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Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Sinbaglustat (OGT2378) is a dual inhibitor of glucosylceramide synthase ( GCS ) and non-lysosomal glucosyl ceramidase ( GBA2 ). Sinbaglustat is an orally available N-alkyl iminosugar that crosses the blood-brain barrier. Sinbaglustat can be used for the research of central neurodegenerative diseases associated with lysosomal dysfunctions.
In Vitro
Sinbaglustat (OGT2378; 20 μM) reduces the synthesis of glucosylceramide and ganglioside by 93% and >95% in MEB4 melanoma cells compared with untreated MEB4 cells, respectively, without either cytotoxic or antiproliferative effects. GBA2 is an enzyme involved in the catabolism of glycosphingolipids (GSLs). Sinbaglustat is 50-fold more potent in inhibiting GBA2 than GCS. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Sinbaglustat (OGT2378; administered p.o., in the powdered chow, at a dose of 2500 mg/kg/day, corresponding to 35-40 mg of Sinbaglustat per mouse per day) is highly effective in impeding melanoma tumor growth in vivo. The effectiveness of p.o. Sinbaglustat in this murine model suggests that inhibition of glycosphingolipid synthesis is a promising approach to inhibit tumor progression . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female syngeneic C57BL/6 mice, 6-8 weeks old bearing MEB4 melanoma tumor Dosage: 35-40 mg per mouse per day Administration: Administered p.o., in the powdered chow, at a dose of 2500 mg/kg/day Result: Inhibited MEB4 melanoma tumor growth in a syngeneic, orthotopic murine model.
Form:Solid
| Canonical Smiles | CCCCCN1C[C@@H]([C@H]([C@@H]([C@@H]1CO)O)O)O |
|---|---|
| Isomeric SMILES | CCCCCN1C[C@@H]([C@H]([C@@H]([C@@H]1CO)O)O)O |
| PubChem CID | 9859470 |
| Molecular Weight | 233.30 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Solubility | DMSO : 83.33 mg/mL (357.18 mM; Need ultrasonic) |
|---|---|
| Molecular Weight | 233.300 g/mol |
| XLogP3 | -0.100 |
| Hydrogen Bond Donor Count | 4 |
| Hydrogen Bond Acceptor Count | 5 |
| Rotatable Bond Count | 5 |
| Exact Mass | 233.163 Da |
| Monoisotopic Mass | 233.163 Da |
| Topological Polar Surface Area | 84.200 Ų |
| Heavy Atom Count | 16 |
| Formal Charge | 0 |
| Complexity | 202.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 4 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
