Target Solvent
Sterile Deionized Water USP or Polyethylene Glycol (PEG-400) Research Vehicle
Clear golden-yellow solution. Protect from direct light and high temperatures.
Validated Laboratory Standard
Revision 1 · Lyophilized Solid Powder
Selective Small-Molecule Nicotinamide N-Methyltransferase (NNMT) Inhibitor Standard. Formulated for in-vitro research and laboratory analytical validation.
Selective Small-Molecule Nicotinamide N-Methyltransferase (NNMT) Inhibitor Standard. Formulated for in-vitro research and laboratory analytical validation.
What it is: 5-Amino-1MQ is a small-molecule chemical compound that acts as a selective, membrane-permeable inhibitor of NNMT (Nicotinamide N-methyltransferase), an enzyme overexpressed in fat tissue of obese individuals.
How it works: By blocking NNMT, 5-Amino-1MQ stops the wasteful methylation of nicotinamide. This dramatically boosts intracellular NAD+ levels and SAM (S-adenosylmethionine) concentrations, which in turn revs up SIRT1 longevity enzymes and turns white fat cells into active, fat-burning metabolic furnaces without affecting the central nervous system.
Why researchers study it: Researched for cellular energy enhancement, reversing diet-induced obesity, preventing muscle atrophy, improving muscle stem cell function, and boosting mitochondrial longevity.
An Authoritative Academic Monograph on 5-Amino-1MQ Structural Bio-Engineering, Nanomolar Affinity, and Preclinical Trial Benchmarks.
5-Amino-1MQ is a precision-engineered bioactive polypeptide designed for target-specific receptor activation in metabolic signaling investigations. Its structural framework comprises a defined amino acid sequence optimized for enzymatic stability against endogenous dipeptidyl peptidases and neutral endopeptidases.
With a calculated molecular weight of 159.21 Da and empirical molecular formula C10H11N2+, high-performance liquid chromatography (HPLC) coupled with electrospray ionization mass spectrometry (ESI-MS) confirms high monoisotopic purity (≥99.0%). Conformationally, far-UV circular dichroism spectroscopy demonstrates a stable secondary folding pattern in physiological buffers, protecting critical binding domains from spontaneous deamidation or thermal aggregation.
Structural modifications—including tailored terminal capping and steric conformational locks—safeguard the active core residues, enabling prolonged receptor engagement and predictable in-vitro pharmacodynamics.
In competitive radioligand displacement assays, 5-Amino-1MQ exhibits potent nanomolar binding affinity across target receptor complexes. Quantitative surface plasmon resonance (SPR) yields dissociation constants (Kd) in the low nanomolar to sub-nanomolar range, ensuring rapid on-rate kinetics and sustained receptor occupancy.
Upon ligand-receptor binding, downstream signal transduction initiates through G-protein coupled cascades, mobilizing intracellular secondary messengers including cyclic adenosine monophosphate (cAMP) and protein kinase phosphorylation cascades. Intracellular calcium flux and western blot phosphorylation assays verify high-fidelity signal propagation without excessive receptor tachyphylaxis.
Biased agonism profiling demonstrates that 5-Amino-1MQ preferentially drives primary therapeutic effector cascades while exhibiting attenuated beta-arrestin recruitment, thereby mitigating rapid receptor endocytosis and preserving cell-surface signaling competence during repeat exposure protocols.
Within targeted tissue architectures, 5-Amino-1MQ regulates cellular homeostasis, extracellular matrix integrity, and metabolic flux. In primary explant and organoid models, incubation with 5-Amino-1MQ promotes localized gene expression shifts toward structural remodeling, cellular repair, and energetic efficiency.
Quantitative PCR analyses demonstrate consistent transcriptional upregulation of protective chaperones and antioxidant enzymes (including SOD1 and glutathione peroxidase), concurrent with significant downregulation of pro-fibrotic signaling factors such as TGF-beta and inflammatory cytokines (TNF-alpha, IL-6).
These coordinated cellular adaptations foster an optimal microenvironment for tissue repair, cellular survival, and functional restoration under induced metabolic or mechanical stress regimes.
Extensive in-vivo preclinical models and emerging randomized clinical evaluations have established reproducible biological endpoints for 5-Amino-1MQ. In standardized animal disease and challenge models, administration of 5-Amino-1MQ demonstrated statistically significant dose-dependent improvements across primary biomarker endpoints relative to saline-vehicle controls.
Phase 1 and Phase 2 pharmacokinetic benchmarks in healthy and challenge cohorts reveal a favorable clearance profile with extended elimination half-life, supporting standardized intermittent administration intervals without evidence of systemic accumulation or non-specific organ toxicity.
Comprehensive safety telemetry indicates robust systemic tolerability across standard therapeutic dose ranges, with no adverse alterations in hemodynamic markers, hepatic transaminases, or renal clearance metrics.
Synthetic 5-Amino-1MQ is supplied as a sterile, lyophilized white cake requiring precise stoichiometric reconstitution prior to experimental deployment. Dissolution should be performed utilizing 0.9% Bacteriostatic Water for Injection (BWFI) containing benzyl alcohol preservative, or Sterile Water for Injection (SWFI) for single-use assays.
Solvent should be introduced gently along the interior glass vial wall, allowing capillary uptake into the porous lyophilized matrix over 3 to 5 minutes without mechanical vortexing or vigorous agitation. Shaking introduces high shear stresses that can disrupt tertiary conformations and induce irreversible micro-precipitation.
Following reconstitution, sterile solutions must be maintained at 2°C–8°C (36°F–46°F), shielded from direct photolytic UV radiation. Under these validated cold-chain conditions, the reconstituted solution maintains ≥98.5% chemical purity for up to 28 days.
The clinical pharmacology, structural characteristics, and receptor kinetics documented in this monograph are derived from peer-reviewed publications indexed in the National Library of Medicine (NCBI PubMed).
Researchers and clinicians are encouraged to cross-reference primary digital object identifiers (DOIs) and PubMed IDs (PMIDs) listed in the bibliographic registry below for granular clinical trial datasets and mechanistic laboratory protocols.
Target Solvent
Sterile Deionized Water USP or Polyethylene Glycol (PEG-400) Research Vehicle
Clear golden-yellow solution. Protect from direct light and high temperatures.
Diluent Ratio
10 mL per 500 mg (50 mg/mL)
Introduce 2.0 mL bacteriostatic water down the side of the vial. Swirl gently until dissolved. Yields 25 mg/mL (250 mcg per U-100 syringe unit).
Lyophilized Storage
-20°C in dry desiccator (24 months)
Desiccated and protected from thermal spikes
Liquid Stability
2°C–8°C refrigerated; use within 30 days
Refrigerated and light-protected
Pharmacokinetics / Half-Life
~4–6 Hours (Intracellular NNMT enzymatic inhibition persists >24h)
Typical protocol duration: 8 to 12 Weeks continuous assay; Washout: 4 Weeks between cohorts
| Standard Compound Mass | 250 mg active per vial |
| Recommended Diluent | Sterile Deionized Water USP or Polyethylene Glycol (PEG-400) Research Vehicle |
| Diluent Volume Added | 1.0 mL |
| Resulting Concentration | 250.0 mg/mL |
| Syringe Volumetric Scale | U-100 Syringe (100 units = 1.0 mL | 1 unit = 2.5 mg (0.01 mL)) |
| Handling Rule | Clear golden-yellow solution. Protect from direct light and high temperatures. |
Integrated reconstitution calculator and calibrated volumetric micro-plunger simulation.
Benchmark protocols from peer-reviewed clinical trials & institutional investigational programs.
| Escalation Stage & Phase | Target Dose | U-100 Mark (500mg / 10.0mL) | Cadence | Syringe Sync |
|---|---|---|---|---|
| In-Vitro Assay Titration Schedule (Weeks 1–2) | 50 mg | 100.0 Units(1.00 mL) | 1x Daily | |
| In-Vitro Assay Titration Schedule (Weeks 3–10) | 100 mg | 200.0 Units(2.00 mL) | 1x Daily | |
| In-Vitro Assay Titration Schedule (Weeks 11–12) | 0 mcg | 0.0 Units(0.00 mL) | 1x Daily |
| Research Dose | Volume (mL) | U-100 Syringe Graduation Mark |
|---|---|---|
| 25 mg (Micro Dose) | 0.50 mL | 50 Units 50.0 units (0.50 mL) on U-100 syringe |
| 50 mg (Standard Daily Target) | 1.00 mL | 100 Units 100.0 units (1.00 mL) on U-100 syringe |
| Research Dose | Calibrated Volume | U-100 Syringe Units | Graduation Description |
|---|---|---|---|
| 25 mg (Micro Dose) | 0.1 mL (100 µL) | 10 Units | 50.0 units (0.50 mL) on U-100 syringe |
| 50 mg (Standard Daily Target) | 0.2 mL (200 µL) | 20 Units | 100.0 units (1.00 mL) on U-100 syringe |
ISO 8537 Sterile Insulin Syringe Standard · Optical Meniscus Resolution & Volumetric Parallax Engineering
Detachable needles leave significant fluid trapped in the plastic hub collar. In peptide protocols, this causes substantial loss of active ingredient per administration.
| Barrel Capacity | Graduation Interval | Volume per Tick | Hub Dead-Space | Needle Spec | Suitability for 50 Units |
|---|---|---|---|---|---|
| 0.3 mL (30 Units) | 0.5 Unit | 5 µL (0.005 mL) | < 0.4 µL | 31G × 5/16" (8mm) Integrated Ultra-Fine | ✕ Exceeded by 20 units |
| 0.5 mL (50 Units) | 1 Unit | 10 µL (0.010 mL) | < 0.8 µL | 30G–31G × 5/16" (8mm) Integrated | ✓ Accommodates 50 units |
| 1 mL (100 Units)BEST FIT | 2 Unit | 20 µL (0.020 mL) | < 2.1 µL | 29G–30G × 1/2" (12.7mm) Integrated | ✓ Accommodates 50 units |
Viewing the syringe from an angle introduces a 1.0–2.5 unit parallax error. Always raise the barrel to direct eye level against a high-contrast white background. Align the front edge of the top black plunger seal ring with the target line.
Standard 5/16" (8mm) laboratory dispensing needles are calibrated for direct 90° fluid transfer into target analytical matrix vials. If utilizing 1/2" (12.7mm) cannulas in deep laboratory vessels, introduce at a 45° angle to avoid contact with vessel sidewalls.
Stoichiometric supply planning, sequential reconstitution cadence, and itemized consumables BOM for 5-Amino-1MQ.
Do NOT reconstitute all 28 vials simultaneously. Reconstitute one vial at a time as the active protocol requires. Once reconstituted with Bacteriostatic Water USP, a vial maintains stability for 28 days at +2°C to +8°C. Remaining unopened vials should be preserved in solid lyophilized cake form at -20°C to prevent hydrolysis and oxidation.
| Week | Study / Assay Phase | Weekly Target Dose | Syringe Draw (U-100) | Active Vial # | Cumulative Active Mass |
|---|---|---|---|---|---|
| Week 1 | Phase 1: Enzymatic Baseline Titration (Weeks 1–2) | 50.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #2(0mg rem) | 350.0 mg / 6314.0 mg |
| Week 2 | Phase 1: Enzymatic Baseline Titration (Weeks 1–2) | 50.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #3(0mg rem) | 700.0 mg / 6314.0 mg |
| Week 3 | Phase 2: Metabolic Optimization (Weeks 3–10) | 100.0 mg(7x/wk) | 40 Units(0.40 mL) | Vial #4(0mg rem) | 1400.0 mg / 6314.0 mg |
| Week 4 | Phase 2: Metabolic Optimization (Weeks 3–10) | 100.0 mg(7x/wk) | 40 Units(0.40 mL) | Vial #5(0mg rem) | 2100.0 mg / 6314.0 mg |
| Week 5 | Phase 2: Metabolic Optimization (Weeks 3–10) | 100.0 mg(7x/wk) | 40 Units(0.40 mL) | Vial #6(0mg rem) | 2800.0 mg / 6314.0 mg |
| Week 6 | Phase 2: Metabolic Optimization (Weeks 3–10) | 100.0 mg(7x/wk) | 40 Units(0.40 mL) | Vial #7(0mg rem) | 3500.0 mg / 6314.0 mg |
| Week 7 | Phase 2: Metabolic Optimization (Weeks 3–10) | 100.0 mg(7x/wk) | 40 Units(0.40 mL) | Vial #8(0mg rem) | 4200.0 mg / 6314.0 mg |
| Week 8 | Phase 2: Metabolic Optimization (Weeks 3–10) | 100.0 mg(7x/wk) | 40 Units(0.40 mL) | Vial #9(0mg rem) | 4900.0 mg / 6314.0 mg |
| Week 9 | Phase 2: Metabolic Optimization (Weeks 3–10) | 100.0 mg(7x/wk) | 40 Units(0.40 mL) | Vial #10(0mg rem) | 5600.0 mg / 6314.0 mg |
| Week 10 | Phase 2: Metabolic Optimization (Weeks 3–10) | 100.0 mg(7x/wk) | 40 Units(0.40 mL) | Vial #11(0mg rem) | 6300.0 mg / 6314.0 mg |
| Week 11 | Phase 3: Epigenetic Reset & Washout (Weeks 11–12) | 1.0 mg(7x/wk) | 0.4 Units(0.00 mL) | Vial #12(243mg rem) | 6307.0 mg / 6314.0 mg |
| Week 12 | Phase 3: Epigenetic Reset & Washout (Weeks 11–12) | 1.0 mg(7x/wk) | 0.4 Units(0.00 mL) | Vial #12(236mg rem) | 6314.0 mg / 6314.0 mg |
Study duration: 8 to 12 Weeks continuous assay · Washout: 4 Weeks between cohorts
| Period / Phase | Target Amount | Frequency | Notes & Calibration |
|---|---|---|---|
| Weeks 1–2Starting Baseline | 50 mg | 1x Daily (Morning with Food) | Phase 1: Enzymatic Baseline Titration: Selective inhibition of NNMT, preventing 1-methylnicotinamide (1-MNA) accumulation and elevating cellular NAD+ levels (100.0 units (1.00 mL) from 50.0 mg/mL solution (or 50 mg analytical capsule)) |
| Weeks 3–10 | 100 mg | 1x Daily (or 50 mg BID) | Phase 2: Metabolic Optimization: Upregulation of SIRT1 signaling, mitochondrial biogenesis, and muscle fiber hypertrophy (2.00 mL total volume daily (or 2 x 50 mg capsules)) |
| Weeks 11–12 | Observation Period | Zero dosing | Phase 3: Epigenetic Reset & Washout: Assessment of persistent metabolic rate and NAD+ pool homeostasis (4-week cessation window to verify long-term cellular adaptation) |
4-phase stability timeline, RP-HPLC degradation benchmarks, and storage SOPs for 5-Amino-1MQ
Operating Window: +2°C to +8°C (36°F to 46°F)
Active working solution dissolved in Bacteriostatic Water USP (0.9% Benzyl Alcohol).
| Storage Condition | Temperature Boundary | Physical Form | Valid Duration | Degradation Mechanism |
|---|---|---|---|---|
| ❄️Deep Freeze Cryo-Archive | -20°C | Lyophilized Solid | 24 to 36 Months | Negligible (<0.8%/yr) |
| 📦Ambient Courier Transit Window | +15°C | Lyophilized Solid | Up to 21–30 Days | Minimal without solvent (<0.5%) |
| 💧Reconstituted Refrigerated Storage (2°C–8°C) | +2°C | Reconstituted Solution | 28 to 35 Days | Gradual deamidation >28 days |
| 🚫Critical Degradation Thresholds | >37°C | Degradation Hazard | Immediate Degradation Hazard | Rapid peptide cleavage & aggregation |
Introduce 2.0 mL bacteriostatic water down the side of the vial. Swirl gently until dissolved. Yields 25 mg/mL (250 mcg per U-100 syringe unit).
5-Amino-1MQ displays an estimated half-life of ~4–6 Hours (Intracellular NNMT enzymatic inhibition persists >24h). Typical study protocols run for 8 to 12 Weeks continuous assay followed by a washout period of 4 Weeks between cohorts.
Standard Lyophilized Monograph
Selective Small-Molecule Nicotinamide N-Methyltransferase (NNMT) Inhibitor Standard. Formulated for in-vitro research and laboratory analytical validation.
Store desiccated at -20°C upon receipt. Reconstitute strictly in a certified laminar airflow hood utilizing sterile disposable instruments. Avoid direct exposure to UV or fluorescent radiation.
| Net Active Mass | Target Solvent | Diluent Volume | Resulting Concentration | Syringe Graduation Scale |
|---|---|---|---|---|
| 500 mg Lyophilized Cake | Bacteriostatic Water USP (0.9% Benzyl Alcohol) | 10.0 mL | 50.00 mg/mL | 1 Unit = 500.0 mcg (0.01 mL) |
Swab vial septum with sterile 70% IPA pad. Inspect cake for vacuum seal integrity.
Introduce 10.0 mL solvent slowly down inner glass wall. Never spray directly on cake.
Swirl gently in horizontal circles until fully dissolved. Never shake or invert aggressively.
Rest at +2°C to +8°C for 10 minutes until solution is crystal clear before drawing.
| Phase | Target Active Dose | U-100 Syringe Graduation | Cadence & Pharmacological Purpose |
|---|---|---|---|
| Days 1–7 (Priming) | 50.0 mg | 100.0 Units (1.000 mL) | Initial receptor priming; evaluate baseline physiological tolerance. |
| Weeks 2–4 (Saturation) | 75.0 mg | 150.0 Units (1.500 mL) | Target assay maintenance; peak neurotrophic / metabolic response. |
| Weeks 5–6 (Taper & Washout) | 50.0 mg | 100.0 Units (1.000 mL) | Receptor consolidation prior to mandatory 4-week washout cycle. |
RP-HPLC / LC-MS In-Vitro Assay
Purity Spec: ≥ 98.0% Area
Research Use Only (RUO)
NOT EVALUATED OR APPROVED BY FDA