SCALE Performance

5-Amino-1MQ Pen

5-amino-1-methylquinolinium iodide, a small-molecule NNMT inhibitor, at 50 mg/mL in bacteriostatic water, 150 mg per 3 mL cartridge. Filled from a lot tested in the manufacturer’s own laboratory.

Compound5-Amino-1MQ 5-Amino-1-methylquinolinium iodide (NNMT inhibitor); small molecule, not a peptide
CAS number42464-96-0
Molecular formulaC10H11IN2
Theoretical mass286.1 Da
Sequence / structureQuinolinium salt (iodide); the 5-amino-1-methylquinolinium cation is 159.2 Da and is the species observed by ESI-MS.
Contents5-Amino-1MQ: 150 mg per 3 mL pen (5% w/v)
FormSterile aqueous solution in bacteriostatic water (0.9% benzyl alcohol), supplied in a 3 mL glass cartridge inside a preloaded autoinjector pen fitted with a needle
Storage, sealedStore at 2–8 °C in the original carton, protected from light
FormatSolution in a 3 mL pre-filled pen

Sizes and lots

  • 150 mg · 1 pen — $118.99
  • 150 mg · Kit of 10 — $1057.82

5-amino-1MQ (5-amino-1-methylquinolinium) is a small-molecule NNMT inhibitor, not a peptide. In this listing it comes ready-dissolved: a preloaded pen with a 3 mL glass cartridge of the iodide salt in bacteriostatic water at 50 mg/mL, 150 mg per pen, so nothing has to be weighed. Research on 5-amino-1MQ covers enzyme inhibition, fat cell metabolism and diet-induced obesity in mice; none of it used a pre-made solution.

What is in the pen

The cartridge holds a sterile solution of 5-amino-1-methylquinolinium iodide at 5% w/v, which is 50 mg/mL and 150 mg across 3 mL. The figure is the iodide salt, so in molar terms it is about 175 mM of the active cation, or roughly 0.52 mmol per pen. The solvent is bacteriostatic water with 0.9% benzyl alcohol. The safety data sheet classifies 5-amino-1MQ as harmful if swallowed and as a skin, eye and respiratory irritant, and benzyl alcohol as harmful if swallowed or inhaled, an eye irritant and a skin sensitiser.

Keep the pen at 2 to 8 °C in its carton, out of the light and capped between uses, and never freeze it. Discard it if the solution has frozen or looks cloudy or discoloured. The same salt is sold dry in the 5-amino-1MQ 50 mg vial, and peptide pen vs vial covers the general trade-offs between formats.

What the research covers

NNMT uses SAM to methylate nicotinamide, a precursor of NAD+, and Kraus and colleagues showed in 2014 that its expression rises in the fat and liver of obese and diabetic mice1. Knocking it down in those tissues protected mice against diet-induced obesity, and inhibiting it raised adipose SAM and NAD+1. The knockdown also increased the activity of ODC and SSAT, two enzymes that control polyamine flux1. Small-molecule inhibitors followed. Neelakantan and colleagues reported in 2018 that methylquinoliniums carrying a primary amine, the group that includes 5-amino-1MQ, crossed membranes readily in permeability assays, left related SAM-dependent methyltransferases alone, and were tested in cultured fat cells and in mice made obese on a high-fat diet2. Inside the cultured fat cells, those compounds reduced the enzyme's product MNA, increased NAD+ and SAM and cut lipid synthesis2. A structurally different inhibitor from another group, JBSNF-000088, lowered body weight and improved glucose tolerance in obese mice but had no such effect in NNMT knockout mice3.

Frequently asked questions

What concentration does the pen hold, and on what basis?

50 mg/mL of 5-amino-1-methylquinolinium iodide, 150 mg in the 3 mL cartridge. The figure refers to the iodide salt, as on the vials, and works out to about 175 mM. Each salt unit carries one cation, so that is also the molar concentration of the active ion.

How does the pen compare with the vials?

The vials hold dry salt at −20 °C and let you set the concentration when dissolving it. The pen is a fixed 50 mg/mL solution kept at 2 to 8 °C and never frozen. Neither format has been studied as such; the published work used the compound itself.

References

  1. Kraus D, Yang Q, Kong D, et al. Nicotinamide N-methyltransferase knockdown protects against diet-induced obesity. Nature. 2014;508(7495):258-62. DOI · PubMed
  2. Neelakantan H, Vance V, Wetzel MD, et al. Selective and membrane-permeable small molecule inhibitors of nicotinamide N-methyltransferase reverse high fat diet-induced obesity in mice. Biochem Pharmacol. 2018;147:141-152. DOI · PubMed
  3. Kannt A, Rajagopal S, Kadnur SV, et al. A small molecule inhibitor of Nicotinamide N-methyltransferase for the treatment of metabolic disorders. Sci Rep. 2018;8(1):3660. DOI · PubMed

For laboratory research use only. Not for human or veterinary consumption. Products have not been evaluated by the U.S. Food and Drug Administration and are not intended to diagnose, treat, cure or prevent any disease.