Eliglustat (C09-0880-894)

InformationEliglustat Eliglustat (GENZ-112638) inhibits glucosylceramide synthase(GCS) (IC50=20 nM in intact MDCK cells), thus reducing the load of glucosylceramide influx into the lysosome.Targetsglucosylceramide synthase (In intact MDCK cells) 20 nMIn vitroEliglustat 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 vivoPreclinical 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. Specification: 0.98 Molecular Formula: C23H36N2O4 Molecular Weight: 404.54 PubChem CID: 23652731 Isomeric SMILES: CCCCCCCC(=O)N[C@H](CN1CCCC1)[C@@H](C2=CC3=C(C=C2)OCCO3)O Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/E413855-SCI_09b2739b005ce7f92751af5165146d83.pdf