What Are SARMs?
SARM stands for Selective Androgen Receptor Modulator. SARMs are a class of synthetic compounds designed to bind the androgen receptor (AR) and activate it in a tissue-selective way — producing anabolic (muscle-building, bone-strengthening) effects in target tissues while minimizing androgenic effects in non-target tissues such as the prostate, scalp, and sebaceous glands.
The "selectivity" concept is the defining feature: traditional androgens (testosterone, DHT) activate AR equally across all tissues, producing a spectrum of both wanted effects (muscle, bone) and unwanted effects (prostate enlargement, virilization, hair loss). SARMs were developed to decouple these effects.
SARMs are currently in various stages of clinical research for conditions including muscle wasting, sarcopenia, cancer cachexia, osteoporosis, and male hypogonadism. None are approved as therapeutic products by any regulatory authority as of 2026. All research chemical supply is For Research Use Only.
Androgen Receptor Mechanism
The androgen receptor (AR) is a ligand-activated transcription factor. When activated:
- Androgens or SARMs bind the AR ligand-binding domain
- AR undergoes conformational change, translocates to nucleus
- AR dimerizes and binds androgen response elements (AREs) in DNA
- Recruits tissue-specific coactivator/corepressor complexes
- Drives tissue-specific gene expression programs
The tissue selectivity of SARMs arises from step 4: different tissues express different coactivator proteins. When a SARM binds AR, it produces a slightly different receptor conformation vs testosterone — recruiting different coactivators in different tissues, producing different gene expression outcomes.
SARMs vs Anabolic Steroids
| Property | Non-Steroidal SARMs | Anabolic Steroids (e.g. Testosterone) |
|---|---|---|
| Chemical structure | Non-steroidal small molecule | Steroidal backbone (cyclopentanoperhydrophenanthrene) |
| AR selectivity | Tissue-selective agonism | Non-selective; activates AR uniformly |
| 5α-reduction (→DHT) | Not applicable | Yes — amplifies androgenic effects in prostate/skin |
| Aromatization (→E2) | No (most SARMs) | Yes — estrogen effects at high doses |
| Oral bioavailability | High (most SARMs, 90%+) | Variable; many require injection or 17α-alkylation |
| Hepatotoxicity | Lower risk (no 17α-AA) | Oral 17α-alkylated steroids: hepatotoxic |
| Regulatory status (US) | Research chemicals (unscheduled) | Schedule III controlled substances |
| Approved therapeutic uses | None (investigational) | Yes (TRT, delayed puberty, wasting) |
Types of SARMs: The Research Compound Class
The "SARM" market category includes several mechanistic classes:
- Non-steroidal AR agonists (true SARMs): RAD-140, LGD-4033, Ostarine (MK-2866), Andarine (S4) — these bind AR directly with tissue selectivity
- Ghrelin receptor agonists: MK-677 (Ibutamoren) — stimulates GH release; does not bind AR; grouped with SARMs for commercial/research categorization
- Rev-erb agonists: SR9009 (Stenabolic) — activates Rev-erb nuclear receptors; circadian and metabolic biology; grouped with SARMs commercially
- PPARδ agonists: Cardarine (GW501516) — activates PPARδ; fatty acid oxidation; grouped with SARMs commercially
- Steroidal SARMs: YK-11 — steroidal backbone; partial AR agonism + follistatin induction
- SERMs (related category): Enclomiphene — ER modulator for HPTA axis; often co-studied with SARMs
Clinical Development Status (2026)
| SARM | Developer | Max Stage | Indication | Status |
|---|---|---|---|---|
| Ostarine (MK-2866) | GTx / Oncternal | Phase III | Cancer cachexia (NSCLC) | Discontinued (mixed Phase III) |
| LGD-4033 (VK5211) | Viking Therapeutics | Phase II | Hip fracture rehabilitation | Phase III planned |
| RAD-140 | Radius Health | Phase I | ER+ breast cancer | Discontinued |
| MK-677 | Merck → Ardea | Phase III | GH deficiency, frailty | No approval; development paused |
| Enclomiphene | Repros → Androvia | Phase III | Secondary hypogonadism | FDA CRL; development ongoing |
WADA & Anti-Doping Status
All SARMs are prohibited in sport under WADA's Prohibited List:
- S1 — Anabolic Agents: RAD-140, LGD-4033, Ostarine, Andarine, YK-11 and all other AR-binding SARMs
- S2 — Peptide Hormones, Growth Factors: MK-677 (GH secretagogue)
- S4 — Hormone Modulators: Some SERMs including enclomiphene
Rainbow Peptide does not supply products for athletic performance enhancement. All products are For Research Use Only.