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Sinbaglustat (OGT-2378; OGT2378) is a novel and potent dual inhibitor of GCS (Glucosyl Ceramide Synthase Inhibitor) and non-lysosomal glucosyl ceramidase (GBA2) with the potential to be used for central neurodegenerative diseases associated with lysosomal dysfunctions.
| ln Vitro |
In comparison to untreated MEB4 cells, sinbaglustat (OGT2378; 20 μM) decreases glucosylceramide and ganglioside production by 93% and >95%, respectively, in MEB4 melanoma cells[1]. It has no cytotoxic or antiproliferative effects. An enzyme called GBA2 is involved in the breakdown of GSLs, or glycosphingolipids. The inhibitory power of sinbaglustat over GCS is 50 times greater[2].
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| ln Vivo |
Highly efficient at inhibiting the formation of melanoma tumors in vivo is Sinbaglustat (OGT2378; po, in the powdered chow, at a dose of 2500 mg/kg/day, corresponding to 35-40 mg of Sinbaglustat each mouse per day). Because po Sinbaglustat works so well in this mouse model, it appears that blocking the synthesis of glycosphingolipids is a viable way to stop tumor growth[1].
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| Animal Protocol |
Animal/Disease Models: Female syngeneic C57BL/6 mice, 6-8 weeks old bearing MEB4 melanoma tumor[1]
Doses: 35- 40 mg per mouse per day Route of Administration: Administered po, in the powdered chow, at a dose of 2500 mg/kg/day Experimental Results: Inhibited MEB4 melanoma tumor growth in a syngeneic, orthotopic murine model. |
| References |
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| Molecular Formula |
C11H23NO4
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|---|---|
| Molecular Weight |
233.3
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| Exact Mass |
233.163
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| CAS # |
441061-33-2
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| PubChem CID |
9859470
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
-0.1
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
16
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| Complexity |
202
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| Defined Atom Stereocenter Count |
4
|
| SMILES |
CCCCCN1C[C@@H]([C@H]([C@@H]([C@@H]1CO)O)O)O
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| InChi Key |
HCZQIIVHWYFIPW-UKKRHICBSA-N
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| InChi Code |
InChI=1S/C11H23NO4/c1-2-3-4-5-12-6-9(14)11(16)10(15)8(12)7-13/h8-11,13-16H,2-7H2,1H3/t8-,9-,10+,11+/m0/s1
|
| Chemical Name |
(2S,3R,4R,5S)-2-(hydroxymethyl)-1-pentylpiperidine-3,4,5-triol
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| Synonyms |
OGT 2378 OGT2378 OGT-2378
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~357.18 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (26.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2863 mL | 21.4316 mL | 42.8633 mL | |
| 5 mM | 0.8573 mL | 4.2863 mL | 8.5727 mL | |
| 10 mM | 0.4286 mL | 2.1432 mL | 4.2863 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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