5-amino-1mq 5 mg*10vials Kit

Description

🧪 Compound Profile: 5-Amino-1MQ

Chemical Name: 5-Amino-1-methylquinolin-1-ium iodide
Synonyms: NNMTi; 5-amino-1-methylquinolinium iodide; 5-Amino-1MQ
CAS Number: 42464-96-0
Category: Nicotinamide N-Methyltransferase (NNMT) inhibitor
Form: Brown to reddish-brown crystalline powder
Molecular Formula: C₁₀H₁₁IN₂
Molecular Weight: 286.11 g/mol
Purity: ≥98% (HPLC, TFA-free formulation)

🔬 Key Properties

• Structural Characteristics:
  • Quinolinium cation core with amino group at C5 position
  • Iodide counterion for enhanced aqueous solubility
  • X-ray crystallography: Orthorhombic crystal system (P2₁2₁2₁ space group)
• Solubility Profile:
  • Water: 25 mg/mL (87.4 mM, clear orange solution)
  • PBS buffer (pH 7.4): 18.3 mg/mL (64.0 mM)
  • DMSO: 12.5 mg/mL (43.7 mM, stable for 30 days at -20°C)
• Stability Requirements:
  • Storage: 2-8°C under inert gas, protected from light
  • Shelf life: 24 months as supplied; 6 months after reconstitution
  • pH stability range: 4.0-8.5 (no degradation observed over 72 hours)

🧠 Mechanism of Action

As a selective NNMT inhibitor, 5-amino-1MQ modulates cellular metabolism through:

• Enzymatic Inhibition: Binds to NNMT active site with Ki=36 nM, competing with SAM (S-adenosylmethionine) substrate
• NAD+ Pathway Regulation: Prevents conversion of nicotinamide (NAM) to 1-methylnicotinamide (MNAM), increasing NAM availability for NAD+ synthesis
• Sirtuin Activation: Elevates SIRT1 activity (EC₅₀=1.2 μM) through NAD+ pool expansion
• Muscle Stem Cell Modulation: Promotes myogenic differentiation via upregulation of MyoD and myogenin expression

🧪 Research Applications

The compound shows promise in multiple preclinical research areas:

1. Metabolic Disorders

• Obesity Models: Reduces white adipose tissue mass by 17-23% in high-fat diet-fed mice (10 mg/kg IP, q.d. for 28 days)
• Hepatic Steatosis: Decreases liver triglyceride content by 31% in ob/ob mice
• Insulin Sensitivity: Improves glucose tolerance test (GTT) results with AUC reduction of 27% in diabetic rodent models

2. Muscle Regeneration

• Myogenesis Promotion: Increases C2C12 myoblast fusion index to 68.4±3.2% vs. 41.2±2.7% in controls
• Aging Muscle Repair: Enhances muscle stem cell (MuSC) regenerative capacity in 22-month-old mice (5 mg/kg SC, weekly injections)
• Atrophy Prevention: Attenuates disuse muscle loss by 42% in hindlimb suspension model

3. Aging and Longevity

• Sirtuin Pathway Activation: Upregulates SIRT1/3 expression in skeletal muscle (1.8-fold and 1.5-fold respectively)
• Oxidative Stress Reduction: Decreases ROS levels by 34% in human dermal fibroblasts
• Mitochondrial Function: Increases ATP production by 29% in C2C12 myotubes

⚙️ Experimental Protocols

• In Vitro Treatment:
  • Cell culture: 1-10 μM in serum-free DMEM (preferred)
  • Incubation time: 24-72 hours for myogenic differentiation assays
  • Vehicle control: 0.1% DMSO (no cytotoxicity observed)
• In Vivo Administration:
  • Rodent dosing: 5-20 mg/kg via intraperitoneal or subcutaneous injection
  • Delivery optimization: Formulate in 10% Captisol® for enhanced bioavailability
  • Tissue distribution: Peak concentration in liver (Tmax=1.2 h) and skeletal muscle (Tmax=2.5 h)

📊 Research Data Summary

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⚠️ Safety & Handling

• Hazard Classification: Not classified under GHS criteria for research use
• Precautionary Statements:
  • Avoid dust inhalation (use fume hood for weighing)
  • Wear nitrile gloves and safety goggles during preparation
  • Dispose as hazardous waste (D009) in accordance with local regulations
• Toxicity Profile:
  • Acute oral LD₅₀ (mouse): >2000 mg/kg
  • No observable adverse effects at therapeutic doses in 28-day studies
  • Potential interference with thyroid function at concentrations >50 μM

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📦 Packaging & Storage

• Standard Packaging: 10 mg, 50 mg, and 100 mg amber glass vials
• Storage Conditions:
  • Short-term (1 month): 4°C desiccated
  • Long-term: -20°C under nitrogen atmosphere
  • Reconstituted solution: Stable for 7 days at 4°C (protect from light)
• Quality Control:
  • Endotoxin level: <0.1 EU/mg
  • Heavy metals: <10 ppm
  • Residual solvents: MeOH <0.5%, EtOAc <0.5%