ACE-031
aka ACVR2B-Fc
Mechanism
ACE-031 (ramatercept) is a soluble fusion protein of the activin receptor IIB (ActRIIB) extracellular domain and human IgG1 Fc, developed by Acceleron Pharma as a myostatin/activin ligand trap for muscle-wasting disorders. Clinical development was HALTED in 2011 after unexpected vascular adverse events (epistaxis, telangiectasia) attributed to off-target BMP-9/10 inhibition. NOT FDA-approved; all further development was terminated. Now sold only as a grey-market research chemical. WADA-prohibited (myostatin inhibitor).
Identification
| CAS number | 1621169-52-5 |
|---|---|
| Molecular formula | C133H227N43O33 |
| Typical dose | 0.02–3 mg/kg subcutaneous (single or every 2–4 weeks; based on Phase 1/2 clinical trials) |
| Half-life | ~10–15 days (human pharmacokinetic data from Phase 1 trial) |
Vendors selling ACE-031
| Vendor | Size | Price | Listed purity | Trust |
|---|---|---|---|---|
| Peptide Tech | 1 mg | $98.99 | — | 94 |
| Peptidology | 1 mg | $159.00 | — | 89 |
| Peptiatlas | — | — | — | 51 |
| zztai Peptide Ltd | — | — | — | 43 |
| Biotech Peptides | 1 mg | $161.00 | — | — |
| Core Peptides | 1 mg | $173.00 | — | — |
| Kimera Chems | — | $141.99 | — | — |
Research
Pharmacological blockade of ligands for the activin receptor type IIB (ActRIIB) e.g., myostatin and activin A is associated with improvements in murine skeletal muscle mass and function.
source →Background Orofacial and limb muscles differ in embryonic origin and regenerative capacity. Neuromuscular junction (NMJ) regeneration is critical for muscle restoration both histologically and functionally. The relative potential of orofacial and limb muscles to form postsynaptic apparatuses remains elusive.
source →Therapeutic peptides are short chains of amino acids used to treat metabolic and endocrine conditions such as obesity and type 2 diabetes.
source →Alongside the considerable advances and accomplishments in drug research and development, the breadth of anti-doping research topics has also continued to grow.
source →Myostatin (Mstn), a well-characterized member of the transforming growth factor-β (TGF-β) superfamily, serves as a key negative regulator of skeletal muscle mass. Its overactivation is closely associated with the pathogenesis of various musculoskeletal and metabolic disorders.
source →The usage of ACE-031 (Ramatercept), a dimeric fusion protein consisting of a human activin receptor IIB (ACVR2B) fragment linked to an Fc-part of human IgG1, is banned according to chapter S4.3 of the "WADA 2024 List of Prohibited Substances and Methods" due to its potential performance enhancing properties.
source →Glucagon-like peptide-1 receptor agonists (GLP-1 RAs) have demonstrated substantial weight loss effects among patients with diabetes and obesity. However, given the rapid weight loss induced, there is concern about the total change in body composition, including lean body mass (LBM).
source →The analytical and technological approaches employed in doping analysis are constantly reviewed and updated to allow for keeping pace with progresses in pharmaceutical and medicinal research and the therein inherent options of misuse as performance enhancing drugs or methods.
source →Osteosarcopenia (OS), a recently recognized syndrome characterized by the simultaneous occurrence of osteopenia/osteoporosis and sarcopenia, has emerged as an important concept in clinical practice.
source →The Myodural Bridge (MDB) is a physiological structure that is highly conserved in mammals and many of other tetrapods. It connects the suboccipital muscles to the cervical spinal dura mater (SDM) and transmits the tensile forces generated by the suboccipital muscles to the SDM.
source →Introduction ACE-031 is a fusion protein of activin receptor type IIB and IgG1-Fc, which binds myostatin and related ligands. It aims to disrupt the inhibitory effect on muscle development and provide potential therapy for myopathies like Duchenne muscular dystrophy (DMD).
source →Introduction ACE-031 is a soluble form of activin receptor type IIB (ActRIIB). ACE-031 promotes muscle growth by binding to myostatin and other negative regulators of muscle mass.
source →The purpose of this study is to determine if ACE-031 is safe and well-tolerated in boys with Duchenne Muscular Dystrophy (DMD) and to select the optimal doses of ACE-031 in terms of safety and pharmacodynamic (PD) activity for designing future studies. \[Note: This study was terminated based on safety data\]
source →To evaluate the long-term safety and tolerability of ACE-031 administration in subjects with Duchenne muscular dystrophy (DMD) who participated in Study A031-03. \[Note: This study was terminated based on preliminary safety data.
source →The purpose of this study is to establish safe dose levels of ACE-031 in healthy postmenopausal women following multiple dose administration. This study will also evaluate if ACE-031 has an effect on muscle.
source →Single center, randomized, single dose study to evaluate the safety, tolerability, pharmacokinetic and pharmacodynamic effects of ACE-031 in healthy postmenopausal volunteers
source →