MEDICAL DISCLAIMER: Educational research guidelines only. Lyophilized peptides are investigational chemical compounds and are NOT approved for human consumption, diagnosis, or therapy. Consult a licensed physician before any research application.
5-Amino-1MQ Dosage Chart, Schedule & Reconstitution Protocol
Quickstart Highlights
5-Amino-1MQ (5-amino-1-methylquinolinium) is a small-molecule — not a peptide — competitive inhibitor of nicotinamide N-methyltransferase (NNMT), the enzyme that methylates nicotinamide and depletes both the cellular methyl pool and the NAD+ precursor pool. NNMT is highly expressed in obese adipose tissue and sustains a metabolic and epigenetic state that promotes lipid storage and reduced energy expenditure. Neelakantan and colleagues (Biochem Pharmacol 2018) reported that 5-Amino-1MQ at 20 mg/kg/day reversed high-fat-diet-induced obesity in mice over 11 days without affecting food intake, and a follow-up study in aged mice showed activation of senescent muscle satellite cells [1][2]. 5-Amino-1MQ is preclinical only — no published human clinical trial exists for any indication. It is sold by research-chemical suppliers strictly for laboratory use.
Reconstitute: Add 2 mL bacteriostatic water → 5 mg/mL concentration.
Easy measuring: At 5 mg/mL, 1 unit = 0.01 mL = 0.0500 mg (50 mcg) on a U-100 insulin syringe.
Storage: Lyophilized frozen at −20 °C; reconstituted refrigerated at 2–8 °C.
Half-life: Plasma half-life approximately 3.8–6.9 hours per rodent pharmacokinetic work (Neelakantan 2018), supporting once-daily oral dosing in animal studies [1].
Regulatory status: Not approved by any regulator for any indication. No published human clinical trial has ever been conducted. Pharmaceutical-grade NNMT inhibitors have not advanced to human trials.
Human data gap: All efficacy claims are extrapolated from rodent and in-vitro work. Research-chemical dosing of 50–150 mg/day comes from simple allometric scaling, not human PK or safety validation.
Quick Protocol Navigation
Reconstitution Instruction & Mixing Step-by-Step
Lyophilized powder must be reconstituted carefully. Agitating peptide chains can shear disulfide bonds and render the peptide biologically inert.
Draw 2.0 mL bacteriostatic water with a sterile syringe.
Inject slowly down the vial wall; avoid foaming.
Gently swirl/roll until dissolved—solution should be clear (do not shake).
Inject slowly; a mild stinging sensation may occur due to the quinolinium structure.
Do not aspirate for subcutaneous injections; inject slowly and steadily[12].
Interactive 5-Amino-1MQ Syringe Calculator
Currently visualizing the 10 mg vial reconstituted with 2 mL bacteriostatic water. Adjust the target dose to dynamically render syringe units.
Reconstitution Calculation: 10mg dry powder in 2mL water yields 5.00 mg/mL. To evaluate a 250mcg dose, pull to 5.0 units (5 syringe ticks).
U-100 Syringe Representation
5.0 Units (5 Ticks)
Educational reference visual. Assumes standard U-100 insulin syringe where 1.0 mL volume = 100 units.
Titration & Dose Escalation Schedules
| Phase | Daily Dose (mg) | Units (per injection) (mL) |
|---|---|---|
| Days 1–2 (Tolerance) | 2.5 mg (2500 mcg) | 50 units (0.50 mL) |
| Days 3+ (Standard) | 5 mg (5000 mcg) | 100 units (1.00 mL) |
| Alternative BID | 2.5 mg twice daily | 50 units (0.50 mL) × 2 |
Administration guidelines: Refer to guidelines | 2 mL Reconstitution
Research Supplies Quantity Planner
Scientific mathematical planning of syringes, bacteriostatic water and dry vials needed for extended research blocks using the 10 mg vial.
5-Amino-1MQ Vials (10 mg each):
- check1 week (5 mg/day = 35 mg total) → 4 vials
- check2 weeks (5 mg/day = 70 mg total) → 7 vials
- check4 weeks (5 mg/day = 140 mg total) → 14 vials
Insulin Syringes (U-100, 1 mL):
- check1 week (once daily): 7 syringes
- check2 weeks (once daily): 14 syringes
- check4 weeks (once daily): 28 syringes
Bacteriostatic Water (10 mL bottles): Use 2.0 mL per vial for reconstitution.
- check1 week (4 vials × 2.0 mL = 8 mL) → 1 × 10 mL bottle
- check2 weeks (7 vials × 2.0 mL = 14 mL) → 2 × 10 mL bottles
- check4 weeks (14 vials × 2.0 mL = 28 mL) → 3 × 10 mL bottles
Alcohol Swabs: One for the vial stopper + one for the injection site each administration.
- check1 week (once daily): 14 swabs
- check2 weeks (once daily): 28 swabs
- check4 weeks (once daily): 56 swabs → recommend 1 × 100-count box
Mechanism of Action (MOA)
5-Amino-1MQ is a membrane-permeable competitive inhibitor of NNMT, with IC50 of approximately 1.5 μM measured in cell-free enzyme assays [1]. NNMT methylates nicotinamide to produce 1-methylnicotinamide, consuming a methyl group from S-adenosyl-methionine in the process. The reaction is metabolically wasteful — it depletes both the methyl pool and the precursor pool for NAD+ salvage — and NNMT is highly expressed in obese adipose tissue, where it sustains an epigenetic and metabolic landscape that promotes adipocyte differentiation, lipid storage and reduced energy expenditure. Genetic NNMT knockdown in adipose tissue of obese mice produced substantial fat-mass reductions and metabolic improvements in earlier work by Kraus et al. (Nature 2014), establishing the target validity. 5-Amino-1MQ replicates these effects pharmacologically. The mechanism has two principal downstream arms. First, NNMT inhibition restores the cellular SAM:SAH ratio and increases tissue NAD+ availability, enabling SIRT1 and PARP enzymatic activity, mitochondrial biogenesis, and elevated metabolic flux through fatty-acid oxidation. Second, the inhibitor relieves the methylation-dependent epigenetic suppression of energy-expenditure genes in adipose tissue and skeletal muscle. In adipocytes, this produces phenotypic conversion toward a more thermogenic, less lipid-storing state. In skeletal muscle, the same effect promotes satellite-cell activation and improves regenerative capacity. The dual adipose-and-muscle effect distinguishes 5-Amino-1MQ from incretin-class drugs, which act primarily on appetite. Administration is oral; the molecule has good oral bioavailability and crosses cellular membranes readily by virtue of its small size and amphipathic character. Plasma half-life is short (estimated 2–4 hours in rodent models), and dosing protocols generally use daily oral administration. The Neelakantan obesity study used 20 mg/kg/day for 11 days in HFD-fed obese mice, producing approximately 7% body-weight reduction with concurrent reductions in adipose-tissue mass, improved glucose tolerance, and no change in food intake [1]. The follow-up muscle-regeneration study used the same dose in aged mice and showed improvement in satellite-cell activity and muscle regeneration capacity within 7–14 days [2]. No published human clinical-trial data exist; research-chemical dosing typically extrapolates 50–150 mg/day for an adult human based on simple allometric scaling, but this dose has not been validated for safety or efficacy in controlled human trials. Other NNMT inhibitors in earlier-stage development may eventually advance to human trials, but 5-Amino-1MQ itself remains a preclinical research tool.
Clinical Trial Efficacy Highlights
- starNeelakantan et al. (Biochem Pharmacol 2018) treated diet-induced-obese mice with 5-Amino-1MQ at 20 mg/kg/day IP for 11 days, producing approximately 7% body-weight reduction, significant adipose-tissue mass reduction, and improved glucose tolerance — all without significant change in food intake [1].
- starIn the same study, NNMT inhibition reduced adipocyte size by approximately 30% and increased expression of thermogenic markers (UCP1, PGC-1α) in white adipose tissue, suggesting conversion toward a beige-adipose phenotype [1].
- starNeelakantan et al. (FASEB J 2019) showed that 5-Amino-1MQ at 20 mg/kg/day in aged mice activated senescent satellite cells and improved muscle regeneration capacity following injury, with substantial increases in MyoD+ cell numbers and faster recovery of muscle fiber cross-sectional area [2].
- starKraus et al. (Nature 2014) had previously established target validity through antisense-oligonucleotide knockdown of NNMT in adipose tissue, demonstrating that genetic suppression produced ~30% reduction in adipose-tissue mass and protection from diet-induced obesity in mice [3].
- starMechanistic studies confirm 5-Amino-1MQ is selective for NNMT over related methyltransferases (PNMT, COMT, GNMT) with at least 100-fold selectivity at the doses used in animal work [1].
- starCell-culture studies of 3T3-L1 adipocytes treated with 5-Amino-1MQ show dose-dependent suppression of adipogenesis, reduced triglyceride accumulation, and increased expression of mitochondrial biogenesis markers — supporting the proposed mechanism of action.
- starNo published randomized human trial has tested 5-Amino-1MQ for obesity, metabolic syndrome, sarcopenia or any other indication; all efficacy data come from rodent models and in-vitro work.
Side Effects & Tolerability Profile
Clinical subjects transiently report mild side effects. Slowly escalating the titration dose represents the single most effective intervention to limit side effects.
- warningNo published human safety data exist for 5-Amino-1MQ; the entire safety profile is extrapolated from rodent preclinical work, which showed no overt toxicity at 20 mg/kg/day for 11 days but did not include extended-duration toxicology or carcinogenicity assessment [1].
- warningTheoretical concerns center on systemic NNMT inhibition: NNMT also regulates methylation of biogenic amines and may affect histamine metabolism, with potential for altered methyl-pool homeostasis affecting epigenetic regulation across tissues.
- warningAnecdotal user reports (not from controlled trials) describe mild gastrointestinal effects (nausea, soft stools), transient mild headache, and occasional insomnia at higher doses — none of which has been characterized in any published clinical trial.
- warningBecause NNMT activity also produces 1-methylnicotinamide, an endogenous compound with vascular and anti-inflammatory effects, NNMT inhibition may reduce circulating 1-MNA — the long-term consequences of this are unstudied in humans.
- warningDrug-drug interactions are essentially uncharacterized; 5-Amino-1MQ's interaction with other methylation-dependent pathways (e.g., COMT, catecholamine metabolism) is theoretically possible but has not been formally studied.
- warningReproductive and developmental toxicity have not been assessed in any published preclinical work, and 5-Amino-1MQ should be considered contraindicated in pregnancy by default.
- warningLong-term cardiovascular effects of sustained NNMT inhibition are unknown; NNMT is expressed in vascular tissue and the consequences of chronic inhibition for endothelial function or blood pressure have not been characterized.
- warningQuality control of research-chemical supply is a significant practical safety issue: purity, identity and contamination of commercial supply have been variable and there is no pharmaceutical-grade source.
Subcutaneous Injection Technique
Most research peptides require subcutaneous injection into fatty tissue. Never inject directly into a blood vessel or deep muscle tissue unless clinically detailed.
1. Site Selection
Common locations include the abdomen (2 inches from navel), outer upper arms, or thighs.
2. Sanitization
Thoroughly clean the selected site, stopper and vial top using 70% isopropyl alcohol prep swabs.
3. Angle & Push
Pinch the skin and insert the needle at a 45 to 90-degree angle. Depress plunger smoothly.
4. Site Rotation
Rotate injection sites continuously to avoid lipodystrophy or tissue scarring.
Frequently Asked Questions
What is the typical 5-Amino-1MQ dosage?expand_more
Research-chemical protocols typically use 50–150 mg orally once daily, with cycles of 4–12 weeks. This range is extrapolated from rodent studies (20 mg/kg/day in mice scales to approximately 100 mg/day for a 70 kg adult by allometric conversion). No human trial has validated this dose for either safety or efficacy. Some protocols cycle with washout periods of 2–4 weeks.
How is 5-Amino-1MQ different from incretin drugs like Semaglutide?expand_more
5-Amino-1MQ is a small-molecule NNMT inhibitor that targets adipose-tissue methylation and mitochondrial metabolism; semaglutide is a GLP-1 receptor agonist that acts on appetite regulation. 5-Amino-1MQ has no human efficacy data — only rodent and in-vitro work. Semaglutide has robust human data showing ~15% weight loss [1].
What are the most common side effects of 5-Amino-1MQ?expand_more
No characterized human safety profile exists. Theoretical concerns include altered methyl-pool homeostasis, effects on biogenic amine metabolism, and unknown cardiovascular consequences. Anecdotal user reports describe mild GI effects, occasional headache, and insomnia at higher doses, none documented in controlled trials [1].
How should 5-Amino-1MQ be reconstituted and stored?expand_more
5-Amino-1MQ is typically supplied as a solid (powder or capsule) for oral administration; no reconstitution is required. Store at room temperature (15–25 C) in a sealed light-protected container; protect from moisture. Once-opened bottles typically remain stable for 12–18 months. If supplied as a solution, refrigerate and use within 30 days.
Is 5-Amino-1MQ FDA approved?expand_more
No. 5-Amino-1MQ has not been approved by any regulator for any indication. No published human clinical trial has been conducted. It is sold by research-chemical suppliers strictly for laboratory use and is not legally available for human therapeutic use. NNMT inhibition as a target remains valid but pharmaceutical-grade NNMT inhibitors have not advanced to human trials.
Academic References & Study Citations
Neelakantan H, Vance V, Wetzel MD, et al. (2018) Biochem Pharmacol 147:141-152. 'Selective and membrane-permeable small molecule inhibitors of nicotinamide N-methyltransferase reverse high fat diet-induced obesity in mice'. View Scientific Paper →
Neelakantan H, Brightwell CR, Graber TG, et al. (2019) FASEB J. 'Small molecule nicotinamide N-methyltransferase inhibitor activates senescent muscle stem-cells and improves regenerative capacity of aged skeletal muscle'. View Scientific Paper →
Kraus D, Yang Q, Kong D, et al. (2014) Nature 508:258-262. 'Nicotinamide N-methyltransferase knockdown protects against diet-induced obesity'. View Scientific Paper →
Pissios P. (2017) Trends Endocrinol Metab. 'Nicotinamide N-Methyltransferase: More Than a Vitamin B3 Clearance Enzyme' — comprehensive review of NNMT biology and obesity link. View Scientific Paper →
Liu KY, Mistry RJ, Aguirre CA, et al. (2021) Roles of Nicotinamide N-Methyltransferase in Obesity and Type 2 Diabetes — comprehensive metabolic review. View Scientific Paper →
Brightwell CR, Latham CM, Thomas NT, et al. (2022) Am J Physiol Cell Physiol. 'A glycolytic-to-oxidative fiber-type switch produced by NNMT inhibition in aged skeletal muscle'. View Scientific Paper →
Roberti A, Fernández AF, Fraga MF. (2021) Mol Metab. 'Nicotinamide N-methyltransferase: At the crossroads between cellular metabolism and epigenetic regulation' — molecular review. View Scientific Paper →
Eckert MA, Coscia F, Chryplewicz A, et al. (2019) Nature 569:723-728. 'Proteomics reveals NNMT as a master metabolic regulator of cancer-associated fibroblasts'. View Scientific Paper →