Glycerol dioleate
Based on 1 Customer Validation
Glycerol dioleate is a lipid capable of forming Lyotropic Liquid Crystal (LLC). When formulated with phosphatidylcholine and exposed to aqueous media, glycerol dioleate constructs an inverted hexagonal (HII) phase structure with sustained-release properties. The in-situ forming gel prepared by optimizing glycerol dioleate with phosphatidylcholine and N-methyl-2-pyrrolidone enables stable release of Risperidone (HY-11018) for up to 60 days in vitro and in vivo. Glycerol dioleate causes minimal side effects in rabbits, making it an ideal carrier component for the development of antischizophrenia agents.Note: Lyotropic liquid crystals (Lyotropic Liquid Crystal, LLC) are ordered fluid phases self-assembled by amphipathic molecules (e.g., lipids, surfactants) in solvents (usually water) at specific concentrations.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 25637-84-7
- Formula: C39H72O5
- Molecular Weight:621.00
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Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Biological Activity
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>10 μM
Compound: 7
|
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 28445049] |
| HepG2 | IC50 |
>10 μM
Compound: 7
|
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 28445049] |
| MDA-MB-231 | IC50 |
>10 μM
Compound: 7
|
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 28445049] |
| Neutrophil | IC50 |
>10 μM
Compound: 7
|
Anti-inflammatory activity in human neutrophils assessed as inhibition of fMLF/CB-induced elastase release by measuring degranulation of azurophilic granules using MeOSuc-Ala-Ala-ProVal-p-nitroanilide as substrate preincubated for 5 mins followed by CB/fM
Anti-inflammatory activity in human neutrophils assessed as inhibition of fMLF/CB-induced elastase release by measuring degranulation of azurophilic granules using MeOSuc-Ala-Ala-ProVal-p-nitroanilide as substrate preincubated for 5 mins followed by CB/fM
|
[PMID: 28445049] |
| Neutrophil | IC50 |
>10 μM
Compound: 7
|
Anti-inflammatory activity in human neutrophils assessed as inhibition of fMLF/CB-induced superoxide anion generation preincubated for 5 mins followed by CB stimulation for 3 mins and subsequent fMLF stimulation for 10 mins by spectrophotometric method
Anti-inflammatory activity in human neutrophils assessed as inhibition of fMLF/CB-induced superoxide anion generation preincubated for 5 mins followed by CB stimulation for 3 mins and subsequent fMLF stimulation for 10 mins by spectrophotometric method
|
[PMID: 28445049] |
Glycerol dioleate-based LLC formulations (PC:GDO ratio of 2.1:1, containing 30% NMP (w/w); stable for up to 60 days) achieve uniform, sustained release of risperidone for up to 60 days in vitro[1].
Glycerol dioleate-based LLC formulations degrade and release free oleic acid in vitro, with a cumulative release of 16.68 mg in 75 mL of culture medium over 60 days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Tmax | Cmax | T1/2 | MRT | AUC0-t |
|---|---|---|---|---|---|---|---|
| Rabbit[1] | 500 mg mg/L | s.c. | 366 ± 4.18 h | 47.31 ± 3.12 ng/mL | 389.22 ± 7.22 h | 850.51 ± 10.48 h | 57523.90 ± 49.76 ng·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:New Zealand rabbit (male, 2 ± 0.1 kg)[1]
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Dosage:500 mg of glycerol dioleate-based LLC formulation (containing 25 mg risperidone)
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Administration:s.c.; single injection
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Result:Formed an opaque, self-assembling gel-like mesophase immediately at the subcutaneous injection site. Reached a maximum risperidone serum concentration (Cmax) of 47.31 ± 3.12 ng/mL at 366 ± 4.18 hours (Tmax). Achieved an elimination half-life (t1/2) of 389.22 ± 7.22 hours, a mean residence time (MRT) of 850.51 ± 10.48 hours, and an area under the serum concentration-time curve (AUC0-t) of 57523.90 ± 49.76 ng·h/mL. Maintained uniform, continuous risperidone serum concentrations for 60 days. Caused subcutaneous adipose tissue necrosis with mononuclear inflammatory cell infiltration at the injection site, but showed no abnormalities, necrosis, hemorrhage, or inflammatory cell infiltration in heart, kidney, or liver tissues.
Chemical Information
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CAS No. 25637-84-7
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Appearance Oil
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Molecular Weight 621.00
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Formula C39H72O5
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Color White to off-white
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SMILES
CCCCCCCC/C=C\CCCCCCCC(OC(COC(CCCCCCC/C=C\CCCCCCCC)=O)CO)=O.CCCCCCCC/C=C\CCCCCCCC(OCC(COC(CCCCCCC/C=C\CCCCCCCC)=O)O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (161.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (268 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6103 mL | 8.0515 mL | 16.1031 mL | 40.2576 mL |
| 5 mM | 0.3221 mL | 1.6103 mL | 3.2206 mL | 8.0515 mL | |
| 10 mM | 0.1610 mL | 0.8052 mL | 1.6103 mL | 4.0258 mL | |
| 15 mM | 0.1074 mL | 0.5368 mL | 1.0735 mL | 2.6838 mL | |
| 20 mM | 0.0805 mL | 0.4026 mL | 0.8052 mL | 2.0129 mL | |
| 25 mM | 0.0644 mL | 0.3221 mL | 0.6441 mL | 1.6103 mL | |
| 30 mM | 0.0537 mL | 0.2684 mL | 0.5368 mL | 1.3419 mL | |
| 40 mM | 0.0403 mL | 0.2013 mL | 0.4026 mL | 1.0064 mL | |
| 50 mM | 0.0322 mL | 0.1610 mL | 0.3221 mL | 0.8052 mL | |
| 60 mM | 0.0268 mL | 0.1342 mL | 0.2684 mL | 0.6710 mL | |
| 80 mM | 0.0201 mL | 0.1006 mL | 0.2013 mL | 0.5032 mL | |
| 100 mM | 0.0161 mL | 0.0805 mL | 0.1610 mL | 0.4026 mL |