Metabolic Peptides

Tesofensine (NS2330, triple monoamine reuptake inhibitor)

Tesofensine is a non-peptide triple monoamine reuptake inhibitor that raises synaptic serotonin, norepinephrine, and dopamine, tracked in the weight-research community for its appetite effects. A Danish Phase 2 study (Astrup, Lancet 2008) reported placebo-subtracted weight loss that outpaced early comparators, though the journal later issued an expression of concern; a Mexican Phase 3 program met its endpoint and sits with COFEPRIS, with a final decision still pending as of 2026 (the widely-repeated '2022 Mexico approval' is inaccurate). The combination Tesomet is in development for hypothalamic obesity and Prader-Willi syndrome. It is research-only in the US; the platform indexes lab-verified COAs and pricing per source.

Cagrilintide (AM833, long-acting amylin analog)

Cagrilintide is a long-acting amylin analog that engages amylin and calcitonin receptors in the brainstem to promote satiety and slow gastric emptying — a mechanism complementary to GLP-1 drugs, which is why Novo Nordisk pairs it with semaglutide as CagriSema. Phase 2 monotherapy showed dose-dependent weight loss, and the Phase 3 REDEFINE 1 trial of the combination reported roughly 22.7% mean body-weight reduction over 68 weeks. Novo Nordisk submitted a CagriSema NDA in December 2025; it is under FDA review in 2026 and not yet approved, and standalone cagrilintide has no approval. The platform indexes lab-verified COAs and pricing per source.

Semaglutide (GLP-1 agonist)

Semaglutide is a long-acting GLP-1 receptor agonist approved by the FDA for type 2 diabetes (Ozempic), chronic weight management plus CV risk reduction in obesity (Wegovy), and oral type 2 diabetes (Rybelsus). It works by enhancing glucose-dependent insulin secretion, suppressing glucagon, delaying gastric emptying, and reducing appetite through central GLP-1 receptor activation. Per the FDA Wegovy label, titrate every 4 weeks: 0.25 → 0.5 → 1.0 → 1.7 → 2.4 mg weekly. Ozempic (T2DM) maxes at 2.0 mg weekly. Carries a boxed warning for medullary thyroid carcinoma (MTC) and MEN 2. HbA1c, fasting glucose, insulin, a full lipid panel, and liver enzymes are the standard biomarkers researchers track, with CRP sometimes added to monitor inflammatory changes.

Tirzepatide (GIP/GLP-1 dual receptor agonist — Mounjaro, Zepbound)

Tirzepatide is a dual GIP + GLP-1 receptor co-agonist FDA-approved as Mounjaro (type 2 diabetes, 2022) and Zepbound (chronic weight management, 2023; moderate-to-severe obstructive sleep apnea with obesity, 2024). Weekly SubQ dosing titrates 2.5 → 5 → 7.5 → 10 → 12.5 → 15 mg, with 4-week intervals between increases per FDA label. In SURPASS-2 it outperformed semaglutide 1 mg for A1C and weight; SURMOUNT-1 showed up to ~20.9% mean body-weight reduction at 15 mg over 72 weeks. Carries a BOXED WARNING for thyroid C-cell tumors — contraindicated with personal/family history of MTC or MEN 2. Common AEs are GI (nausea, vomiting, diarrhea); serious risks include pancreatitis, gallbladder disease, hypoglycemia when combined with insulin or sulfonylureas, AKI from volume depletion, and diabetic retinopathy complications. HbA1c, fasting glucose, insulin, lipid panel, CRP, and body composition are the standard biomarkers researchers track.

Retatrutide (LY3437943 — GLP-1/GIP/Glucagon triple agonist)

Retatrutide (LY3437943) is Eli Lilly's investigational triple-agonist peptide activating GLP-1, GIP, and glucagon receptors in parallel, and it remains research-only — it is NOT FDA-approved as of April 2026. The glucagon-receptor arm is what distinguishes it from tirzepatide: glucagon agonism drives thermogenesis, hepatic fat mobilization, and energy expenditure on top of the appetite-suppression and insulin-sensitizing effects of GLP-1/GIP. Published Phase 2 data showed approximately 24% mean body weight loss at 48 weeks on 12 mg weekly (Jastreboff, NEJM 2023), with parallel Phase 2 programs in T2D (Rosenstock, Lancet 2023) and MASLD (Sanyal, Nat Med 2024). The Phase 3 TRIUMPH program is ongoing with anticipated NDA filing in 2026. Phase 3 trials titrate from 2 mg to 12 mg weekly subcutaneously; the compound has a half-life of roughly 6 days, supporting once-weekly dosing. Researchers monitor HbA1c, fasting glucose, insulin, full lipid panel, liver enzymes (ALT/AST), body composition, and especially heart rate — a consistent ~7 bpm elevation is a class effect that warrants monitoring.

Mitochondrial Open reading frame of the Twelve S rRNA type-c

MOTS-c is a 16 amino acid mitochondrial-derived peptide (sequence MRWQEMGYIFYPRKLR) encoded within the mitochondrial 12S rRNA — reported by Lee, Cohen, and colleagues at USC in 2015. Preclinical research focuses on AMPK activation in skeletal muscle, increased glucose uptake, and fatty acid oxidation. Human clinical data are limited to a single Phase 1a/1b study of the modified analog CB4211 (CohBar), which reported acceptable tolerability but mixed exploratory readouts; CohBar divested from the program and wound down in 2023. Grey-market protocols commonly use ~10mg subcutaneously 2–3 times per week in 4–8 week cycles, but this dosing is not clinically validated. Fasting glucose, insulin, HbA1c, lactate, and CRP are the biomarkers typically tracked.

Synthetic ERRα/β/γ Agonist (Exercise Mimetic)

SLU-PP-332 is the prototype pan-ERR agonist from the Burris lab at Saint Louis University — a non-peptide small molecule studied preclinically as an “exercise mimetic.” In mice it activates ERRα/β/γ (with a modest ERRα preference), increases type IIa oxidative muscle fibers, raises skeletal-muscle fatty-acid oxidation, and improves treadmill endurance without training. Critically, it lacks oral bioavailability and was dosed by intraperitoneal injection in every in-vivo study — the limitation that motivated its orally active successor, SLU-PP-915. There is no validated human dose and no human safety data, yet it is sold as a grey-market research chemical and has been flagged in anti-doping research. Disclosed Labs tracks hepatic enzymes and metabolic markers as the relevant response labs.

Orally Bioavailable Pan-ERR Agonist

SLU-PP-915 is the second-generation successor to SLU-PP-332 and is described as the first orally bioavailable pan-ERR agonist. It activates ERRα/β/γ with roughly balanced potency (~400 nM at each isoform); a medicinal-chemistry redesign swapped earlier phenol/aniline groups for a boronic-acid moiety on a thiophene scaffold, improving metabolic stability and oral exposure while preserving activity. In mice, oral SLU-PP-915 matches intraperitoneal SLU-PP-332’s gains in running distance and duration after adjusting for exposure. There is no validated human dose and no human safety data, yet it is already sold by grey-market research-chemical vendors and has been flagged in anti-doping research for doping potential. Disclosed Labs tracks hepatic enzymes and metabolic markers as the relevant response labs.

PPARδ Agonist (Synthetic Metabolic Modulator)

GW-0742 is a synthetic small-molecule PPARδ agonist (~1000-fold selective, EC50 = 1.1 nM) from GlaxoSmithKline’s research series, structurally related to GW501516. It activates PPARδ, altering transcription of genes governing fatty-acid oxidation, glucose utilization, and inflammatory signaling. Preclinical rodent studies explored pulmonary hypertension, gut ischemia/reperfusion injury, hepatic steatosis, and lung inflammation; however, mouse studies also revealed hepatomegaly, peroxisome proliferation, and skeletal myopathy driven by off-target PPARα cross-activation. No human efficacy or safety trials exist beyond a single-dose bioanalytical study for anti-doping detection. GW-0742 remains preclinical-stage only and is prohibited at all times by WADA as a metabolic modulator (PPARδ agonist class ban).

Thyroid Hormone Metabolite (Mitochondrial Fat-Oxidation Modulator)

3,5-Diiodo-L-thyronine (3,5-T2) is an endogenous thyroid hormone metabolite and non-peptide small molecule (C₁₅H₁₃I₂NO₄, MW 525.08) formed by deiodination of T3/T4. Unlike classical thyroid hormones, 3,5-T2 acts largely independently of nuclear thyroid hormone receptors, instead binding directly to mitochondrial cytochrome-c oxidase subunit Va to abolish ATP’s allosteric inhibition of respiration and rapidly increase oxygen consumption and fatty-acid oxidation. Preclinical rodent studies show reduced adiposity, increased resting metabolic rate, and AMPK pathway activation. The only human data are a single 2-person case report (~5 µg/kg oral for 28 days) reporting ~15% RMR increase and ~4 kg weight loss with no observed adverse effects; no validated human dose or approved indication exists. Sold gray-market as “research use only” with unverified purity.

Thyroid Hormone Receptor Beta (TRβ) Agonist (Lipid-Lowering Thyromimetic)

Sobetirome (GC-1, QRX-431) is a synthetic thyroid hormone analog engineered to activate thyroid hormone receptor beta (TRβ) with reduced affinity for TRα, yielding tissue-selective thyromimetic activity. In hypothyroid mice, it lowered plasma triglycerides and cholesterol comparably to T3 without raising heart rate, consistent with TRβ-selective action. Company-reported Phase 1 trials in healthy volunteers (10–450 mcg doses) showed LDL-C reductions up to 41% with no significant heart-rate or TSH change; these results were never peer-reviewed and development for dyslipidemia was discontinued. Planned human trials in adrenoleukodystrophy were withdrawn before enrolling any participants. Preclinical studies in mouse models of X-ALD and experimental autoimmune encephalomyelitis showed reductions in very-long-chain fatty acids and disease severity, respectively. No FDA/EMA approval exists; sobetirome is sold as a research chemical with no validated human dose.

TBK1/IKKε Kinase Inhibitor (Anti-inflammatory Small Molecule)

Amlexanox is a non-peptide small-molecule TBK1/IKKε kinase inhibitor (CAS 68302-57-8) originally approved as a topical treatment for canker sores (FDA 1996, discontinued) and in Japan for allergic conditions. Preclinical research identified it as an inhibitor of inflammatory kinases implicated in obesity-linked insulin resistance; in diet-induced obese mice it increased energy expenditure, produced weight loss, improved insulin sensitivity, and reduced hepatic steatosis. One small proof-of-concept trial (42 obese patients with type 2 diabetes and NAFLD) showed statistically significant HbA1c and fructosamine reductions versus placebo, with a responder subgroup demonstrating improved insulin sensitivity and reduced hepatic fat. Amlexanox is NOT approved for any metabolic or obesity indication and is sold by research-chemical vendors labeled not for human consumption. No validated human dose exists for metabolic use.

Nonsteroidal Selective Androgen Receptor Modulator (SARM)

Ligandrol (LGD-4033) is a nonsteroidal selective androgen receptor modulator (SARM) that binds the androgen receptor with high affinity (Ki ≈ 1 nM) and drives muscle- and bone-selective anabolic activity in preclinical models. A Phase 1 trial in 76 healthy men (0.1–1.0 mg/day for 21 days) showed dose-dependent lean-mass increases and dose-dependent suppression of testosterone, SHBG, HDL cholesterol, and triglycerides, which normalized after discontinuation. A Phase 2 trial in 108 hip-fracture-recovery patients (0.5–2.0 mg/day for 12 weeks) reported placebo-adjusted lean-mass gains of 4.8–9.1%. Published case reports document severe cholestatic liver injury and marked hormone suppression in individuals using unsupervised gray-market product at doses far above trial levels. LGD-4033 has no FDA-approved medical use and is prohibited at all times by WADA under S1.2 (SARMs class).

Nonsteroidal Selective Androgen Receptor Modulator (SARM)

LGD-3303 is a nonsteroidal selective androgen receptor modulator (SARM) of the pyrrolo[3,2-f]quinolinone chemotype. In castrated rat models, it demonstrated potent anabolic activity on levator ani muscle while acting only as a partial agonist in androgenic tissues (ventral prostate, preputial gland), never raising prostate weight above intact-animal levels despite rising plasma concentrations. Tissue selectivity persisted across oral and continuous-infusion dosing routes and was independent of local tissue drug concentrations — suggesting receptor-level rather than pharmacokinetic mechanisms. No human data exist; LGD-3303 has never been evaluated in clinical trials or approved for any indication. It is prohibited under WADA’s S1.2 category covering SARMs as a class.

Nonsteroidal Selective Androgen Receptor Modulator (SARM)

ACP-105 is a nonsteroidal selective androgen receptor modulator (SARM) discovered via high-throughput receptor selection and amplification screening. Preclinical studies in castrated male rats demonstrated tissue-selective partial AR agonism, suppression of the LH surge, and anabolic effects on levator ani muscle after oral dosing. Additional rodent research showed preserved sensorimotor performance after radiation exposure in female mice and reduced anxiety-like behavior in gonadectomized male Alzheimer’s-model mice; combined with an ER-β agonist, it improved cognition and reduced brain amyloid-β levels. No human clinical trials have been conducted, and no validated human dose exists. ACP-105 is prohibited under WADA S1.2 as a SARM and is sold in the gray market as a “research chemical.”

Selective Androgen Receptor Modulator (Partial Agonist)

AC-262536 is a non-peptide nonsteroidal selective androgen receptor modulator (SARM) characterized by partial agonist activity at the androgen receptor. In a 2008 rat study, it demonstrated tissue-selective effects—stimulating levator ani muscle growth and suppressing luteinizing hormone while producing only weak androgenic effects on prostate and seminal vesicle weight compared to testosterone. The compound has never entered human trials and remains unapproved by any regulatory authority. It is sold as a research chemical by online vendors and catalogued as an analytical reference standard by laboratory suppliers. SARMs as a class are prohibited at all times under WADA’s S1.2 category (Other Anabolic Agents).

Selective β3-Adrenergic Receptor Agonist (FDA-Approved Pharmaceutical)

Mirabegron is a non-peptide selective β3-adrenergic receptor agonist FDA-approved for overactive bladder (25–50 mg/day oral). It relaxes detrusor smooth muscle during bladder filling without affecting voiding contractions. β3-AR is also expressed on brown/beige adipose tissue, prompting investigational metabolic research at a supratherapeutic 100 mg/day dose (off-label, not FDA-approved). Despite pharmaceutical approval, mirabegron is sold as unregulated ‘research use only’ powder by reagent vendors, labeled not for human consumption. FDA labeling warns of blood-pressure increases; not recommended in severe uncontrolled hypertension. Pharmacologically distinct from WADA-prohibited β2-agonists, though doping status unconfirmed against primary WADA text.

Nonsteroidal Selective Androgen Receptor Modulator (SARM)

GSK-2881078 is a nonsteroidal selective androgen receptor modulator (SARM) — an indole-5-carbonitrile small molecule designed to bind the androgen receptor and produce tissue-selective anabolic effects in skeletal muscle while minimizing activity in prostate and other androgen-sensitive tissues. Developed by GlaxoSmithKline, it has completed Phase I safety/pharmacokinetic studies in healthy adults and a Phase IIa randomized controlled trial in COPD patients with muscle weakness, demonstrating dose-dependent lean body mass gains alongside reversible HDL-cholesterol reductions and transient liver enzyme elevations. Never approved for any indication and not in active clinical development. SARMs as a class are prohibited in sport under WADA S1.2 (Other Anabolic Agents). Sold in the gray/research-chemical market without human-use labeling.

PPARδ Agonist (Endurance Exercise Mimetic)

Cardarine (GW-501516) is a PPARδ agonist — a non-peptide small molecule often mis-sold as a “SARM,” which it is not. In muscle it drives PGC-1-dependent fatty-acid oxidation and, with training, increased endurance in mice, giving it an “exercise mimetic” reputation. GSK ran human lipid trials (2.5–10 mg/day) that improved cholesterol, but discontinued development around 2007 after a rodent carcinogenicity study reported tumors across multiple organs; a 2019 mouse study likewise showed accelerated colorectal cancer. A human case report documents severe rhabdomyolysis and liver injury from self-use. It is WADA-prohibited at all times and unregulated on the gray market.

REV-ERB Agonist (Circadian/Metabolic Modulator)

SR-9011 is a REV-ERBα/β agonist — a non-peptide small molecule that enhances the clock receptor’s transcriptional repression, altering core clock and metabolic genes. In diet-induced obese mice it increased energy expenditure and reduced fat mass, but it has never been tested in humans: no trials, no dose, no pharmacokinetics, no safety data. It is WADA-prohibited at all times (named explicitly under the Rev-erbα agonists), and gray-market powder is unregulated. Note the widespread naming error — “Stenabolic” is the analog SR9009, not SR-9011 — which can cause the wrong compound to be sold or identified.

Acadesine (AMPK Activator)

AICAR (acadesine) is an AMP-mimetic that activates AMPK, the cell’s energy sensor — a non-peptide nucleoside, not a hormone. In sedentary mice, four weeks of AICAR raised treadmill endurance ~44%, the source of its “exercise in a pill” marketing. In humans it was tested only as acadesine by IV infusion: the large RED-CABG cardioprotection trial was stopped for futility, and a leukemia Phase I/II study set an IV dose. No trial ever studied it for exercise, fat loss, or longevity, and no validated oral/injected human dose exists. It is WADA-prohibited at all times.

Mitochondrial Uncoupler (Protonophore)

BAM15 is a mitochondrial uncoupler — a non-peptide small molecule that makes the inner mitochondrial membrane leak protons, burning more fuel as heat instead of storing it as ATP. Unlike the notorious uncoupler DNP it does not depolarize the plasma membrane at working doses and is less cytotoxic than FCCP in cells. In obese mice it cut fat mass and improved insulin sensitivity without reducing food intake, and it shows benefit in mouse diabetes and kidney-injury models. But it has never been tested in humans — no dose, no safety data — and uncouplers as a class carry a real hyperthermia risk. It is WADA-prohibited and has appeared as an undisclosed supplement adulterant.

Mildronate (Carnitine-Synthesis Inhibitor)

Meldonium (Mildronate) shifts cellular energy metabolism away from fatty-acid oxidation toward glucose by blocking L-carnitine synthesis — a non-peptide small molecule marketed as anti-ischemic and “anti-fatigue.” It is a registered cardiovascular drug in Latvia, Russia and other ex-Soviet states (500 mg twice daily), but it is not FDA- or EMA-approved and has no pivotal Western efficacy trial. It became famous when WADA banned it in January 2016; it stays detectable in urine for weeks to months. Rodent studies show reduced infarct size, but Western human evidence is limited, and gray-market products are unregulated.

Evrenzo (HIF-PH Inhibitor / EPO Booster)

Roxadustat (Evrenzo, FG-4592) is an oral HIF-prolyl-hydroxylase inhibitor that tricks the body into a hypoxia response — stabilizing HIF to raise endogenous erythropoietin and hemoglobin. It is a genuinely approved anemia drug for chronic kidney disease in China, Japan and the EU, backed by large trials, but the US FDA voted against approval in 2021 citing thrombosis, seizures, infections and higher mortality. That same EPO-boosting effect makes it an oral doping agent: it is WADA-prohibited at all times under S2, and it is diverted to endurance athletes and bodybuilders outside legitimate pharmacy channels, where purity is unverified and the documented safety signals apply.

Anti-Obesity Drug 9604

AOD-9604 is a 16-amino-acid synthetic peptide corresponding to the C-terminal fragment of human growth hormone (residues 177-191) with an additional N-terminal tyrosine. Developed by Metabolic Pharmaceuticals (Australia) to isolate a purported 'lipolytic' activity of GH without GH-receptor-mediated growth or diabetogenic effects. AOD-9604 is NOT FDA-approved for any indication; controlled human trials for obesity did not demonstrate clinically meaningful weight loss, and obesity development was terminated in 2007.

5-Amino-1-methylquinolinium

5-Amino-1MQ is a small heterocyclic molecule (not a peptide) that acts as a selective, membrane-permeable inhibitor of nicotinamide N-methyltransferase (NNMT). It is under preclinical investigation for obesity and non-alcoholic fatty liver disease. It is not FDA-approved and has not completed human clinical trials; it is commonly tracked alongside peptides because grey-market vendors sell it for metabolic protocols.

Victoza

Liraglutide is an FDA-approved GLP-1 receptor agonist marketed as Victoza (type 2 diabetes, approved 2010) and Saxenda (chronic weight management, approved 2014). It was the first GLP-1 analog approved for obesity and carries an FDA boxed warning for the risk of thyroid C-cell tumors. Pediatric indications include type 2 diabetes in patients ≥10 years (Victoza) and obesity in patients ≥12 years with BMI ≥95th percentile (Saxenda).

Nicotinamide Adenine Dinucleotide

NAD+ (nicotinamide adenine dinucleotide) is a coenzyme present in all living cells, not a peptide. It is classified here alongside peptides for user convenience in the anti-aging / metabolic category. NAD+ plays a central role in cellular energy metabolism and redox reactions and is studied for its involvement in mitochondrial function, DNA-damage signaling via sirtuins and PARPs, and age-associated metabolic decline. IV NAD+ is not FDA-approved for any clinical indication; it is administered off-label through compounding pharmacies and functional-medicine clinics with limited rigorous outcome data.

FOXO4-D-Retro-Inverso

FOXO4-DRI is a D-retro-inverso peptide designed to disrupt the FOXO4-p53 interaction in senescent cells. It is studied as a senolytic agent that selectively induces apoptosis in senescent cells while sparing normal cells.

Pancragen

A short synthetic peptide bioregulator (Lys-Glu-Asp-Trp) from the Khavinson family, marketed for pancreatic/metabolic support. Evidence is largely Russian-language and preclinical.

IBI362

Mazdutide is a dual GLP-1 / glucagon receptor agonist licensed from Eli Lilly to Innovent Biologics for Greater China. Approved by China's NMPA in June 2025 for chronic weight management and in September 2025 for glycemic control in type 2 diabetes; NOT FDA-approved in the US.

BI 456906

Survodutide is a dual GLP-1 / glucagon receptor agonist co-developed by Boehringer Ingelheim and Zealand Pharma. NOT FDA-approved; received FDA Breakthrough Therapy Designation in 2024 for non-cirrhotic MASH with moderate/advanced fibrosis. Phase 3 ongoing (SYNCHRONIZE in obesity/T2DM; LIVERAGE and LIVERAGE-Cirrhosis in MASH).

LY3502970

Orforglipron (brand name Foundayo) is Eli Lilly's oral non-peptide small-molecule GLP-1 receptor agonist. Unlike oral semaglutide (Rybelsus), it does not require the SNAC absorption enhancer or fasting/water restrictions — it can be taken any time of day. Not a peptide.

FTPP

Adipotide (FTPP) is a chimeric peptidomimetic developed in the Arap/Pasqualini lab (originally at MD Anderson) that couples a 9-residue homing motif (CKGGRAKDC) — isolated by in vivo phage display as a ligand for prohibitin on white-adipose-tissue vasculature — to the D-amino-acid pro-apoptotic domain D(KLAKLAK)2. It is an experimental research compound, NOT FDA-approved for any indication. A clinical-development program in prostate-cancer-associated obesity reached early-phase testing and was ultimately discontinued.

cagrisema

CagriSema is Novo Nordisk's investigational once-weekly fixed-dose co-formulation of cagrilintide 2.4 mg (long-acting amylin analog) with semaglutide 2.4 mg (GLP-1 receptor agonist) for chronic weight management. Unlike the other grey-market blends, it has a proper Phase 3 clinical program. Novo Nordisk filed an FDA NDA in December 2025; as of April 2026 it is under FDA review and not yet approved.