5-Amino-1MQ Oral: Scientific Profile
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Small-molecule inhibitor of the enzyme Nicotinamide N-Methyltransferase (NNMT) designed for metabolic modulation and the increase of NAD+ in cellular and animal research models.
5-amino-1-methylquinolinium (5-Amino-1MQ) is a small, selective, cell-permeable molecule that acts as an inhibitor of NNMT, a cytosolic enzyme that catalyzes the methylation of nicotinamide. In metabolic research, overexpression of NNMT has been observed to correlate with decreased NAD+ levels and disruption of energy homeostasis. By inhibiting this enzyme, 5-Amino-1MQ favors conservation of the intracellular NAD+ pool, promoting the activity of sirtuins and other processes dependent on this cofactor.
Preclinical studies suggest that this compound possesses low toxicity and high efficacy in the prevention of adipogenesis and the promotion of fatty acid oxidation. By preventing the methylation of nicotinamide, 5-Amino-1MQ allows this precursor to be recycled more efficiently toward NAD+, reducing the accumulation of white adipose tissue and improving the basal metabolic rate in models subjected to hypercaloric diets.
Additionally, its role in musculoskeletal function is being investigated. The inhibition of NNMT in skeletal muscle satellite progenitor cells has shown potential to improve the cellular metabolic environment, accelerating regeneration and mitigating the muscle degradation associated with metabolic aging or inactivity. This oral presentation facilitates administration in chronic research models without requiring invasive procedures.
Mechanism of action
5-Amino-1MQ acts as a competitive inhibitor of the enzyme Nicotinamide N-Methyltransferase (NNMT). NNMT is responsible for converting nicotinamide into 1-methylnicotinamide, using S-adenosylmethionine (SAM) as the methyl donor. By blocking this process, the compound increases the levels of nicotinamide available to be recycled into NAD+ through the salvage pathway. The increase in intracellular NAD+ activates AMP-activated protein kinase (AMPK) and raises the activity of sirtuins, resulting in greater efficiency of the mitochondrial electron transport chain and an optimization in the utilization of lipids.
Mechanism summary
Selective inhibition of the NNMT enzyme to increase intracellular NAD+ concentrations and promote metabolic flexibility.
Clinical Studies (8)
- Selective and membrane-permeable small molecule inhibitors of nicotinamide N-methyltransferase reverse high fat diet-induced obesity in mice (Neelakantan, et al. · Biochemical Pharmacology · 2018) PMID 29155147.
- Reduced calorie diet combined with NNMT inhibition establishes a distinct microbiome in DIO mice (Dimet-Wiley, et al. · Scientific Reports · 2022) PMID 35013352.
- Nicotinamide N-methyltransferase inhibition mitigates obesity-related metabolic dysfunction. (Babula JJ, et al. · Diabetes Obes Metab · 2024) PMID 39161060.
- Development & validation of LC-MS/MS assay for 5-amino-1-methyl quinolinium in rat plasma: Application to pharmacokinetic and oral bioavailability studies. (Awosemo O, et al. · J Pharm Biomed Anal · 2021) PMID 34304009.
- NAD(+) metabolism enzyme NNMT in cancer-associated fibroblasts drives tumor progression and resistance to immunotherapy by modulating macrophages in urothelial bladder cancer. (Yang M, et al. · J Immunother Cancer · 2024) PMID 39067875.
- Small Molecule Inhibitors of Nicotinamide N-Methyltransferase Enzyme for the Treatment of Osteosarcoma and Merkel Cell Carcinoma: Potential for the Development of a Targeted Therapeutic Strategy. (Pompei V, et al. · Biomolecules · 2025) PMID 41301471.
- Small molecule inhibitor of nicotinamide N-methyltransferase shows anti-proliferative activity in HeLa cells. (Akar S, et al. · J Obstet Gynaecol · 2021) PMID 33645410.
- Nicotinamide N-methyltransferase in endothelium protects against oxidant stress-induced endothelial injury. (Campagna R, et al. · Biochim Biophys Acta Mol Cell Res · 2021) PMID 34153425.
Warnings
5-Amino-1MQ Oral is a research-use-only (RUO) compound; the following warnings and handling considerations apply to its laboratory use:
- Product exclusively for use in research laboratories
- Requires precise dose adjustment according to the molecular weight of the study subject
- Handle with appropriate personal protective equipment
- Models with known hypersensitivity to 5-Amino-1MQ
- Pregnant or lactating models (insufficient data)
- Models under 18 years old
- Models with severe hepatic or renal insufficiency
- Models with active neoplasia
- Models with severe gastrointestinal disorders
Technical data
- CAS
- 685079-15-6
- Molecular formula
- C10H11N2
- Molecular weight
- 159.21 Da
- Compound type
- metabolic
- Storage
- 15-25°C dry
- Shelf life (lyophilized)
- 24 months
- Shelf life (reconstituted)
- Not applicable (solid oral presentation)
- Light-sensitive
- No
Available for research
5-Amino-1MQ Oral is available as a research reagent (RUO):
Frequently asked questions about 5-Amino-1MQ Oral
What is Oral 5-Amino-1MQ?
Small-molecule inhibitor of the enzyme Nicotinamide N-Methyltransferase (NNMT) designed for metabolic modulation and the increase of NAD+ in cellular and animal research models.
What is the mechanism of action of Oral 5-Amino-1MQ?
Selective inhibition of the NNMT enzyme to increase intracellular NAD+ concentrations and promote metabolic flexibility.
What is 5-Amino-1MQ Oral investigated for?
In preclinical research, 5-Amino-1MQ Oral is studied mainly in: Research on mitochondrial weight reduction; Modulation of systemic lipid metabolism; Increased expression of glucose transporters (GLUT4). Material exclusively for scientific research.
What are the chemical properties of 5-Amino-1MQ Oral?
Molecular formula C10H11N2; molecular weight 159.21 Da; CAS number 685079-15-6.
How is 5-Amino-1MQ Oral stored?
Storage conditions: 15-25°C dry; lyophilized stability: 24 months; once reconstituted: Not applicable (solid oral presentation).
What routes of administration are studied for 5-Amino-1MQ Oral?
In research models the following are described: Oral. Use is exclusively for scientific research.
