ACE-031 (1mg)

Description

ACE-031 Peptide (CE-031): Myostatin Inhibition for Muscle Growth and Metabolic Support

ACE-031, also known as ActRIIB-IgG1 peptide or soluble activin type IIB receptor (ActRIIB-IgG1-Fc), is a synthetic peptide that functions as a myostatin inhibitor. It is a fusion compound combining the activin receptor type IIB (ACV2RB) and a recombinant IgG1 Fc antibody, which allows it to circulate in the bloodstream and target specific growth factors.

Myostatin, or GDF8, is a negative regulator of skeletal muscle growth. It binds to ACV2RB receptors, activating a signaling cascade through Smad2/3, which limits muscle hypertrophy. ACE-031 appears to block circulating myostatin and other ligands from the TGF-β superfamily, keeping the ACV2RB receptors available. As a result, skeletal muscle growth is promoted, potentially enhancing muscle mass, metabolism, and bone density without affecting cardiac or smooth muscle.

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Chemical Composition of ACE-031

• Molecular Formula: C₃₄₁₈H₅₁₈₈N₉₂₈O₁₀₆₂S₃₈

• Molecular Weight: 77,489.82 g/mol

• Other Names: ActRIIB-IgG1 peptide, soluble activin type IIB receptor

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Research and Clinical Insights

ACE-031 and Muscle Hypertrophy

In double-blind, placebo-controlled studies, ACE-031 demonstrated significant muscle growth. After 29 days, participants exhibited a 3.3% increase in total body lean mass and a 5.1% increase in quadriceps volume, measured using DXA and MRI. Serum biomarkers also suggested enhanced bone and fat metabolism, reflecting the peptide’s potential systemic benefits.

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ACE-031 and Fat Metabolism

Research indicates that myostatin overexpression in obesity models correlates with decreased muscle mass and increased fat accumulation. ACE-031 may counteract these effects by:

1. Upregulating lipolysis and fatty acid oxidation enzymes (e.g., CPT1a, CPT2), enhancing energy use and reducing lipid storage.

2. Promoting brown/beige fat formation, converting energy-storing white fat into thermogenic fat that burns calories.

Animal studies show ACE-031 may reduce obesity phenotypes and limit fat accumulation under high-calorie diets.

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ACE-031 and Muscle Contractile Force

ACE-031 may improve muscle performance beyond hypertrophy. Studies in murine models report:

• 33% increase in muscle volume without altering fiber type distribution

• 22% rise in basal oxygen consumption

• 23% increase in energy expenditure

• Enhanced maximum and total contractile force by 40% and 24%, respectively

These effects suggest ACE-031 may optimize metabolic and contractile functions of skeletal muscles.

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ACE-031 and Bone Density

In murine models of Duchenne Muscular Dystrophy, ACE-031 increased femoral bone volume by ~80% and trabecular number by +70%. Vertebral bone mass also increased by 20–30%. Histological studies reported fewer osteoclasts and higher expression of osteoblast marker genes, indicating improved bone formation and reduced resorption. Biomechanical testing confirmed increased bone strength and stiffness, highlighting ACE-031’s potential for skeletal support.

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References:

1. Campbell C, McMillan HJ, Mah JK, Tarnopolsky M, Selby K, McClure T, Wilson DM, Sherman ML, Escolar D, Attie KM. Myostatin inhibitor ACE-031 treatment of ambulatory boys with Duchenne muscular dystrophy: Results of a randomized, placebo-controlled clinical trial. Muscle Nerve. 2017 Apr;55(4):458-464. https://pubmed.ncbi.nlm.nih.gov/27462804/
2. McPherron AC, Lawler AM, Lee SJ. Regulation of skeletal muscle mass in mice by a new TGF-beta superfamily member. Nature. 1997 May 1;387(6628):83-90. https://pubmed.ncbi.nlm.nih.gov/9139826/
3. Attie KM, Borgstein NG, Yang Y, Condon CH, Wilson DM, Pearsall AE, Kumar R, Willins DA, Seehra JS, Sherman ML. A single ascending-dose study of muscle regulator ACE-031 in healthy volunteers. Muscle Nerve. 2013 Mar;47(3):416-23. https://pubmed.ncbi.nlm.nih.gov/23169607/