Side-by-side · Research reference
5-Amino-1MQvsLL-37
Side-by-side comparison across mechanism, dosage, evidence, side effects, administration, and stack synergies. Citations on every claim where available.
AAnimal-StrongAUTO-DRAFTED8/38 cited
BHuman-MechanisticHUMAN-REVIEWED15/35 cited
5-Amino-1MQ
NNMT inhibitor · Methylation / SAM modulation
Oral · Once daily fasted
LL-37
Cathelicidin · Human AMP
Broad-spectrumAntimicrobial activity
Endogenous · Secreted at inflammation sites
01Mechanism of Action
Parameter
5-Amino-1MQ
LL-37
Primary target
Nicotinamide N-methyltransferase (NNMT)Neelakantan 2018
Pathway
NNMT inhibition → preserved cellular SAM + NAD⁺ → restored methylation balance + ↑ thermogenic gene expressionNeelakantan 2018
hCAP-18 precursor → Proteinase-3 cleavage → LL-37 release → Membrane insertion/disruption
Downstream effect
Reversal of HFD-induced obesity in murine models; improved metabolic profileNeelakantan 2018
Membrane permeabilization, cytokine induction, autophagy, phagosome-lysosome fusion, chemotaxisAhmad 2026Zhang 2026
Feedback intact?
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Origin
Selective small-molecule inhibitor designed in academic medicinal chemistry programsNeelakantan 2018
Endogenous human cathelicidin (37-AA fragment, residues 134–170 of hCAP-18)
Antibody development
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02Dosage Protocols
Parameter
5-Amino-1MQ
LL-37
Frequency
Once daily, fasted
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Lower / starter dose
50 mg / day
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Evidence basis
Animal-strong; no human RCT dataNeelakantan 2018
In vitro, animal models, human observational
Duration
8–12 weeks per cycle
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Form
Oral capsule
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Timing
Morning fasted preferred
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Half-life
Hours (estimated; no human PK published)
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Endogenous expression
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Constitutive in neutrophils, epithelial tissues
Upregulated during infection and inflammation.Pinheiro 2026
Exogenous (experimental)
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Dose varies by study; antimalarial ~10–50 μM in vitro
No FDA-approved exogenous formulation.
04Side Effects & Safety
Parameter
5-Amino-1MQ
LL-37
GI symptoms
Mild nausea (anecdotal)
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Methylation disruption
Theoretical risk if NNMT is over-inhibited (B vitamin metabolism)
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Long-term safety
Unknown — no human trials
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Cancer risk
Unclear — NNMT also studied in oncology contexts
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Pregnancy / OB
Avoid
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Drug interactions
Theoretical with niacin / B-vitamin supplements
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Cytotoxicity (high dose)
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Membrane disruption in host cells at supraphysiological concentrations
Pro-inflammatory signaling
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Can exacerbate inflammation in certain contexts (context-dependent)Pinheiro 2026
Theoretical cancer risk
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Immunomodulatory roles in tumor microenvironment under investigation
Absolute Contraindications
5-Amino-1MQ
- ·Pregnancy / breastfeeding
- ·Active malignancy
LL-37
—Relative Contraindications
5-Amino-1MQ
- ·Methylation-sensitive conditions (MTHFR mutation)
- ·Concurrent niacin / NAD+ precursor supplementation (theoretical interference)
LL-37
- ·Active autoimmune disease (theoretical immune dysregulation)
05Administration Protocol
Parameter
5-Amino-1MQ
LL-37
1. Form
Oral capsule. No injection.
LL-37 is constitutively expressed in neutrophils and epithelial cells, cleaved from hCAP-18 by proteinase-3 at sites of infection or inflammation.
2. Administration
Take with water, fasted preferred.
Synthetic LL-37 and derivatives (e.g., SAMP-12aa) tested in vitro and animal models. Administered via topical, intraperitoneal, or intravenous routes in research settings.
3. Timing
Morning fasted.
LL-37 is resistant to pepsin degradation at gastric pH. Synthetic short peptides designed to retain this stability while reducing toxicity.Lu 2026
4. Storage
Room temp ≤25 °C, dry place.
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5. Caveat
Monitor B-vitamin status with chronic use.
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