.10.617261] | PubMed: 39464161 |
Glucosylceramide Synthase Inhibitors Induce Ceramide Accumulation and Sensitize H3K27 Mutant Diffuse Midline Glioma to Irradiation [ Int J Mol Sci, 2023, 24(12)9905] | PubMed: 37373053 |
Tyrosine-phosphorylation and activation of glucosylceramide synthase by v-Src: Its role in survival of HeLa cells against ceramide [ Biochim Biophys Acta Mol Cell Biol Lipids, 2021, 1866(1):158817] | PubMed: 32980536 |
Amyloid Beta-Peptide 25-35 (Aβ25-35) Induces Cytotoxicity via Multiple Mechanisms: Roles of the Inhibition of Glucosylceramide Synthase by Aβ25-35 and Its Protection by D609 [ Biol Pharm Bull, 2021, 44(10):1419-1426] | PubMed: 34602551 |
N-Glycan Modification in Covid-19 Pathophysiology: In vitro Structural Changes with Limited Functional Effects [ J Clin Immunol, 2020, 1-10] | PubMed: 33245474 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.