Semaglutide GLP-1 Agonists
Moderate Risk GLP-1 receptor agonist with C18 fatty diacid albumin binding (~168h half-life). Activates Gs/cAMP/PKA/CREB signaling; central anorexigenic via ARC NPY/AgRP inhibition.
GLP-1R 4 effects
Tirzepatide GLP-1 Agonists
Moderate Risk Dual GLP-1R/GIPR agonist (GIP-scaffold peptide, 39aa). Biased GLP-1R agonism + balanced GIPR full agonism. ~5-day half-life via C20 fatty diacid albumin binding.
GLP-1R GIPR 3 effects
Retatrutide GLP-1 Agonists
Moderate Risk Triple GLP-1R/GIPR/GCGR agonist (26aa). GCGR arm adds hepatic CPT1-mediated fat oxidation + energy expenditure. ~6-day half-life.
GLP-1R GIPR 3 effects
Gastric pentadecapeptide. Acts via eNOS upregulation, VEGFR2/VEGF-mediated angiogenesis, and FAK/paxillin cytoskeletal pathway. No known cognate GPCR identified.
eNOS pathway VEGFR2 2 effects
TB-500 (Thymosin β-4) Repair Peptides
Low Risk Actin-sequestering peptide; LKKETQ domain binds G-actin, releasing it from F-actin pool. Downstream ILK/Akt/NF-κB cascade drives anti-inflammatory, angiogenic, and pro-survival effects.
G-actin ILK 2 effects
GHK-Cu (Copper Tripeptide) Repair Peptides
Low Risk Copper-chelated tripeptide (Gly-His-Lys·Cu²⁺). Copper is essential for activity — free GHK lacks most effects. TGF-β1/SMAD2-3 collagen synthesis + Nrf2/GCLC antioxidant + VEGF/VEGFR2 angiogenesis.
TGF-β1/SMAD2-3 Nrf2/Keap1 3 effects
NAD+ (β-Nicotinamide Adenine Dinucleotide) Longevity
Low Risk Redox coenzyme and SIRT1/SIRT3 substrate. NAD+ depletion drives mitochondrial dysfunction and aging. Repletion activates PGC-1α biogenesis, SOD2 deacetylation, IDH2 activation.
SIRT1/SIRT3 PARP1 2 effects
MK-677 (Ibutamoren) GH Secretagogues
Low Risk Oral GHSR-1a full agonist (non-peptide spiroindoline). ~24h half-life via oral bioavailability. Increases GH pulse amplitude and IGF-1. Does not require injection.
GHSR-1a 3 effects
Ipamorelin GH Secretagogues
Low Risk D-2-Nal² GHRP analog. Most selective GHSR-1a agonist — no cortisol, ACTH, or prolactin elevation at therapeutic doses. Synergizes with GHRH analogs (CJC-1295 No DAC) for 8–12× GH amplification.
GHSR-1a 2 effects
CJC-1295 No DAC (Mod GRF 1-29) GH Secretagogues
Low Risk Stabilized GHRH(1-29) fragment with four-point substitution for DPP-4 resistance. ~30 min half-life, pulsatile GH stimulation. Synergizes with ipamorelin via Gs/cAMP + Gq/IP3 orthogonal pathways.
GHRHr 1 effects
PT-141 (Bremelanotide) Melanocortin Peptides
Moderate Risk Cyclic heptapeptide melanocortin agonist. MC4R/PVN oxytocinergic pathway mediates sexual arousal effects (CNS mechanism vs PDE5 peripheral mechanism). Non-selective — activates MC1R/MC3R as well.
MC1R MC3R 4 effects
Melanotan II Melanocortin Peptides
Moderate Risk Cyclic lactam heptapeptide, Ac-Nle⁴-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH₂. Non-selective melanocortin agonist. MC1R/melanogenesis + MC4R/oxytocinergic arousal + MC3R/area postrema nausea.
MC1R MC3R 3 effects
Thymosin Alpha-1 (Tα1) Immunology
Low Risk N-terminal acetylated 28aa peptide from prothymosin-α. TLR2/4/9 co-agonist → IFN-α/γ + IL-12 + dendritic cell maturation + NK activation. Th1 polarization without Th2 suppression.
TLR2 TLR4 1 effects
KPV (α-MSH 11-13 fragment) Immunology
Low Risk C-terminal tripeptide of α-MSH. MC1R/MC3R selective without MC2R (no cortisol) or MC4R (no appetite) activation. NF-κB inhibition via IκBα stabilization → IL-6/TNF-α suppression.
MC1R MC3R 2 effects
SS-31 (Elamipretide) Longevity
Low Risk Szeto-Schiller tetrapeptide (D-Arg-2',6'-Dmt-Lys-Phe-NH₂). 1000× mitochondrial accumulation via charge gradient. Cardiolipin binding stabilizes respiratory supercomplexes, reduces ROS, restores Complex I.
Cardiolipin No canonical receptor 1 effects
Epitalon (Epithalon) Longevity
Low Risk Ala-Glu-Asp-Gly tetrapeptide. Activates telomerase (TRAP assay 2.4×, Khavinson 2003), upregulates TERT mRNA. Restores pineal AANAT → melatonin in aged animals.
TERT Pineal gland AANAT enzyme 1 effects
Mitochondria-derived 16aa peptide (12S rRNA sORF). AMPK activation via AICAR/folate cycle → GLUT4 nuclear translocation → insulin sensitization. Exercise mimetic in DIO models.
AMPK GLUT4 1 effects
Heptapeptide tuftsin analog (TKPRPGP). Non-GABAergic anxiolytic via tuftsin receptor. Upregulates BDNF via IL-6 immunomodulation. No sedation or dependence potential.
Tuftsin receptor Presynaptic GABA modulation 1 effects
ACTH(4-7)PGP heptapeptide analog. Melanocortin binding without cortisol/ACTH activation (no MC2R). BDNF and VEGF upregulation in CNS; nootropic effects via hippocampal neurogenesis.
Melanocortin receptors BDNF receptor TrkB 1 effects
Posterior pituitary nonapeptide. OTR Gq signaling in hypothalamus/limbic system. HPA dampening via PVN OTR. Requires intranasal delivery for CNS behavioral effects — peripheral OT does not cross BBB.
OTR V1aR 2 effects