Innaxon

Metformin Lipodisq™ Sterile Solution

CHF 244.00

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IAX-700-103-L0011 mlCHF 244.00

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Product Details
Synonyms	1,1-Dimethylbiguanide . HCl; NSC 91485; DMGG; LA 6023
Product Type	Chemical
Properties
Formula	C₄H₁₁N₅ . HCl
MW	129.2 . 36.5
CAS	1115-70-4
RTECS	DU1800000
Purity Chemicals	≥95% (HPLC)
Appearance	Colourless clear aqueous solution
Solubility	Soluble in water, PBS, Tris and other physiological solutions as formulated in a proprietary, thermostable, aqueous lipid nanoparticulate formulation (Lipodisq).
Reconstitution	Avoid the use of buffers with divalent ions such as Ca or Mg or pH <6.5 or >8.0, which can cause particle instability. Unformulated metformin is soluble in water or DMSO.
Formulation	Liquid, detergent-free discoidal nano-formulation made of styrene-maleic acid lipid particles (SMALP), lecithin and sterile water.
Concentration	1mg/ml (0.1% w/vol)
Biological Activity	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.
Declaration	Manufactured by Innaxon.
Other Product Data	Click here for Original Manufacturer Product Datasheet: Our product description may differ slightly from the original manufacturers product datasheet. Lipodisq™ technology is covered by one or more of the following patents owned by Malvern Cosmeceutics Limited: AU2006253886, CA2611144, CN101184473B, EP1890675, GB2426703, IN261468, JP5142898, US8623414 and WO/2021/005340A1 pending. The purchaser is licensed under those patents to use these assemblies for the purpose of research and development only, but not for the purpose of delivery of agents for clinical use to humans or veterinary use to animals for therapeutic, diagnostic or prophylactic purposes, which uses are specifically prohibited.
InChi Key	OETHQSJEHLVLGH-UHFFFAOYSA-N
Smiles	CN(C(NC(N)=N)=N)C.Cl
Shipping and Handling
Shipping	AMBIENT
Short Term Storage	+4°C
Long Term Storage	-20°C
Handling Advice	Keep cool and dry. Avoid skin and eye contact.
Use/Stability	Stable for at least 1 year after receipt when stored at +4°C.
Documents
MSDS	Download PDF
Product Specification Sheet
Datasheet	Download PDF

Product-specific References

Description

Metformin Lipodisq Sterile Solution is a ready-to-use nano-formulated aqueous solution.
Metformin is an antihyperglycemic agent of the biguanide class, used for the management of type II diabetes and is currently prescribed to at least 120 million people worldwide. It is an AMPK activator and a mitochondrial electron transport chain complex I inhibitor, reducing mitochondrial reactive oxygen species (ROS). This antidiabetic and anti-hyperglycemic agent reduces blood glucose levels, improves insulin sensitivity, and decreases insulin resistance. Insulin sensitizer in non-alcoholic fatty liver disease (NAFLD). Increases plasma concentrations of the glucose-lowering gut incretin hormone glucagon-like peptide-1 (GLP-1), which may contribute to metformin’s glucose-lowering effect. An anticancer agent with antiproliferative and proapoptotic activity in cancer cell lines. Autophagy activator. Targets brown adipose tissue (BAT) in vivo and reduces oxygen consumption. Anti-inflammatory agent by inhibition of nuclear factor κB (NF-κB) via AMPK-dependent and independent pathways. Also described to inhibit NLRP3 inflammasome activation, subsequent caspase-1 cleavage and interleukin-1β secretion. Since the emergence of SARS-CoV-2, Metformin has been investigated as a prophylactic agent for the prevention of COVID-19.
Metformin 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 specialized 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.

Product References

Cellular and molecular mechanisms of metformin: an overview: B. Viollet, et al.; Clin. Sci. 122, 253 (2012)
Metformin in 2019: J. Flory & K. Lipska; JAMA 321, 1926 (2019)
Metformin Use Is Associated With Reduced Mortality in a Diverse Population With COVID-19 and Diabetes: A.B. Crouse, et al.; Front. Endocrinol. 11, 600439 (2021)
Metformin inhibition of mitochondrial ATP and DNA synthesis abrogates NLRP3 inflammasome activation and pulmonary inflammation: J. Flory & K. Lipska; Immunity 54, 1463 (2021)
Metformin in Patients With COVID-19: A Systematic Review and Meta-Analysis: Y. Li, et al.; Front. Med. 8, 704666 (2021)
Outpatient metformin use is associated with reduced severity of COVID-19 disease in adults with overweight or obesity: C.T. Bramante, et al.; J. Med. Virol. 93, 4273 (2021)
Metformin inhibition of mitochondrial ATP and DNA synthesis abrogates NLRP3 inflammasome activation and pulmonary inflammation: H. Xian, et al.; Immunity 54, 1463 (2021)
Metformin and Covid-19: Focused Review of Mechanisms and Current Literature Suggesting Benefit: S. Ibrahim, et al.; Front. Endocrinol. 12, 587801 (2021)

General References for Lipodisq™ Technology:

Responsive Hydrophobically Associating Polymers: A Review of Structure and Properties: S.R. Tonge & B.J. Tighe; Adv. Drug Deliv. Rev. 53, 109 (2001)
Detergent-free formation and physico-chemical characterization of nanosized lipidpolymer complexes: Lipodisq; M.C. Orwick, et al.; Angew. Chem. 51, 4653 (2012)
Physicochemical Characterization, Toxicity and In Vivo Biodistribution Studies of a Discoidal, Lipid-Based Drug Delivery Vehicle: Lipodisq Nanoparticles Containing Doxorubicin: M.L. Torgersen, et al.; J. Biomed. Nanotechnol. 16, 41 (2020)
Applications of Synthetic Polymer Discoidal Lipid Nanoparticles to Biomedical Research: M. Tanaka; Chem. Pharm. Bull. 70, 507 (2022)
Mechanisms of Formation, Structure, and Dynamics of Lipoprotein Discs Stabilized by Amphiphilic Copolymers: A Comprehensive Review: P.S. Orekhov, et al.; Nanomaterials 12, 361 (2022)

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