Compounds

Dual GLP-1/GIP receptor agonist; GIP agonism sensitizes adipocytes and augments incretin effect beyond GLP-1 alone

Increases intracellular phosphocreatine, enhancing ATP resynthesis during high-intensity activity

Triple GLP-1/GIP/glucagon receptor agonist; adds hepatic fat mobilization and increased energy expenditure to GLP-1/GIP incretin effects

GLP-1 receptor agonist: delays gastric emptying, suppresses appetite via hypothalamic signaling, stimulates glucose-dependent insulin secretion

Dual GLP-1/glucagon receptor agonist; adds hepatic fat mobilization and increased energy expenditure to GLP-1 satiety effects

Weak DAT inhibition raises synaptic dopamine; activates orexin/hypocretin neurons; increases histamine and NE

Binds GH receptor on hepatocytes → IGF-1 production; directly stimulates lipolysis in adipose; promotes nitrogen retention and tissue repair via IGF-1/mTOR/PI3K

L-citrulline converts to arginine → NO via NOS → vasodilation; malate fuels Krebs cycle ATP synthesis and accelerates ammonia clearance

EPA and DHA compete with arachidonic acid for COX/LOX enzymes, shifting eicosanoid production toward anti-inflammatory SPMs; DHA incorporates into cell membranes affecting fluidity and receptor function

Withanolides modulate HPA axis, reduce cortisol, potentiate GABA-A signaling, and inhibit NF-kB inflammation

Precursor to calcitriol; binds vitamin D receptor (nuclear receptor) in all cell types; regulates calcium homeostasis, immunity, muscle function, and expression of 200+ genes

Rate-limiting carnosine precursor; muscle carnosine buffers intramuscular H+ ions during high-intensity glycolytic activity

Porcine brain peptide mixture with neurotrophic factor-like activity; activates BDNF/NGF signaling pathways; promotes neuroplasticity, neuronal survival, and synaptogenesis

NMDA receptor voltage-dependent block, calcium channel regulation, HPA axis modulation, ATP synthesis cofactor, melatonin precursor support

GABA-A positive allosteric modulation, NMDA/AMPA antagonism, alpha-wave induction, catecholamine modulation

Electron shuttle in mitochondrial ETC (complex I-III); lipophilic antioxidant protecting cell membranes; regenerates vitamins C and E; replenishes statin-depleted CoQ10

AMPK activator; inhibits complex I of mitochondrial respiratory chain (similar to metformin); reduces hepatic gluconeogenesis; activates GLUT4 translocation; reduces intestinal glucose absorption

Oral DHT-derived anabolic; binds AR in muscle/bone without aromatization; high anabolic-to-androgenic ratio; FDA-approved for wasting conditions

Binds androgen receptor as full agonist; activates muscle, bone, erythropoiesis, and CNS AR programs; aromatizes to estradiol via CYP19A1

MC3R and MC4R agonist in the hypothalamus; activates central arousal pathways independent of vascular mechanisms

Stabilized GHRH analog binding pituitary GHRH receptors; stimulates GH/IGF-1 production, reducing visceral fat via lipolysis

Orally bioavailable NAD+ precursors; NR converts to NMN then NAD+; NMN converts directly to NAD+; elevates NAD+ for sirtuin activation, PARP DNA repair, and mitochondrial biogenesis

Alternative mitochondrial electron carrier in complex I-IV chain; improves oxidative phosphorylation; MAO inhibitor; antioxidant at low doses; hormetic dose-response

Reduces SHBG and cortisol to free more testosterone; possible direct LH/FSH stimulation; eurycomanone (active quassinoid) drives most studied effects

Rapidly absorbed choline donor; crosses BBB and upregulates acetylcholine synthesis in cortical neurons

Phenyl-substituted piracetam; enhances dopamine and norepinephrine activity; increases NMDA/AMPA receptor density; stimulant and cognitive-enhancing properties

Dipeptide nootropic; metabolizes to cycloprolylglycine; upregulates NGF and BDNF; modulates AMPA and NMDA receptors; anxiolytic-nootropic profile

Mitochondria-to-nucleus retrograde signaling via AMPK and AICAR; improves insulin sensitivity, metabolic flexibility, and exercise capacity

High-affinity selective AR agonist; near-complete receptor occupancy at low doses produces significant muscle anabolism with moderate bone activation

Selectively partitions to inner mitochondrial membrane via cardiolipin binding; stabilizes cristae, reduces ROS, and restores ATP production efficiency

Highly anabolic 19-nor androgen; partial AR agonist with progestogenic activity; minimal aromatization; high anabolic-to-androgenic ratio via tissue-specific AR binding

Selective AR agonist with tissue selectivity for muscle and bone over prostate and sebaceous glands; anabolic without full androgenic activity

Stimulates hippocampal neurogenesis via unknown mechanism; increases stem cell proliferation and differentiation; demonstrated hippocampal volume increase on MRI in Phase I

Hericenones and erinacines stimulate NGF and BDNF synthesis, promoting neuroplasticity, myelination, and neuroprotection

MAO-A/B inhibitor; promotes dopaminergic neuron proliferation and differentiation; neuroprotective in MPTP Parkinson's models; increases BDNF and GDNF expression (preclinical only)

Ghrelin receptor (GHSR-1a) agonist; stimulates pulsatile GH release from anterior pituitary; elevates IGF-1 without suppressing endogenous GH axis

Potentiates HGF/c-Met receptor signaling, dramatically enhancing synaptogenesis, dendritic spine density, and hippocampal LTP

Activates collagen synthesis and wound healing genes; broad anti-inflammatory and antioxidant effects via Nrf2 and NF-κB pathways

GHRH receptor agonist on pituitary somatotrophs; stimulates pulsatile GH release and downstream IGF-1 production

DHT-derived anabolic; binds AR without aromatization; no estrogenic activity; anabolic with low androgenicity; notable immune-modulatory effects

Upregulates VEGF and GH receptors; activates FAK-paxillin tendon repair pathway; modulates NO-cGMP system

Sequesters G-actin, promotes cell migration and angiogenesis via eNOS upregulation and anti-inflammatory cytokine modulation

PPARδ/β agonist; transcriptionally activates fatty acid oxidation genes (CPT1, ABCA1) in skeletal muscle; dramatically increases mitochondrial biogenesis and fat burning

Ghrelin mimetic at GHS-R1a receptors; amplifies GH pulse without raising cortisol or prolactin

Potent selective AR agonist; high muscle:prostate anabolic ratio; also activates neuroprotective AR pathways in brain

Partial AR agonist with structural similarity to DHT; upregulates Follistatin to inhibit myostatin, potentially removing the ceiling on muscle hypertrophy

DHT-derived androgen with intrinsic anti-estrogenic activity; no aromatization; competes with estrogen at receptor level; moderate AR agonist with hardening/drying cosmetic effects

Beta-3 adrenergic receptor agonism increases lipolysis in adipocytes; mimics GH lipolytic domain without activating somatotropic axis; may inhibit lipogenesis

Competitive inhibitor of alpha-glucosidase and pancreatic alpha-amylase in small intestine; delays breakdown of complex carbs to glucose; reduces postprandial glucose spike by 30-50%; modifies gut microbiome

Acetyl donor for acetylcholine synthesis; mitochondrial membrane repair; NGF signaling; carnitine palmitoyltransferase support for beta-oxidation

S-allylcysteine inhibits ACE and activates eNOS → vasodilation and BP reduction; polysulfides activate TRPA1/H2S signaling; organosulfur compounds reduce oxidative stress and inflammation

Mitochondrial PDH/KGDH cofactor; recycles vitamins C, E, Q10, and glutathione; activates AMPK; Nrf2 induction; inhibits NF-kB; chelates heavy metals

Reversible competitive inhibitor of aromatase (CYP19A1); blocks conversion of testosterone → estradiol; reduces circulating estrogen by 70-80% in men

Full agonist at androgen receptor in muscle/bone; partial agonist at AR in prostate and eye; promotes nitrogen retention, protein synthesis; fat oxidation via beta-AR upregulation

Bacosides inhibit acetylcholinesterase; induce BDNF and dendrite branching; antioxidant via SOD/CAT induction; serotonin 5-HT3 antagonism; cortisol reduction

Inhibits SHBG production in liver; activates CYP27B1 for vitamin D conversion; modulates sex steroid binding; supports bone calcium retention

AKBA directly inhibits 5-lipoxygenase (5-LOX), preventing leukotriene B4/C4/D4 synthesis; reduces inflammatory infiltrate without COX inhibition; MMP inhibition in cartilage

Upregulates AADC (dopa decarboxylase) gene expression; increases dopamine and serotonin synthesis capacity; non-releasing, non-reuptake mechanism; heat shock protein induction

GHRH receptor agonist with albumin-binding DAC moiety extending half-life to ~8 days; creates sustained (non-pulsatile) GH and IGF-1 elevation

Beta-2 adrenergic receptor agonist; increases cAMP via Gs → activates PKA → phosphorylates HSL (hormone-sensitive lipase) → lipolysis; thermogenic via uncoupled mitochondrial respiration

Cordycepin (adenosine analog) modulates adenosine receptors; adenosine 5'-monophosphate increases ATP availability; AMPK activation drives mitochondrial biogenesis

IKKβ inhibition → NF-kB nuclear translocation block; COX-2 and 5-LOX inhibition; Nrf2 activation; AMPK activation; reduces TNF-alpha, IL-1beta, IL-6

Adrenal steroid precursor converted to testosterone/estradiol via 3β-HSD and 17β-HSD; also a neurosteroid modulating GABA-A, NMDA, and sigma-1 receptors

Modulates sleep architecture toward slow-wave (delta) sleep; reduces HPA axis cortisol reactivity; modulates GABA, serotonin, and glutamate systems without direct receptor binding — acts as a neuromodulatory peptide

Shifts estrogen metabolism toward 2-hydroxylation (2-OHE1) and away from 16α-hydroxylation (16α-OHE1); modulates estrogen receptor signaling without blocking aromatase

Dual Type I/II 5-alpha reductase inhibitor; reduces DHT by ~90%

Blocks ER-alpha in hypothalamus and pituitary, reducing estrogen negative feedback; pulsatile GnRH/LH/FSH increase drives testicular testosterone production and spermatogenesis

Indirect sympathomimetic (releases NE/E from presynaptic terminals); direct alpha and beta adrenergic agonism; mild MAO inhibition; increases thermogenesis, lipolysis, bronchodilation

Telomerase activation via epigenetic (DNA methylation) changes; pineal gland stimulation increasing melatonin; antioxidant enzyme induction; p53/Bcl-2 apoptosis modulation

Upregulates mGluR2/3 (Group II metabotropic glutamate receptors); GABA-B receptor agonism (anxiolytic); choline uptake facilitation; reverses mGluR downregulation from stimulant use

Selective Type II 5-alpha reductase inhibitor; reduces DHT by ~70% to prevent follicle miniaturization

Bcl-2/Bcl-xL/Bcl-W inhibitor (senolytic) — selectively kills senescent cells dependent on these anti-apoptotic proteins; Nrf2 activation; SIRT1 activation; mTOR inhibition

Potent ghrelin mimetic at GHS-R1a; amplifies GH pulse via calcium-dependent exocytosis; also activates ACTH/cortisol and prolactin pathways (less selective than ipamorelin)

Ghrelin receptor (GHSR-1a) agonist in pituitary and hypothalamus; amplifies GHRH-driven GH pulse; stimulates appetite via hypothalamic NPY/AgRP neurons

PAF (platelet-activating factor) antagonism; inhibits phosphodiesterase → increased cGMP; free radical scavenging (flavonoids); inhibits EAA receptor-mediated excitotoxicity (bilobalide)

Inhibitory glycine receptor agonist; NMDA co-agonist; collagen precursor; glutathione precursor via GCL; reduces core body temperature

GnRH receptor agonist on pituitary gonadotrophs; pulsatile administration stimulates LH/FSH release, preserving spermatogenesis and intratesticular testosterone during exogenous T administration

GHS-R1a agonism causing pulsatile GH release with downstream IGF-1 increases

LH/hCG receptor agonist on Leydig cells; maintains intratesticular testosterone and spermatogenesis during exogenous testosterone administration

Reversible acetylcholinesterase inhibitor (IC50 ~74nM); NMDA antagonist; upregulates NGF; protects against beta-amyloid neurotoxicity

IGF1R activation with prolonged exposure due to reduced binding to IGF-binding proteins

Anti-inflammatory; reduces TNF-alpha and interleukins via NFkB inhibition

KISS1R (GPR54) agonist on hypothalamic GnRH neurons; triggers GnRH pulsatile release → LH/FSH secretion. The most upstream activator of the reproductive axis.

Substrate for eNOS, iNOS, nNOS → NO synthesis → cGMP → vasodilation; stimulates pituitary GH release; precursor for ornithine/polyamine synthesis; urea cycle component

Primary fuel for enterocytes and lymphocytes; precursor for glutathione; maintains tight junction integrity; nitrogen transporter

Catecholamine synthesis precursor (DOPA decarboxylase pathway); thyroid hormone precursor; competes for large neutral amino acid transporter at BBB

TR-alpha and TR-beta nuclear receptor agonist → increased mitochondrial uncoupling proteins → thermogenesis; upregulates beta-adrenergic receptors; increases Na+/K+-ATPase expression

Macamides inhibit fatty acid amide hydrolase (FAAH), elevating endocannabinoids; glucosinolates converted to isothiocyanates; monoamine modulation

Uniquely elevates cerebrospinal fluid and synaptic magnesium; increases synaptic density via NMDA receptor modulation; activates PKA/PKC signaling for synaptic plasticity

Exogenous IGF-1 replacement activating IGF1R/PI3K-AKT-MAPK signaling to restore growth and anabolic signaling

Non-selective melanocortin receptor agonist (MC1-4R); MC1R drives melanogenesis; MC3R/MC4R drive libido, appetite suppression, and pro-erectile pathways in hypothalamus

AMPK activation via complex I inhibition; mTOR inhibition downstream; NF-kB suppression; GLP-1 secretion enhancement; gut microbiome modification (increases Akkermansia)

Pre-activated B vitamins; bypass MTHFR variants for methylation support and homocysteine management

Potassium channel opener; vasodilator that increases follicular blood flow and prolongs anagen phase

GHRH receptor agonist; produces discrete, physiological GH pulses (unlike DAC variant which creates sustained elevation). Four amino acid substitutions resist DPP-IV degradation.

Cysteine donor for glutathione synthesis; direct thiol antioxidant; mucolytic via disulfide bond cleavage; modulates glutamate signaling via cystine-glutamate antiporter

AR agonist with lower DHT conversion; progestogen receptor agonism; increases collagen synthesis (II and III); stimulates EPO; IGF-1 upregulation; glucocorticoid antagonism

Direct fibrin degradation (cleaves Bβ chain); activates tissue plasminogen activator (tPA) and urokinase; degrades PAI-1; reduces blood viscosity and platelet aggregation

BPC-157 structural replacement; tissue repair via angiogenesis and GH receptor upregulation

Experimental IGF-axis splice-variant signaling intended to influence muscle repair pathways

Ginsenosides activate glucocorticoid receptors, modulate NO production, inhibit neuroinflammation, enhance ACh signaling, support HPG axis via LH stimulation

Structural membrane phospholipid; activates PKC (cell signaling); inhibits cortisol release via HPA axis; supports acetylcholine and dopamine release

REM sleep bioregulator; stimulates pinealocytes for natural melatonin production

BDNF induction via TrkB receptor; hippocampal neurogenesis promotion; AChE inhibition; sigma-1 receptor modulation; cAMP/CREB pathway activation

Master steroid precursor (cholesterol → pregnenolone → all steroid hormones); neurosteroid modulating NMDA (positive) and GABA-A (negative) receptors; enhances memory and cognitive flexibility

5-HT2A full agonist in PFC, DMN, and limbic system; increases synaptic density (rapid, AMPA-mediated); Default Mode Network (DMN) disruption; neuroplasticity via BDNF and TRKB

SIRT1 activator (more potent than resveratrol); AMPK activation; superior BBB penetration; NF-kB inhibition; PPARα activation for fat oxidation; BDNF upregulation

Activates eNOS → increases NO bioavailability; potent antioxidant (procyanidins scavenge ROS); inhibits NF-κB; reduces platelet aggregation via COX inhibition

Bcl-2/Bcl-xL inhibitor (senolytic); AMPK activator; SIRT1 activator; zinc ionophore; NF-kB inhibitor; 5-lipoxygenase and COX inhibitor; mast cell stabilizer

FKBP12 binding → mTORC1 inhibition → reduced protein synthesis, increased autophagy, reduced senescence-associated secretory phenotype (SASP), improved lysosomal function

SIRT1 deacetylase activation (caloric restriction mimetic); AMPK activation; NF-kB inhibition; eNOS upregulation; autophagy induction; aromatase inhibition

Inhibits MAO-A/B (mild); modulates stress kinases (JNK, AMPK); upregulates SDF-1/HSP70 stress proteins; increases serotonin, dopamine, norepinephrine availability

Full agonist at AR in muscle and bone; near-complete LH/FSH suppression via hypothalamic/pituitary AR activation; partial agonist in prostate; no aromatization

Rev-Erbα/β nuclear receptor agonist; represses BMAL1/CLOCK circadian transcription; upregulates mitochondrial biogenesis and fatty acid oxidation genes; suppresses gluconeogenesis

Schisandrins modulate NF-kB and Nrf2 pathways; induce CYP3A4/CYP2C19; hepatoprotective via antioxidant induction; HPA axis normalization

Enkephalinase inhibition increases endogenous enkephalins; GABA-A modulation without direct binding; BDNF induction; IL-6/interferon modulation; serotonin normalization

BDNF/CNTF upregulation in hippocampus; D-Asp-HFP sequence binds melanocortin MC4R; modulates dopaminergic and serotonergic systems; anti-inflammatory via IL-6 reduction

GHRH receptor agonist in anterior pituitary somatotrophs; increases cAMP via Gs-coupled receptor; amplifies pulsatile GH release; preserves hypothalamic-pituitary axis

Inhibits EP300 acetyltransferase → Nrf2 and LC3 deacetylation → autophagy induction; eIF5A hypusination for translation of specific proteins; anti-inflammatory via NF-kB suppression

AR agonist with DHT backbone; potent SHBG competitor; displaces testosterone from SHBG increasing free T; C17-alpha alkylated (oral) for oral bioavailability causing hepatotoxicity

Selective PDE5 inhibitor; prevents cGMP degradation in vascular smooth muscle → eNOS-derived NO maintains vasodilation → sustained vasodilation in penile corpus cavernosum, pulmonary vasculature, prostate

Osmoregulation, membrane stabilization, mitochondrial quality control, GABA-A modulation, antioxidant via bile salt conjugation

Binds androgen receptor; drives muscle protein synthesis via mTOR/PI3K/Akt; inhibits glucocorticoid receptors; erythropoietin stimulation; aromatizes to estradiol

Esterified testosterone cleaved by esterases → free testosterone; identical mechanism to other testosterone esters; ester length determines release rate and half-life only

TLR2/9 agonism activates dendritic cells; T-cell differentiation (Th1 skew) via IL-12/IFN-γ; NK cell maturation; upregulates MHC class I expression on tumor cells

Highly potent AR agonist (5x testosterone affinity); direct IGF-1 upregulation; glucocorticoid receptor competition; does not aromatize; progestogenic activity

Selective mitophagy induction via PINK1/Parkin pathway; upregulates mitochondrial biogenesis via PGC-1alpha; reduces IL-6, TNF-alpha, CRP; extends lifespan in C. elegans, rodents

Collagen prolyl and lysyl hydroxylase cofactor; reduces ferric to ferrous iron for absorption; recycles oxidized glutathione and vitamin E; supports catecholamine synthesis

Cofactor for gamma-glutamyl carboxylase; activates MGP (prevents arterial calcification) and osteocalcin (bone mineralization, glucose metabolism)

Cofactor for >300 enzymes; 5α-reductase and aromatase inhibition; androgen receptor signaling; thymulin production for T-cell maturation