Side-by-side · Research reference

5-Amino-1MQvsACE-031

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

BPhase 2HUMAN-REVIEWED10/44 cited

5-Amino-1MQ

NNMT inhibitor · Methylation / SAM modulation

100–200 mgDaily dose (oral)Neelakantan 2018

AnimalEvidence levelNeelakantan 2018

HoursHalf-life (est)

Oral · Once daily fasted

ACE-031

ActRIIB-Fc Fusion · Phase 2 Halted

Phase 2Highest trial stage

2011Development halted

~58.4 kDaMolecular weightReichel 2025

SQ · Weekly dosing investigated

01Mechanism of Action

Parameter

5-Amino-1MQ

ACE-031

Primary target

Nicotinamide N-methyltransferase (NNMT)Neelakantan 2018

Myostatin, GDF11, activin A — TGF-β superfamily ligands

Pathway

NNMT inhibition → preserved cellular SAM + NAD⁺ → restored methylation balance + ↑ thermogenic gene expressionNeelakantan 2018

Soluble decoy receptor binds circulating myostatin/TGF-β ligands → prevents ActRIIB activation → SMAD2/3 pathway inhibition

Downstream effect

Reversal of HFD-induced obesity in murine models; improved metabolic profileNeelakantan 2018

Disinhibition of myogenic signaling, increased skeletal muscle mass and strength

Feedback intact?

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Origin

Selective small-molecule inhibitor designed in academic medicinal chemistry programsNeelakantan 2018

Recombinant fusion protein: human ActRIIB extracellular domain + IgG1-Fc fragmentReichel 2025

Antibody development

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02Dosage Protocols

Parameter

5-Amino-1MQ

ACE-031

Standard dose

100–200 mg / day oralNeelakantan 2018

Anecdotal community range; murine doses scaled.

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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

Phase 2 trial discontinued — incomplete dataset

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)

Days to weeks (Fc-fusion typical kinetics)

IgG1-Fc domain confers extended circulation time.

Clinical dosing

—

Weekly or biweekly SQ injections (exact doses undisclosed pre-halt)

Phase 2 DMD trial protocol not fully published.

Black market products

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Variable purity; 12/14 tested products contained target protein plus contaminantsReichel 2025

SDS-PAGE revealed multiple protein bands; quality control absent.Reichel 2025

Duration investigated

—

12–24 weeks (trial cut short)

04Side Effects & Safety

Parameter

5-Amino-1MQ

ACE-031

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

—

Pregnancy / OB

Avoid

—

Drug interactions

Theoretical with niacin / B-vitamin supplements

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Epistaxis (nosebleeds)

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Significant incidence in Phase 2 DMD trial — primary safety signal

Telangiectasia

—

Dilated capillaries / spider veins observed

Vascular abnormalities

—

Mechanism: ActRIIB/ALK1 pathway disruption affects vascular homeostasis

Injection site reactions

—

Local erythema, induration (biologics class effect)

Antibody development

—

Potential for anti-drug antibodies (Fc-fusion proteins); incidence not reported

Black market contaminants

—

12/14 tested products contained multiple unidentified proteins alongside ACE-031Reichel 2025

Absolute Contraindications

5-Amino-1MQ

·Pregnancy / breastfeeding
·Active malignancy

ACE-031

·History of vascular disorders (epistaxis, telangiectasia, HHT)
·Pregnancy (TGF-β pathway critical for fetal development)
·Active malignancy (myostatin inhibition may affect tumour growth)
·Use of non-pharmaceutical grade ACE-031 (contamination risk)Reichel 2025

Relative Contraindications

5-Amino-1MQ

·Methylation-sensitive conditions (MTHFR mutation)
·Concurrent niacin / NAD+ precursor supplementation (theoretical interference)

ACE-031

·Coagulation disorders or anticoagulant use (epistaxis risk)
·Hereditary hemorrhagic telangiectasia (HHT) family history
·Cardiovascular disease (vascular remodeling effects unknown)

05Administration Protocol

Parameter

5-Amino-1MQ

ACE-031

1. Form

Oral capsule. No injection.

ACE-031 is not FDA-approved or commercially available. Phase 2 development was discontinued in 2011 due to safety concerns. Any ACE-031 on the black market is unregulated research chemical.

2. Administration

Take with water, fasted preferred.

12 of 14 tested black market ACE-031 products contained the target protein but also carried multiple unidentified protein contaminants detectable by SDS-PAGE. Two products contained no ACVR2B-immunoreactive material.Reichel 2025

3. Timing

Morning fasted.

ACE-031 is prohibited under WADA S4.3 (Myostatin Inhibitors). Gel electrophoresis and Western blotting using ACVR2B-specific antibodies can detect the ~58.4 kDa protein in biological samples.Reichel 2025

4. Storage

Room temp ≤25 °C, dry place.

Phase 2 protocol used subcutaneous injections at weekly or biweekly intervals. Exact dosing protocols remain unpublished.

5. Caveat

Monitor B-vitamin status with chronic use.

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