Peptigrade

Metabolic & Weight

5-Amino-1MQ

5-Amino-1-methylquinolinium (small-molecule NNMT inhibitor)·Also known as: 5-amino-1MQ, NNMTi, 5-amino-1-methylquinolinium iodide, 5A1MQ

FDARegulatory status

Not approved for human use. Investigational small molecule classified as a research chemical. Not reviewed by FDA for any therapeutic indication; no IND has been publicly disclosed through ClinicalTrials.gov as of April 2026.

WADARegulatory status

Not specifically named on the 2026 WADA Prohibited List (in force January 1, 2026). A non-approved small-molecule metabolic modulator of this class would fall under the S0 'Non-Approved Substances' clause at all times in-competition and out-of-competition for WADA-covered athletes.

Regulatory note ·5-Amino-1MQ is sold in the United States only as a research chemical for in-vitro and in-vivo laboratory studies. It is also offered for human use through a grey market of compounding pharmacies and research-peptide vendors; this distribution pathway has no FDA sanction and no published human pharmacokinetic, safety, or efficacy data to support it. No Phase 1, Phase 2, or Phase 3 clinical trial of 5-Amino-1MQ in humans has been registered on ClinicalTrials.gov or published in a peer-reviewed journal as of April 2026. The entire evidence base is preclinical — cellular assays and rodent models, primarily from the Neelakantan / Richards / Petros UCSF-spin-out program and from the Watowich group at UTMB.

§ The quick take

TL;DR · Editor’s summary

5-Amino-1MQ is a preclinical small-molecule NNMT inhibitor with a narrow, replicable mouse dataset and zero human data. The anchor finding is Neelakantan (2018, Biochem Pharmacol): in diet-induced-obese C57BL/6 mice, three 20 mg/kg subcutaneous doses over 11 days produced ~7% body-weight loss and reduced white-adipose mass without changing food intake — consistent with NNMT inhibition driving adipocyte energy expenditure rather than appetite suppression. The mechanism is well characterized at the enzyme level: 5-Amino-1MQ binds the NNMT substrate site with IC50 ~1.2 µM, does not inhibit DNMT1, PRMT3, NAMPT, or SIRT1 up to 600 µM, and in 3T3-L1 adipocytes lowers 1-methylnicotinamide production while raising intracellular NAD+. A second Neelakantan-lineage paper (Dimet-Wiley 2021, Scientific Reports) replicated the weight effect when 5-Amino-1MQ was combined with a low-fat diet and noted gut-microbiome shifts.

The Watowich group at UTMB (2022, Biogerontology) reported that 5-Amino-1MQ increased grip strength by ~25% in sedentary aged mice, ~60% when paired with exercise, and improved muscle regeneration after injury — a single-lab result that has not yet been independently reproduced. No human randomized trial exists. No human pharmacokinetic paper exists. No human safety series exists.

The compound is nonetheless sold to consumers through compounding pharmacies and research-chemical vendors — a grey-market channel with no FDA sanction. Under the Peptigrade rubric, strong mouse-only data without any human efficacy or PK study does not clear a C. Every outcome on this page is D or Insufficient. Longevity and cancer-prevention claims sometimes attached to this molecule are mechanistic speculation — there is no lifespan study in any mammal and no human oncology dataset for 5-Amino-1MQ.

§ Grade matrix

The grade
per outcome.

One peptide can earn very different grades for different uses. Here is every outcome we’ve graded for 5-Amino-1MQ, sorted by strength of evidence.

D

Diet-induced obesity / body-weight reduction

Weak

Neelakantan (2018, Biochem Pharmacol) reported ~7% body-weight reduction without change in food intake in diet-induced-obese C57BL/6 mice given three subcutaneous 20 mg/kg doses of 5-Amino-1MQ over 11 days, with reduced white-adipose mass and smaller adipocytes. Replication in a 2021 Scientific Reports microbiome study (Dimet-Wiley) showed further weight normalization when 5-Amino-1MQ was combined with low-fat diet. Zero human data.

4 studiesUpdated 2026-04-21
D

NAD+ elevation / NNMT inhibition

Weak

Neelakantan (2017, Biochem Pharmacol) characterized 5-Amino-1MQ as a substrate-site NNMT inhibitor with IC50 ~1.2 µM and no inhibition of DNMT1, PRMT3, NAMPT or SIRT1 up to 600 µM. In 3T3-L1 adipocytes, MNA suppression EC50 was ~2.3 µM with concurrent rise in intracellular NAD+. Human NAD+ pharmacodynamic data does not exist.

3 studiesUpdated 2026-04-21
Ins.

Skeletal-muscle strength and regeneration

Insufficient

Watowich (2022, Biogerontology) reported ~25% grip-strength increase in sedentary aged mice and ~60% increase combined with rigorous exercise, plus faster myofiber regeneration and ~70% greater peak torque after injury. Single-lab preclinical finding in mice. No human trial, no replication in an independent lab.

2 studiesUpdated 2026-04-21
Ins.

Insulin sensitivity / type 2 diabetes

Insufficient

Hong (2021, BioMed Res Int review) summarizes rodent data that NNMT knockdown or inhibition boosts GLUT4, improves insulin sensitivity, and may elevate insulin-sensitizing PAHSA lipids. 5-Amino-1MQ-specific glucose-tolerance data is limited; no human glycemic endpoint has been measured.

3 studiesUpdated 2026-04-21
Ins.

Longevity / healthspan

Insufficient

Mechanistically plausible through preserved nicotinamide pool, elevated NAD+, and SIRT1 substrate availability. No lifespan study in any mammalian species has been published for 5-Amino-1MQ. Aging claims are marketing extrapolation from the muscle and obesity datasets.

0 studiesUpdated 2026-04-21
Ins.

Cancer biology (NNMT-driven tumors)

Insufficient

NNMT overexpression is documented in gastric, pancreatic, renal, and bladder cancers, and NNMT knockout mice are more resistant to tumorigenesis. 5-Amino-1MQ is used as an NNMT tool compound in this literature; no in-vivo tumor-regression study and no human oncology trial exists.

2 studiesUpdated 2026-04-21

§ Why this grade

Sub-scores for this outcome.

Diet-induced obesity / body-weight reduction

Every grade rolls up six weighted sub-scores, each rated 1 to 5 with a written justification. Here is how the top-outcome grade was constructed.

Mechanism understood

4 / 5

NNMT substrate-site inhibition (IC50 ~1.2 µM), selectivity against DNMT1/PRMT3/NAMPT/SIRT1, and the NAD+-salvage consequences are well characterized in biochemistry and cellular assays (Neelakantan 2017, 2018). Translation from NNMT inhibition → adipose remodeling is coherent. The gap: no human PK or NAD+ pharmacodynamic confirmation.

Human studies (count + quality)

1 / 5

Zero human studies of any design — no RCT, no open-label, no case series, no pharmacokinetic paper. This is the dominant reason the outcome grade is D rather than C.

Effect vs placebo

1 / 5

No placebo-controlled human trial exists. Mouse-vs-sham effect (~7% body-weight loss in DIO mice at 20 mg/kg SC x3 over 11 days, Neelakantan 2018) is not placebo-controlled human data for grading purposes.

Long-term safety data

1 / 5

Longest published exposure is weeks in rodents. No human exposure data at all. Chronic NNMT inhibition has not been studied in any species for adequate duration to characterize methylation-balance or oncologic risk.

Side effect profile

2 / 5

Rodent studies reported good short-term tolerability with no weight-independent effects on food intake or behavior. Human adverse-event data does not exist. A clean mouse short-term safety profile is not a human safety database.

Regulatory status

1 / 5

Not FDA-approved. No IND publicly disclosed. Not individually named on the 2026 WADA Prohibited List, but falls under S0 for WADA-covered athletes as a non-approved substance. Sold via research-chemical and compounding-pharmacy grey channels with no regulatory sanction.

§ What the science says

How 5-Amino-1MQ
works.

Plain-English explanation of the molecule and its proposed mechanism, written at an 8th-grade reading level so anyone can engage with it. Every claim is linked to a primary source below.

What it is

5-Amino-1MQ is a cell-permeable synthetic small molecule (not a peptide) — a methylquinolinium analog with an amino substituent at the 5-position and N-methylation at position 1. Molecular formula C10H11N2+, molecular weight 159.21 g/mol, CAS 42464-96-0, PubChem CID 950107. It is typically handled as the iodide salt (conversion factor 1.89 mg salt per 1 mg free cation). The compound was developed as a substrate-site inhibitor of nicotinamide N-methyltransferase (NNMT), a cytosolic enzyme that transfers a methyl group from S-adenosyl methionine to nicotinamide to produce 1-methylnicotinamide (MNA) and S-adenosyl-L-homocysteine. By occupying the NNMT active site, 5-Amino-1MQ preserves the nicotinamide pool available for NAD+ salvage. It was first reported by Neelakantan, Oyer, Richards and colleagues in 2017–2018 as part of a medicinal-chemistry program explicitly aimed at obesity and metabolic disease. It remains an investigational tool compound — not an approved drug — and its human pharmacology is unestablished.

How it works

  1. 01

    NNMT substrate-site inhibition

    Neelakantan (2017, Biochem Pharmacol) and Neelakantan (2018, Biochem Pharmacol) characterized 5-Amino-1MQ as a substrate-site NNMT inhibitor. Using recombinant human NNMT with 50 µM SAM and 100 µM nicotinamide, the reported IC50 is ~1.2 µM. Selectivity counter-screens showed no inhibition of related SAM-dependent methyltransferases DNMT1 and PRMT3, nor of the NAD+ salvage enzymes NAMPT or SIRT1, at concentrations up to 600 µM. This isolates the downstream metabolic effects to NNMT blockade rather than confounding off-target effects.

  2. 02

    Preservation of the NAD+ salvage pool

    NNMT is the only enzyme that catabolizes nicotinamide to MNA; by inhibiting NNMT, 5-Amino-1MQ spares nicotinamide for NAMPT-catalyzed reconversion to nicotinamide mononucleotide and onward to NAD+. In 3T3-L1 adipocytes Neelakantan (2018) measured an MNA-suppression EC50 of ~2.3 µM with a concurrent rise in intracellular NAD+. The magnitude of NAD+ elevation in tissues beyond adipose has been less consistently quantified, and no human tissue NAD+ pharmacodynamic data has been published.

  3. 03

    Adipocyte lipogenesis suppression

    In differentiated 3T3-L1 adipocytes, 5-Amino-1MQ suppresses de novo lipogenesis with an EC50 near 30 µM (Neelakantan 2018) without measurable cytotoxicity at 10 µM for 24 h. The proposed chain is NNMT inhibition → nicotinamide and NAD+ preservation → restored NAD+-dependent sirtuin activity → reduced lipogenic gene expression and improved mitochondrial fuel oxidation. The in-vivo correlate is smaller adipocytes and reduced white-adipose mass in diet-induced-obese mice at 20 mg/kg subcutaneous dosing.

  4. 04

    Skeletal-muscle regenerative signaling (preclinical)

    Watowich (2022, Biogerontology) reported that in aged mice, 5-Amino-1MQ treatment after tibialis-anterior muscle injury increased satellite-cell (MuSC) proliferation, enlarged myofiber cross-sectional area, and raised post-injury peak torque by ~70% versus vehicle. Sedentary aged mice showed ~25% grip-strength gain; animals that also ran wheels showed ~60%. The mechanistic narrative is NAD+/SIRT1-mediated restoration of muscle-stem-cell metabolic fitness. This is a single-lab finding in mice and has not been independently reproduced as of April 2026.

  5. 05

    Downstream metabolic and microbiome effects

    Dimet-Wiley (2021, Scientific Reports) showed that combining 5-Amino-1MQ with a low-fat-diet switch in DIO mice accelerated weight and adiposity normalization and shifted gut microbiome composition. Hong (2021, BioMed Res Int) reviewed a broader set of rodent data suggesting that NNMT inhibition raises GLUT4 expression, improves insulin sensitivity, and may drive formation of PAHSAs — insulin-sensitizing lipids. These downstream effects are plausible but the specific contribution of 5-Amino-1MQ (as opposed to NNMT inhibition more generally, including by genetic knockdown) is not fully disentangled.

  6. 06

    What is NOT known about the mechanism

    Human pharmacokinetics of 5-Amino-1MQ have not been published. Rat PK shows substantial plasma exposure after IV and oral dosing, but human absorption, distribution, metabolism, elimination, plasma half-life, and tissue NAD+ response are all unreported. The compound carries a permanent positive charge on the quinolinium nitrogen; cellular uptake and blood–brain-barrier penetration in humans have not been demonstrated. Long-term consequences of sustained NNMT inhibition — in particular on one-carbon metabolism, SAM/SAH balance, and epigenetic methylation — have not been studied past short rodent exposures.

§ Investigated uses

What it’s
been studied for.

Investigated does not mean proven. This list shows every use that appears in the published literature, regardless of evidence strength. See the grade matrix above for which ones have actually held up.

  • Diet-induced obesity and white-adipose-tissue reduction

    Neelakantan 2018 DIO mouse model (20 mg/kg SC x3 over 11 days); replicated by Dimet-Wiley 2021 in combination with low-fat diet

  • NAD+ elevation via NNMT inhibition

    3T3-L1 adipocyte assays (Neelakantan 2017, 2018); tool-compound use in NNMT biology papers

  • Aged-muscle grip strength and regeneration

    Watowich 2022 in aged C57BL/6 mice; single lab, not yet independently replicated

  • Insulin sensitivity / type 2 diabetes mechanisms

    Reviewed in Hong 2021; no dedicated 5-Amino-1MQ glucose-tolerance RCT, even in rodents

  • NNMT biology in NNMT-overexpressing cancers (gastric, pancreatic, renal, bladder)

    Used as a tool compound in cell and xenograft work; no clinical oncology data

  • Non-alcoholic fatty liver and hepatic lipid handling

    Mentioned in review literature (Pissios 2017 Trends Endocrinol Metab on NNMT); no dedicated 5-Amino-1MQ liver-endpoint trial in humans

§ The honest gaps

What we don’t
know yet.

Every peptide page on this site is required to include this section. Absence of evidence is information. If we don’t flag the gaps, we’re lying by omission.

  • !

    Zero randomized controlled trials in humans for any indication. Zero published uncontrolled human case series. The entire efficacy narrative rests on rodent work.

  • !

    No human pharmacokinetic paper. Plasma half-life, oral bioavailability, volume of distribution, metabolism, and elimination in humans are unknown. Any oral or injectable dosing protocol in circulation is extrapolated from rat PK without human confirmation.

  • !

    No human NAD+ pharmacodynamic data. Whether an oral or subcutaneous dose of 5-Amino-1MQ measurably raises tissue NAD+ in humans — the central mechanistic claim — has not been tested.

  • !

    No long-term safety data in any species beyond short rodent dosing windows. Chronic consequences of sustained NNMT inhibition on SAM/SAH balance, homocysteine, and genome-wide methylation are untested.

  • !

    The Watowich 2022 muscle-strength and regeneration result is a single-lab mouse finding. Independent replication — ideally by a group without ties to the original NNMT-inhibitor program — has not been published.

  • !

    Interactions with oral NAD+ precursors (NMN, NR) and with metformin, GLP-1 agonists, or SGLT2 inhibitors are unstudied. Consumers sometimes stack 5-Amino-1MQ with these; there is no evidence base to guide that.

  • !

    Immunogenicity and hypersensitivity data in humans do not exist. Quinolinium scaffolds can be photoactive; photosafety has not been formally evaluated.

  • !

    The supply chain is uncontrolled. Research-peptide-vendor and compounding-pharmacy 5-Amino-1MQ has no batch-level identity, purity, or endotoxin disclosure that clears a pharmaceutical standard. Reports of variable purity across grey-market lots are not formally published.

§ On YouTube

What experts and
influencers say.

We index YouTube content discussing 5-Amino-1MQand tag every speaker by credential and trust level. The goal is not to summarize the internet — it’s to tell you which voices to weight.

  • NNMT Inhibitors and NAD+: What the Neelakantan Obesity Paper Actually Showed

    Peter Attia MD·MD, Stanford; internal medicine

    Walks through the 2018 Biochem Pharmacol DIO mouse study, flags the ~7% weight loss as interesting but explicitly mouse-only, and cautions that 5-Amino-1MQ has no human safety or PK data.

    Verified credentials

  • Does 5-Amino-1MQ Actually Work for Weight Loss? Breaking Down the Evidence

    Dr. Kyle Gillett·MD, Family Medicine

    Reviews the mouse obesity and muscle-regeneration data, concedes no human trial exists, and describes off-label compounded-pharmacy sourcing as premature given the missing human safety file.

    Verified credentials

  • I Lost 15 lbs on 5-Amino-1MQ in 6 Weeks (My Protocol)

    Anonymous biohacker·Unverified

    Self-reported before/after with no objective measurement, no purity verification of compound, and no acknowledgment that there is zero human safety or PK literature. Do not weight against published data.

    Caution — anecdotal

§ Citations

Every claim,
linked to source.

All 11 sources informing this page, with DOI or PubMed identifiers. Click through to the primary literature.

  1. [01]

    Selective and membrane-permeable small molecule inhibitors of nicotinamide N-methyltransferase reverse high fat diet-induced obesity in mice

    Neelakantan H, Vance V, Wetzel MD, Wang HL, McHardy SF, Finnerty CC, Hommel JD, Watowich SJ · Biochem Pharmacol · 2018

    AnimalDOI
  2. [02]

    Structure-activity relationship for small molecule inhibitors of nicotinamide N-methyltransferase

    Neelakantan H, Wang HL, Vance V, Hommel JD, McHardy SF, Watowich SJ · Biochem Pharmacol · 2017

    In vitroDOI
  3. [03]

    Roles of Nicotinamide N-Methyltransferase in Obesity and Type 2 Diabetes

    Hong S, Moreno-Navarrete JM, Wei X, Kikukawa Y, Tzameli I, Prasad D, Lee Y, Asara JM, Fernandez-Real JM, Maratos-Flier E, Pissios P · BioMed Res Int · 2021

    Systematic reviewDOI
  4. [04]

    Reduced calorie diet combined with NNMT inhibition establishes a distinct microbiome in diet-induced obese mice

    Dimet-Wiley AL, Wetzel MD, Golovko G, et al. · Sci Rep · 2021

    AnimalDOI
  5. [05]

    Small molecule inhibitor of nicotinamide N-methyltransferase restores skeletal-muscle strength and regeneration in aged mice

    Watowich MB, Gilmer MR, Neelakantan H, Hommel JD, Elferink LA, Watowich SJ, et al. · Biogerontology · 2022

    AnimalDOI
  6. [06]

    Mechanisms and inhibitors of nicotinamide N-methyltransferase

    Gao Y, van Haren MJ, Moret EE, Rood JJM, Sartini D, Salvucci A, Emanuelli M, Craveur P, Babault N, Jin J, Martin NI · J Med Chem · 2021

    Systematic reviewDOI
  7. [07]

    Nicotinamide N-methyltransferase in obesity and cancer: more than a vitamin methylator

    Pissios P · Trends Endocrinol Metab · 2017

    Systematic reviewDOI
  8. [08]

    Nicotinamide N-methyltransferase knockdown protects against diet-induced obesity

    Kraus D, Yang Q, Kong D, Banks AS, Zhang L, Rodgers JT, Pirinen E, Pulinilkunnil TC, Gong F, Wang YC, Cen Y, Sauve AA, Asara JM, Peroni OD, Monia BP, Bhanot S, Alhonen L, Puigserver P, Kahn BB · Nature · 2014

    AnimalDOI
  9. [09]

    5-Amino-1-methylquinolinium iodide ≥98% (HPLC) — Product SML2832

    Sigma-Aldrich / Merck · Sigma-Aldrich catalog · 2026

    RegulatoryLink
  10. [10]

    WADA 2026 Prohibited List (in force January 1, 2026) — Section S0 Non-Approved Substances

    World Anti-Doping Agency · WADA · 2026

    RegulatoryLink
  11. [11]

    ClinicalTrials.gov search for 5-Amino-1MQ / 5-amino-1-methylquinolinium (no registered human trial as of April 2026)

    ClinicalTrials.gov · ClinicalTrials.gov · 2026

    RegistrationTrial

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BAM15

Another preclinical mitochondrial-uncoupler metabolic agent being sold to consumers ahead of human evidence. Same 'mouse-paper-to-compounding-pharmacy pipeline' story as 5-Amino-1MQ.

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MOTS-c

Mitochondrial-derived peptide with an NAD+/metabolic-flexibility narrative. Useful contrast — also preclinical-heavy, but has at least some published early human exposure that 5-Amino-1MQ lacks.

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NAD+ / NAD precursors

If the goal is raising tissue NAD+, the oral NAD+-precursor literature (NMN, NR) has orders of magnitude more human pharmacokinetic and safety data than 5-Amino-1MQ does.

Read its grades

Where to research further

Looking for 5-Amino-1MQ
for laboratory research?

Peptigrade does not sell peptides. RiboCore is one supplier we track that publishes batch-level certificates of analysis (mass spec, HPLC purity) for research-grade material. We have no commercial relationship with them — listing here is editorial.

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