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  4. Glycerol dioleate

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.

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Glycerol dioleate

Glycerol dioleate Chemical Structure

CAS No. : 25637-84-7

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Glycerol dioleate Related Antibodies

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  • Purity & Documentation

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Description

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[1].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[1].

In Vitro

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.

Glycerol dioleate Related Antibodies
Parmacokinetics
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
In Vivo

A glycerol dioleate-based LLC formulation (500 mg; s.c.; single injection) achieves uniform and sustained maintenance of serum risperidone concentrations in rabbits for up to 60 days, with an elimination half-life of 389.22 h, and causes no histopathological damage to major organs[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: New Zealand rabbit (male, 2 ± 0.1 kg)[1]
Dosage: 500 mg of glycerol dioleate-based LLC formulation (containing 25 mg risperidone)
Administration: s.c.; single injection
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.
Molecular Weight

621.00

Formula

C39H72O5
CAS No.
Appearance

Oil

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6103 mL 8.0515 mL 16.1031 mL
5 mM 0.3221 mL 1.6103 mL 3.2206 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
Purity & Documentation
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
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Glycerol dioleate Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Glycerol dioleate25637-84-7Biochemical Assay Reagentssustained drug delivery systemsschizophreniapolarized optical microscopyphosphatidylcholinein-situ forming gelrisperidonereverse hexagonal (HII) phaseN-methyl-2-pyrrolidonerabbitlyotropic liquid crystalInhibitorinhibitorinhibit

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