5-Amino-1MQ 50mg x 25ct

Compound Name: 5-Amino-1-MQ

Synonyms: 5-amino-1-methylquinolinium, 5MQ

CAS Number: 685079-15-6

Molecular Formula: C₁₀H₁₁N₂+

Molecular Weight: ~159.21 g/mol

Structure: Quinoline core with a methyl group at the 1-position and an amino group at the 5-position⁴.

Peptide Sequence: N/A; Not a peptide

Chemical Structure:

Source: PubChem

Mechanism of Action: 5-Amino-1MQ acts as a highly selective inhibitor of the enzyme nicotinamide N-methyltransferase (NNMT), blocking the methylation of nicotinamide (a form of vitamin B3) using S-adenosyl methionine (SAM) as a methyl donor. By inhibiting NNMT, 5-Amino-1MQ increases cellular SAM and NAD+ levels, enhances NAD+ salvage pathway flux, activates SIRT-1, boosts oxidative phosphorylation (OXPHOS), and influences cellular energy homeostasis and epigenetic modifications. These metabolic shifts increase energy expenditure, suppress lipogenesis, and rejuvenate muscle stem cell function, providing a unique mechanism for combating obesity, fatty liver, and age-related muscle decline^1-3.

Biological Activity: In animal models, 5-Amino-1MQ markedly reduces body weight and fat mass, improves insulin sensitivity, and reverses diet-induced hepatic steatosis and adiposity^2,3. In aged mice, it nearly doubles muscle fiber size and enhances muscle stem cell proliferation, resulting in superior muscle regeneration post-injury¹. At the cellular level, 5-Amino-1MQ promotes differentiation and metabolic reprogramming of precursor cells while being well-tolerated in repeated dosing studies⁴. It exhibits an IC₅₀ of approximately 1 μM for NNMT inhibition⁴, with favorable pharmacokinetic properties.

Storage: Store at 4°C in a dry, sterile, light-protected environment.

Drug Categories: Experimental metabolic modulator, NNMT inhibitor, anti-obesity agent, muscle regenerative enhancer.

Additional Notes: 5-Amino-1MQ is for research use only.

Summary Table:

Disclaimer: For Research Use Only. Not intended for human or veterinary use. This compound is supplied solely for laboratory and R&D purposes.

Detailed Product Description

5-Amino-1-Methylquinolinium (5-Amino-1MQ) is a first-in-class, selective NNMT inhibitor designed for research into metabolic regulation, obesity, diabetes, nonalcoholic fatty liver disease, and age-associated muscle degeneration. Preclinical studies have demonstrated that 5-Amino-1MQ effectively reprograms metabolism in key energy-regulating tissues: it counteracts obesity and associated fat accumulation, reduces pathological liver fat, and enhances the regenerative potential of aged skeletal muscle^1-3. By blocking NNMT activity, it increases critical cellular metabolites (SAM, NAD⁺) that drive downstream increases in energy expenditure and metabolic health^1-4. Further, it activates muscle stem cells, promoting tissue regeneration, and reverses insulin resistance in relevant animal models, all with good systemic tolerability^1,2. In preclinical studies, 5-Amino-1MQ provides a powerful tool to dissect the cellular and molecular consequences of NNMT inhibition. Its unique profile makes it an attractive compound for exploring the therapy of metabolic disease and muscle aging, as well as evaluating the intricate links between metabolism, epigenetics, and tissue function^1-4.

Research Highlights

• Metabolic Regulation and Anti-Obesity Effects: Potent inhibition of nicotinamide N-methyltransferase (NNMT) increases cellular NAD⁺ and S-adenosylmethionine (SAM) levels, enhances polyamine flux, boosts energy expenditure, and suppresses lipogenesis; in diet-induced obese mice, 5-Amino-1-MQ significantly reduces total body weight, fat mass, and adipocyte size, while improving insulin sensitivity and glucose tolerance^2,3.
• Liver Health and Anti-Steatosis Activity: Reverses diet-induced hepatic steatosis by normalizing liver fat content to lean control levels, reduces liver adiposity by over 45%, improves hepatic metabolic profiles, and shifts lipid metabolism away from de novo synthesis toward enhanced fatty acid oxidation².
• Muscle Regeneration and Anti-Aging Benefits: Activates senescent muscle stem cells (muSCs) in aged muscle, promoting proliferation, fusion, and regeneration; nearly doubles muscle fiber cross-sectional area and increases muscle contractile strength by ~70%, restoring regenerative function to levels comparable to youthful muscle¹.
• Epigenetic and Cellular Reprogramming: By blocking NNMT-mediated methylation of nicotinamide, preserves NAD⁺ salvage pathway activity, increases SIRT-1 signaling, reduces histone deacetylation, and promotes metabolic reprogramming toward oxidative phosphorylation and glycolysis balance, supporting tissue repair and energy homeostasis^1-4.

Mechanism of Action

NNMT (Nicotinamide N-Methyltransferase) Inhibition

• Potently and selectively binds to the nicotinamide binding site of NNMT, blocking the methylation of nicotinamide using SAM⁴.
• Elevates NAD+ and S-adenosylmethionine (SAM) levels, shifting metabolic flux toward energy expenditure and away from fat storage^1-4.
• Increases SIRT-1 activity as a result of enhanced NAD+ salvage, leading to beneficial epigenetic and metabolic reprogramming, including increased oxidative phosphorylation (OXPHOS) and muscle stem cell activation^1-3.
• In adipose tissue, inhibition of NNMT suppresses de novo lipogenesis, normalizes fat content, and improves insulin sensitivity^2-3.
• In skeletal muscle, promotes stem cell proliferation, regeneration, and muscle fiber hypertrophy post-injury¹.

Pharmacokinetic Profile

• Route of Administration: Oral, Intravenous
• Dosing Frequency: Once per day
• Half-Life: ~6-8 hours

Formulation & Handling

• Soluble in saline.
• Store at 4°C in a dry, sterile, light-protected environment.

Selected Clinical Trial Activity

5-Amino-1MQ is a research-grade compound that has been studied in laboratory settings but has not undergone full clinical development. It is not approved for therapeutic use in humans, and no large-scale clinical trials have been conducted to evaluate its safety or efficacy as a medication. 5-Amino-1MQ is supplied strictly for laboratory research and investigational purposes only.

References

¹Neelakantan, H., Brightwell, C. R., Graber, T. G. et al. Small molecule nicotinamide N‐methyltransferase inhibitor activates senescent muscle stem cells and improves regenerative capacity of aged skeletal muscle. Biochem. Pharmacol. 163, 481–492 (2019).

²Sampson, C. M., Dimet, A. L., Neelakantan, H. et al. Combined nicotinamide N-methyltransferase inhibition and reduced-calorie diet normalizes body composition and enhances metabolic benefits in obese mice. Sci. Rep. 11, 5637 (2021).

³Liu, J.-R., Deng, Z.-H., Zhu, X.-J. et al. Roles of Nicotinamide N-Methyltransferase in Obesity and Type 2 Diabetes. BioMed Res. Int. 2021, 9924314 (2021).

⁴Iyamu, I. D., Huang, R. Mechanisms and inhibitors of nicotinamide N-methyltransferase. RSC Med. Chem. 12, 232–243 (2021).