深圳欣博盛生物科技有限公司

Melatonin Lipodisq™ Sterile Solution

N-Acetyl-5-methoxytryptamine; NSC 56423; NSC 113928; Regulin

Melatonin (high purity) Lipodisq Sterile Solution is a ready-to-use nano-formulated aqueous solution. Melatonin, an evolutionarily ancient derivative of serotonin with hormonal properties, is the main neuroendocrine secretory product of the pineal gland. It regulates circadian rhythmicity and also exerts anti-oxidative, anti-inflammatory, immunomodulatory, and anti-tumor capacities. Melatonin levels in individuals increase from birth and peak around puberty. Its synthesis and levels decline in middle-aged and most elderly individuals along with a simultaneous reduction in the urinary excretion of its metabolites. Moreover, it stimulates antioxidant defense systems in the brain. The decline in melatonin production in aged individuals is itself a significant factor that may contribute to age-related neurodegenerative disease processes and has been suggested as one of the primary reasons for the development of Alzheimer Disease (AD). Melatonin exerts antibacterial activities not only on classic Gram-negative and Gram-positive bacteria, but also on members of other bacterial groups, such as Mycobacterium tuberculosis. In recent years, an increasing number of studies have described the anticancer effects of melatonin. Melatonin is also a mitophagy regulator. It may exert an essential effect on mitochondrial physiology and facilitates mitochondrial function. A central mechanism by which melatonin protects mitochondria is by restoring the mitochondrial membrane potential (MMP) through blocking mitochondrial permeability transition pore (mPTP) opening under stress and activating uncoupling proteins (UCPs) to marginally decrease MMP under normal conditions. Melatonin Lipodisq is based on a nanoparticle (11-40nm) drug delivery system comprising a discoidal phospholipid bilayer membrane stabilized by a chaperone molecule annulus. Internal properties of the phospholipid membrane support the disposition and stabilization of drug molecule candidates and preserve the native conformation of membrane molecules. The resulting encapsulated actives are rendered water-soluble and specialised for intra-cellular penetration/delivery via endosomal uptake mechanisms. Lipodisq solutions show a good safety profile and are suitable for in vitro and in vivo investigations.

1mg/ml (0.1% w/vol)

+4°C

Ambient

232.28

liquid

Liquid, detergent-free discoidal nano-formulation made of styrene-maleic acid lipid particles (SMALP), lecithin and sterile water.

Stable for at least 1 year after receipt when stored at +4°C.

瑞士

>95% (HPLC)

Discoidal nano-particles can incorporate hydrophobic, poorly water-soluble compounds, such as lipids, lipoproteins and glycolipids. - Cell culture tested (human macrophage cell line) (MTT). - Recommended starting dilution: 1:200 or higher. - Optimal working concentrations depend on the applications and need to be determined. - Published procedures using Lipodisq formulations (Curcumin and IAXO TLR4 antagonists) in vivo rodent models at 3-10mg/kg. Recommended route of administration is subcutaneous (s.c.) with oral or nasal application as a possible alternative, which needs to be optimized.

73-31-4

C13H16N2O2

Soluble in water, PBS, Tris and other physiological solutions as formulated in a proprietary, thermostable, aqueous lipid nanoparticulate formulation (Lipodisq).