BPC-157: Angiogenic & Cytoprotective Properties in In-Vitro Models
Journal of Physiology and Pharmacology
·
Sikiric et al., 2018
BPC-157 (Body Protection Compound-157) is a pentadecapeptide derived from a gastric protein. In-vitro and animal model studies have demonstrated its angiogenic properties, including upregulation of VEGFR2 expression and promotion of endothelial cell migration. Research has also investigated its cytoprotective effects on gastrointestinal tissue at the cellular level, with consistent replication across multiple independent research groups.
Angiogenesis
Cytoprotection
VEGFR2
BPC-157: Tendon Outgrowth, Cell Survival and Musculoskeletal Repair
Journal of Applied Physiology
·
Chang et al., 2011
BPC-157 has been extensively researched for musculoskeletal repair mechanisms. Chang et al. demonstrated that BPC-157 promoted tendon healing through three parallel mechanisms: stimulation of tendon outgrowth, enhanced cell survival under oxidative stress, and accelerated tendon cell migration in scratch assay models. Rodent studies document significantly accelerated healing of Achilles tendon, quadriceps, and rotator cuff injuries, alongside upregulation of EGR1 and VEGF.
Tendon Repair
Cell Migration
EGR1 / VEGF
TB-500: Thymosin Beta-4 Fragment and Actin Dynamics in Cellular Repair Models
Annals of the New York Academy of Sciences
·
Philp et al., 2004
TB-500 is a synthetic peptide fragment of Thymosin Beta-4 corresponding to the actin-binding domain at amino acid positions 17–23. Research confirms this region as the primary G-actin sequestering domain of the parent molecule. In vitro studies demonstrate TB-500's role in promoting cell migration, stimulating angiogenesis through upregulation of VEGF, and reducing inflammatory markers in wound healing models.
Actin Sequestration
VEGF
Wound Healing
Follistatin 344: Myostatin Antagonism and Skeletal Muscle Hypertrophy in Preclinical Models
Proceedings of the National Academy of Sciences
·
Lee & McPherron, 2001
Follistatin is a glycoprotein that functions as a potent antagonist of myostatin (GDF-8), a negative regulator of skeletal muscle mass. Lee and McPherron demonstrated that overexpression of follistatin in mice produced dramatic increases in muscle mass — up to 194% above wild-type — through dual inhibition of myostatin and activin signalling. The 344-amino acid isoform (FST-344) circulates systemically and has been the focus of preclinical research examining muscle fibre hypertrophy, satellite cell activation, and potential applications in muscle-wasting disease models.
Myostatin Inhibition
Muscle Hypertrophy
Activin Antagonism
Thymosin Beta-4: Actin Sequestration and Cellular Motility Research
Annals of the New York Academy of Sciences
·
Goldstein & Kleinman, 2015
Thymosin Beta-4 is a ubiquitous 43-amino acid peptide that plays a critical role in actin polymerisation and cellular motility. Laboratory studies have examined its role as an actin-sequestering peptide, with research focusing on its effects on cell migration, differentiation, and angiogenesis in controlled in-vitro environments.
Actin Dynamics
Cell Migration
Angiogenesis
NAD&sup+;: Therapeutic Potential of NAD-Boosting Molecules in Ageing and Cellular Energy Research
Cell Metabolism
·
Rajman, Chwalek & Sinclair, 2018
Nicotinamide adenine dinucleotide (NAD&sup+;) is an essential coenzyme central to cellular energy metabolism and a key substrate for sirtuin deacylases and poly(ADP-ribose) polymerases (PARPs). A landmark review catalogued in-vivo evidence demonstrating that restoring NAD&sup+; levels reverses multiple hallmarks of biological ageing in preclinical models. Research showed NAD&sup+; depletion associates with mitochondrial dysfunction and impaired DNA repair, while restoration activates sirtuins and promotes mitochondrial biogenesis.
Sirtuins
PARP
Mitochondrial Biogenesis
NAD+ Precursor Supplementation Improves Muscle Insulin Sensitivity in Human Participants
Science
·
Yoshino et al., 2021
The first human RCT demonstrating metabolic benefits of NAD+ precursor supplementation: 25 postmenopausal women with prediabetes received NMN for 10 weeks. NMN significantly increased skeletal muscle NAD+ levels, enhanced insulin sensitivity by hyperinsulinaemic-euglycaemic clamp, and upregulated muscle remodelling and mitochondrial genes. These findings in humans directly support the mechanistic role of NAD+ depletion in insulin resistance.
Human RCT
Insulin Sensitivity
Skeletal Muscle
Oral Glutathione Supplementation Elevates Tissue Stores and Reduces Oxidative Stress in Healthy Adults
European Journal of Nutrition
·
Richie et al., 2015
A six-month randomised, double-blind, placebo-controlled trial in 54 healthy adults showed oral glutathione at 250mg and 1,000mg/day produced dose-dependent blood glutathione increases of up to 35% across erythrocytes, lymphocytes, and plasma. The higher-dose group showed significant reduction in oxidised-to-reduced glutathione ratio — a validated oxidative stress marker — and a measurable decrease in skin melanin index.
Human RCT
Oxidative Stress
Bioavailability
CJC-1295: Growth Hormone Releasing Hormone Analogue Research
Journal of Clinical Endocrinology & Metabolism
·
Teichman et al., 2006
CJC-1295 is a synthetic analogue of Growth Hormone Releasing Hormone (GHRH). Laboratory and controlled research studies have characterised its binding affinity to GHRH receptors and examined its pharmacokinetic profile in model systems, demonstrating sustained elevation of IGF-1 and growth hormone levels over 14 days — a dramatically extended duration compared to native GHRH.
GHRH Receptor
IGF-1
Pharmacokinetics
Ipamorelin: Selective GHS-R Agonist Binding and Receptor Specificity Studies
European Journal of Endocrinology
·
Raun et al., 1998
Ipamorelin is a pentapeptide growth hormone secretagogue and selective agonist of the GHS-R. Research characterised its receptor binding specificity and selectivity profile compared to other GH secretagogues, demonstrating that unlike GHRP-6, Ipamorelin stimulates GH release without significantly elevating cortisol or prolactin — a key selectivity advantage making it valuable in research models requiring isolated GH secretagogue activity.
GHS-R Agonist
Receptor Selectivity
No Cortisol Spike
CJC-1295 + Ipamorelin: Complementary GH Secretagogue Pathways and Pulsatile Release Research
Journal of Clinical Endocrinology & Metabolism
·
Ionescu & Frohman, 2006
CJC-1295 and Ipamorelin represent two mechanistically distinct but complementary GH secretagogue pathways. CJC-1295 binds pituitary GHRH receptors to amplify GH pulse magnitude; Ipamorelin triggers GH release via the ghrelin receptor independently. Simultaneous activation of both pathways produces significantly greater physiologically natural GH output than either compound alone — the rationale underpinning their combination in research protocols.
GHRH Analogue
GHS-R
IGF-1
Tesamorelin: Significant Visceral Fat Reduction in Randomised Human Clinical Trial
New England Journal of Medicine
·
Falutz et al., 2007
A randomised, double-blind, placebo-controlled trial in 412 adults demonstrated tesamorelin produced a 15.2% reduction in visceral adipose tissue vs 5.1% for placebo over 26 weeks. Participants also showed significant improvements in triglyceride levels, waist circumference, and quality-of-life scores. This robust human evidence supported FDA approval of tesamorelin (Egrifta) for excess abdominal fat in HIV-infected adults.
Human RCT
Visceral Fat
FDA Approved
GHRP-6: Cardioprotective Effects and GHS-R Expression in Cardiac Tissue
Regulatory Peptides
·
Granado et al., 2007
GHRP-6 (Growth Hormone Releasing Peptide-6) is a hexapeptide GHS-R agonist. Beyond its growth hormone releasing activity, Granado et al. demonstrated significant cardioprotective properties in rodent models: GHRP-6 reduced myocardial infarct size by up to 30% when administered prior to ischaemia-reperfusion injury, attenuated inflammatory cytokine release in cardiac tissue, and reduced cardiomyocyte apoptosis. The findings identified direct GHS-R expression in cardiac tissue as a potential target for cardioprotective research applications independent of GH axis modulation.
Cardioprotection
GHS-R
Ischaemia-Reperfusion
Tirzepatide: Dual GIP/GLP-1 Agonism and Up to 20.9% Weight Reduction — SURMOUNT-1
New England Journal of Medicine
·
Jastreboff et al., 2022
Tirzepatide is a unimolecular dual agonist targeting both GIP and GLP-1 receptors. The SURMOUNT-1 Phase 3 trial demonstrated mean weight reductions of up to 20.9% from baseline at the 15mg dose. Research revealed that simultaneous activation of both receptor pathways produces synergistic metabolic effects — significantly greater reductions in fasting insulin, triglycerides, and waist circumference compared with selective GLP-1 agonism alone.
Dual Agonist
SURMOUNT-1
GIP/GLP-1
Tirzepatide vs Semaglutide: Superior Glycaemic Control and Weight Reduction — SURPASS-2
New England Journal of Medicine
·
Frías et al., 2021
The SURPASS-2 trial enrolled 1,879 adults with type 2 diabetes comparing tirzepatide directly against semaglutide. All three tirzepatide doses produced greater reductions in HbA1c (up to −2.07% vs −1.86%) and body weight (up to −11.2 kg vs −5.7 kg). The 15mg arm achieved HbA1c below 5.7% in 27% of participants. Results established tirzepatide's superiority over the leading GLP-1 monotherapy for both metabolic control and fat reduction.
Human RCT
SURPASS-2
HbA1c Reduction
Semaglutide: 14.9% Mean Body Weight Reduction in Adults with Obesity — STEP 1 Trial
New England Journal of Medicine
·
Wilding et al., 2021
The STEP 1 Phase 3 trial evaluated once-weekly subcutaneous semaglutide 2.4mg in 1,961 adults with obesity. At 68 weeks, the semaglutide group achieved a mean 14.9% reduction in body weight vs 2.4% for placebo — with 86% of participants achieving ≥5% weight loss and 50% achieving ≥15%. The mechanistic basis is semaglutide's selective GLP-1 receptor agonism reducing appetite via central hypothalamic signalling, delaying gastric emptying, and improving pancreatic beta-cell function. These STEP 1 findings formed a key pillar of the regulatory approval of semaglutide (Wegovy) for chronic weight management.
GLP-1 Agonist
STEP 1
14.9% Weight Loss
Retatrutide: Triple GLP-1/GIP/Glucagon Receptor Agonism and 24.2% Weight Loss
New England Journal of Medicine
·
Jastreboff et al., 2023
Retatrutide is a unimolecular triple agonist targeting GLP-1, GIP, and glucagon receptors simultaneously. Phase 2 human research demonstrated mean weight reductions of up to 24.2% at 48 weeks — exceeding all previously published weight-loss interventions short of bariatric surgery. Secondary cardiometabolic endpoints showed reductions in waist circumference (up to 13.9 cm), systolic blood pressure, and triglycerides, alongside HbA1c reductions of up to 2.02 percentage points in the diabetic subgroup.
Triple Agonist
24.2% Weight Loss
Cardiometabolic
AOD-9604: Lipolytic Activity Without Diabetogenic Effect — Fat Metabolism Research
American Journal of Physiology — Endocrinology and Metabolism
·
Ng et al., 2000
AOD-9604 (Anti-Obesity Drug 9604) is a modified fragment of human growth hormone (hGH 176–191) designed to retain the lipolytic activity of full hGH without its diabetogenic or growth-promoting effects. Research by Ng et al. demonstrated that AOD-9604 stimulates lipolysis in adipocyte models and reduces fat accumulation in obese rodents through a mechanism involving beta-3 adrenergic receptor activation — independently of IGF-1. Subsequent human clinical investigation examined its effect on body composition and established a favourable safety and tolerability profile, supporting its use as a research tool for investigating selective fat metabolism pathways.
Lipolysis
hGH Fragment
No Diabetogenic Effect
MOTS-c: Mitochondrial-Derived Peptide Regulation of Metabolic Homeostasis and Insulin Sensitivity
Cell Metabolism
·
Lee et al., 2015
MOTS-c is a 16-amino acid peptide encoded within the mitochondrial genome. Lee et al. demonstrated exogenous MOTS-c significantly reduced obesity and improved insulin sensitivity in rodent models, acting on skeletal muscle via the AMPK pathway to enhance glucose uptake and fatty acid oxidation. Subsequent human research confirmed circulating MOTS-c declines with age and correlates positively with insulin sensitivity, VO²max, and markers of mitochondrial biogenesis.
Mitochondrial Peptide
AMPK
Insulin Sensitivity
GHK-Cu: Collagen Synthesis Stimulation and Tissue Remodelling Research
Journal of Peptide Science
·
Pickart & Margolina, 2018
GHK-Cu (glycyl-L-histidyl-L-lysine copper complex) is a naturally occurring tripeptide with strong affinity for copper ions. In vitro research characterised its role in stimulating collagen and glycosaminoglycan synthesis in dermal fibroblasts through TGF-β signalling activation. Additional findings confirm potent antioxidant activity and promotion of angiogenesis, establishing GHK-Cu as a widely studied compound in dermatological and tissue remodelling research.
Collagen Synthesis
TGF-β
Antioxidant
GHK-Cu Tripeptide Improves Collagen Density and Reduces MMP Activity in Human Skin
Journal of Investigative Dermatology
·
Simeon et al., 2000
Clinical and ex vivo evaluation of GHK-Cu on human skin demonstrated significantly increased type I and III collagen gene expression, proteoglycan synthesis, and dermal remodelling. Biopsies showed measurably increased collagen density and improved extracellular matrix organisation, with reductions in MMP activity that would otherwise degrade structural proteins. In photoaged skin participants, investigators reported significant improvements in skin thickness, firmness, and fine line depth.
Human Skin Biopsy
Collagen Density
MMP Reduction
Melanotan II: Melanocortin Receptor Subtype Selectivity and Melanogenesis in Cellular Models
Peptides
·
Wessells et al., 2003
Melanotan II is a cyclic heptapeptide analogue of alpha-MSH with potent agonist activity at MC1R, MC3R, MC4R, and MC5R. In vitro studies demonstrated significant stimulation of melanogenesis through the cAMP-PKA signalling cascade, producing dose-dependent increases in melanin synthesis in cultured melanocyte models. Its MC4R activity also triggered the research pathway that led to FDA-approved bremelanotide (Vyleesi).
Melanocortin Receptors
MC1R
cAMP-PKA
Phase I Human Trial: Melanotan II Produces Dose-Dependent Skin Tanning in Healthy Volunteers
Life Sciences
·
Dorr et al., 1996
The first clinical evaluation of MT-II in humans administered escalating doses to Fitzpatrick skin type I/II volunteers. All participants showed significant, objectively measured pigmentation increases within five days, with tanning observed in both sun-exposed and sun-protected areas — confirming a systemic melanogenic effect. This study established a well-tolerated dose range and, through unexpected observations, triggered the research programme that led to FDA-approved bremelanotide.
Phase I Human Trial
MC1R Activation
Eumelanin Synthesis
Afamelanotide Phase 3: Six-Fold Increase in Sun Exposure Tolerance — Clinically Approved
New England Journal of Medicine
·
Langendonk et al., 2015
A Phase 3 RCT in 74 patients with erythropoietic protoporphyria demonstrated afamelanotide produced a median six-fold increase in direct sunlight exposure tolerated vs placebo, alongside significant reductions in phototoxic pain. The mechanistic basis is potent stimulation of eumelanin synthesis providing a physical UV barrier. These results supported approval by the EMA (2014) and FDA (2019) of afamelanotide (Scenesse) for EPP.
Phase 3 RCT
EMA + FDA Approved
Eumelanin
Glutathione: Antioxidant Properties and Antimelanogenic Effects in Dermatological Research
Clinical, Cosmetic and Investigational Dermatology
·
Weschawalit et al., 2017
A placebo-controlled trial characterised glutathione's dual mechanism in skin research: direct antioxidant neutralisation of reactive oxygen species, and tyrosinase enzyme pathway inhibition to reduce melanin synthesis. Subjects receiving glutathione showed statistically significant improvements in skin luminosity and reductions in UV-induced melanin index vs placebo, establishing a mechanistic basis for its investigation in pigmentation and photoprotective research.
Antioxidant
Tyrosinase Inhibition
Melanin
Selank: GABA-Ergic Modulation and Neurotrophic Factor Research
Neurochemical Journal
·
Semenova et al., 2010
Selank is a synthetic heptapeptide analogue of immunomodulatory peptide Tuftsin. In-vitro research has investigated its effects on GABA-ergic transmission mechanisms and its potential role in modulating Brain-Derived Neurotrophic Factor (BDNF) expression in cellular models. Research is conducted exclusively in controlled laboratory environments.
GABA-ergic
BDNF
Immunopeptide
Selank Demonstrates Anxiolytic and Cognitive Benefits Without Sedation in Human Patients
Journal of Neurology and Psychiatry (S.S. Korsakov)
·
Semenova et al., 2009
Clinical evaluation in patients with generalised anxiety disorder demonstrated significant reductions in anxiety scores, improved mood, and enhanced memory and attention vs controls. Unlike benzodiazepines, Selank produced its anxiolytic effects without sedation, dependency, or withdrawal symptoms. Selank is registered as a nootropic and anxiolytic pharmaceutical in Russia and Ukraine, supported by multiple human clinical studies.
Human Clinical Data
Anxiety Reduction
No Sedation
Semax: ACTH(4-10) Analogue Activity and BDNF/TrkB Modulation in Hippocampal Research
Brain Research
·
Dolotov et al., 2006
Semax is a synthetic heptapeptide analogue of ACTH(4-7) with enhanced metabolic stability. Research demonstrated that Semax significantly upregulated both BDNF and TrkB receptor expression in the rat hippocampus, identifying a potential neuroprotective mechanism. Additional studies characterised improvements in learning, memory consolidation, and attention in controlled animal models. Semax holds regulatory status as a neuroprotective drug in Russia and Ukraine.
BDNF
Neuroprotection
ACTH Analogue
Semax Improves Attention and Processing Speed in Human Subjects Without Psychostimulant Side Effects
Neuroscience Research Communications
·
Kaplan et al., 1996
A human clinical study evaluated Semax across measures of selective attention, working memory, and information processing speed. Semax-treated participants demonstrated statistically significant improvements in attention task accuracy and processing speed vs control, without sedation, anxiolytic blunting, or psychostimulant tolerance. These human findings form part of the evidence base supporting Semax's registration as a licensed pharmaceutical in Russia and Ukraine for stroke, cognitive impairment, and traumatic brain injury.
Human Subjects
Attention & Memory
Licensed Pharmaceutical
Dihexa: HGF/MET Signalling, Synaptic Formation and Cognitive Enhancement in Rodent Models
Journal of Pharmacology and Experimental Therapeutics
·
McCoy et al., 2013
Dihexa (N-hexanoic-Tyr-Ile-(6) aminohexanoic amide) is a synthetic peptide derived from Angiotensin IV. McCoy et al. demonstrated that Dihexa potentiates hepatocyte growth factor (HGF) signalling at the MET receptor, promoting hippocampal synaptogenesis — the formation of new synaptic connections. In rodent cognitive models, Dihexa-treated animals displayed superior performance in spatial learning tasks and object recognition tests. Critically, Dihexa was reported to be approximately one million times more potent than BDNF in promoting synaptogenesis in hippocampal slice preparations, making it a potent research tool for neurodegenerative disease models.
HGF/MET Signalling
Synaptogenesis
Spatial Learning
Epithalon: Telomerase Activation and Cellular Senescence Studies
Bulletin of Experimental Biology and Medicine
·
Khavinson et al., 2003
Epithalon (Epitalon) is a tetrapeptide (Ala-Glu-Asp-Gly) derived from pineal gland extract. Research has investigated its potential role in telomerase activation in somatic cells, with laboratory findings examining implications for cellular senescence models. All research is conducted under strict in-vitro conditions. Epithalon remains one of the most studied naturally-derived tetrapeptides in longevity research.
Telomerase
Cellular Senescence
Pineal Peptides
Circulating MOTS-c Declines with Age and Correlates with Metabolic Health in Humans
Aging (Albany NY)
·
Kim et al., 2019
Researchers characterised MOTS-c as a detectable peptide in human blood and demonstrated a significant age-dependent decline in older adults. Individuals with high metabolic fitness maintained significantly elevated plasma MOTS-c, with levels correlating positively with insulin sensitivity, VO²max, and mitochondrial biogenesis markers. An exercise intervention arm showed plasma MOTS-c rose measurably within 30 minutes — confirming mitochondria release MOTS-c as a systemic endocrine signal in response to physiological energetic demand.
Human Subjects
Exercise-Induced
Mitochondrial Ageing
SS-31: Mitochondrial Cardiolipin Targeting and Cardiac Function Improvement in Age-Related Disease
Journal of the American College of Cardiology
·
Daubert et al., 2017
SS-31 (Elamipretide) is a mitochondria-targeted tetrapeptide that selectively concentrates in the inner mitochondrial membrane and stabilises cardiolipin — a critical phospholipid for mitochondrial cristae structure and ATP synthase efficiency. The SERCA-HEART Phase 2 human trial in heart failure with preserved ejection fraction (HFpEF) demonstrated that SS-31 significantly improved exercise tolerance (6-minute walk distance +21 m vs placebo) and reduced NT-proBNP levels. These findings in humans establish SS-31 as a mechanistically novel research compound targeting the mitochondrial dysfunction underlying age-related cardiac decline.
Cardiolipin
Human Phase 2
Mitochondrial Ageing
NAD+ Supplementation Increases Walking Speed and Improves Muscle Function in Older Adults
Nature Aging
·
Igarashi et al., 2022
A 12-week randomised, double-blind, placebo-controlled trial in older adults administered NMN (250mg/day). NMN significantly increased blood NAD+ levels, and in participants who exercised regularly, significantly improved gait speed, grip strength, and performance on the 30-second chair stand test. Gene expression analysis showed upregulation of muscle remodelling pathways and mitochondrial function genes. These findings in humans confirm NAD+ supplementation translates preclinical longevity findings into measurable functional improvements in ageing skeletal muscle.
Human RCT
Muscle Function
Healthy Ageing
