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White pill bottle labeled 'AC-262 10 mg' with capsules on a beige background
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AC-262 100x10mg

AC-262 100x10mg

€55,00 EUR
Taxes included.

                                                  NOT FOR HUMAN CONSUMPTION

AC-262 is an oral, non-steroidal selective androgen receptor modulator (SARM) discovered in the early Acadia/industry SARM programs. It binds the androgen receptor (AR) and drives ARE-regulated transcription with a muscle/bone-biased anabolic profile and comparatively less prostate/skin stimulation than testosterone. AC-262,536 is not FDA/EMA-approved and is prohibited by WADA as an anabolic agent.

Additional Benefits of AC-262,536 Now Under Investigation

Benefit Key take-aways
1 Anabolic effect with partial-agonist safety Preclinical studies show lean-mass gain and myofiber hypertrophy with attenuated prostate stimulation versus testosterone—consistent with partial AR agonism and co-activator selectivity. <br/><em>Journal of Medicinal Chemistry; JPET</em>
2 Functional strength Rodent/bench models report increased specific force and grip strength, aligning molecular anabolism with performance endpoints. <br/><em>FASEB Journal; MSSE</em>
3 Bone support In osteopenic models, SARMs in this chemical class raise BMD, improve trabecular architecture, and enhance three-point bend strength with minimal androgenic effects—AC-262 follows this trend. <br/><em>Journal of Bone and Mineral Research; Bone</em>
4 Anti-catabolic protection Under disuse, glucocorticoid, or illness stress, AC-262–class signaling down-shifts atrogenes (MAFbx/MuRF1) and preserves CSA. <br/><em>AJP–Endocrinology; Endocrine Reviews</em>
5 Lower sebaceous/prostate drive (vs testosterone) Lack of 5-α reduction and aromatization helps limit DHT/E2-mediated side effects per mg anabolic effect. <br/><em>J Pharmacol Exp Ther</em>
6 Oral convenience Intended once-daily oral dosing improves adherence in research settings compared with injectables. <br/><em>Clinical Pharmacology & Therapeutics</em>
7 Rehab synergy Additive improvements when paired with progressive resistance training and adequate protein intake (preclinical → feasibility). <br/><em>Sports Medicine</em>
8 Hematologic tone (modest) AR activation may slightly raise hemoglobin/hematocrit below testosterone’s magnitude—monitor in at-risk individuals. <br/><em>Hematology; Andrology</em>
9 Doping-control relevance Long-term metabolites enable weeks-long detection; positives and supplement contaminations have been reported. <br/><em>Drug Testing & Analysis</em>

2. Molecular Mechanism of Action

2.1 Receptor Pharmacodynamics

AC-262,536 binds AR → nuclear translocation → ARE transcription. In skeletal muscle it up-regulates mTOR/S6K/4E-BP1 and local IGF-1, while suppressing FoxO-driven atrogenes. Partial agonism and ligand-specific co-activator recruitment underlie tissue selectivity vs testosterone.

2.2 Down-stream Biology

Pathway Functional outcome Context
AR → mTOR/S6K ↑ protein synthesis, myofiber hypertrophy Skeletal muscle
AR ↔ Wnt/β-catenin/Osterix ↑ osteoblast activity, ↑ BMD Bone
↓ FoxO/MAFbx/MuRF1 ↓ proteolysis (anti-catabolic) Catabolic stress
HPG feedback ↓ LH/FSH/testosterone (suppression) Pituitary–gonadal axis

3. Pharmacokinetics

  • Route: Oral.

  • Half-life/exposure: Human PK not formally published; rodent PK supports once-daily paradigms.

  • Metabolism: Hepatic oxidative/conjugative clearance typical of non-steroidal SARMs; no aromatase/5-αpathways.

  • Detection: Anti-doping labs report identifiable urinary metabolites enabling long detection windows.

4. Pre-clinical and Translational Evidence

4.1 Muscle & Function

Preclinical dosing increases lean mass, CSA, and force with reduced prostate weight versus testosterone controls.

4.2 Bone

SARM-class effects include BMD and strength gains in ovariectomized/castrated models; AC-262,536 follows similar bone-anabolic signatures.

4.3 Human data

No completed pivotal trials publicly available. Most efficacy/safety knowledge derives from animal studies, in-vitro data, and forensic anti-doping literature.

Evidence quality note: AC-262,536 has limited, primarily preclinical evidence. Any human efficacy/safety inferences are hypothesis-generating.

5. Emerging Clinical Interests

Field Rationale Current status
Sarcopenia/frailty Oral anabolic with selective profile Preclinical/early translational
Rehabilitation/immobilization Preserve lean mass, improve function Concept/pilot frameworks
Osteopenia Bone-anabolic without high prostate drive Preclinical
Cachexia Appetite-neutral anabolic alternative Preclinical

6. Safety and Tolerability

  • Endocrine: Dose-dependent HPG suppression (↓ LH/FSH/testosterone) expected; recovery typically weeks after stop.

  • Lipids: HDL-C reductions (± ↑ LDL/TG) common in SARM class—monitor CV risk.

  • Hepatic: Short-term SARM studies show small median ALT/AST shifts, but real-world cases of liver injury have occurred with unregulated SARM products.

  • CV: No outcomes data; lipid shifts warrant caution.

  • Dermatologic: Possible acne/oiliness; hair shedding in predisposed.

  • Neuropsych: Occasional insomnia/irritability reported for the class.

  • Drug interactions: Potential with hepatic enzyme modulators; avoid in pregnancy.

Comparative safety matrix

Concern AC-262,536 Enobosarm (MK-2866) LGD-4033
Human evidence Very limited Phase 2 signals Small RCT (21 d)
HPG suppression Moderate (expected) Moderate Moderate
HDL impact Likely ↓ ↓ ↓
Prostate stimulation Low (preclinical) Low Low
Oral dosing Once daily (intended) Once daily Once daily

7. Regulatory Landscape

  • Approvals: None.

  • Sport: WADA-prohibited (S1 Anabolic Agents) at all times; strict liability for athletes.

  • Supply: Often appears in research-chemical markets; adulteration/mislabeling common.

8. Future Directions

  • First-in-human PK/PD with GMP supply: define half-life, metabolites, exposure–response.

  • Head-to-head vs other SARMs on anabolic:androgenic ratio, lipid neutrality, and HPG suppression.

  • Long-term safety: lipids/CV, hepatic, endocrine recovery, mood/CNS.

  • Rehab/sarcopenia trials coupled with standardized resistance training and protein targets.

  • Doping science: comprehensive metabolite ID and detection windows.

Selected References

  • Journal of Medicinal Chemistry; Journal of Pharmacology & Experimental Therapeutics — Discovery and pharmacology of non-steroidal SARMs including AC-262,536.

  • FASEB Journal; American Journal of Physiology–Endocrinology — SARM anti-catabolic signalling (mTOR up, FoxO/atrogenes down).

  • Journal of Bone and Mineral Research; Bone — SARM effects on BMD and biomechanical strength in osteopenic models.

  • Clinical Pharmacology & Therapeutics — Oral SARM PK/PD principles.

  • Drug Testing & Analysis — Identification of AC-262,536 metabolites and anti-doping detection.

  • Hepatology Communications; J Clin Transl Hepatol — Case reports of liver injury associated with unregulated SARM use (class context)