Cardioprotective Research Peptides

23 research peptides demonstrate cardioprotective properties. This collection covers their mechanisms, evidence base, and research applications.

Preclinical | Healing & Recovery

TB-500 is a synthetic fragment of thymosin beta-4 (Tβ4), a naturally occurring 43-amino-acid peptide found throughout human tissues.

Mechanism: TB-500 works primarily through actin sequestration — it binds to G-actin monomers, preventing premature polymerization, which allows repair cells to migrate rapidly to injured areas.

FDA Approved | Metabolic / GLP-1 Agonist

Semaglutide is an FDA-approved GLP-1 receptor agonist (MW ~4113.6 g/mol, molecular formula C187H291N45O59) with 94% sequence homology to human GLP-1.

Mechanism: Semaglutide mimics the GLP-1 hormone by binding to GLP-1 receptors on pancreatic beta cells (glucose-dependent), brain (hypothalamus appetite centers), stomach, and intestines.

Preclinical | Growth Hormone Secretagogue

GHRP-6 (Growth Hormone-Releasing Peptide 6) is a synthetic hexapeptide that functions as a potent growth hormone secretagogue by binding to the ghrelin receptor (GHS-R1a).

Mechanism: GHRP-6 functions as a synthetic ghrelin mimetic by binding to GHS-R1a in the pituitary and hypothalamus, triggering pulsatile GH release and raising IGF-1 levels.

FDA Approved | Metabolic / Mitochondrial

SS-31 (Elamipretide) is a mitochondria-targeted tetrapeptide that selectively concentrates in the inner mitochondrial membrane, binding to cardiolipin and stabilizing cristae structure.

Mechanism: SS-31 is a cell-permeable peptide with an alternating aromatic-cationic motif (D-Arg-Dmt-Lys-Phe-NH2) that allows it to cross membranes without a carrier.

Phase I–II Clinical Trials | Growth Hormone Secretagogue

Hexarelin is a synthetic hexapeptide growth hormone secretagogue that binds to the ghrelin receptor (GHS-R1a). It is considered one of the most potent GHRPs available, stimulating greater GH release than GHRH alone.

Mechanism: Hexarelin binds to and activates the ghrelin/growth hormone secretagogue receptor (GHS-R1a) in the pituitary and hypothalamus through a triple mechanism: direct stimulation of pituitary somatotroph...

Preclinical | Metabolic / Mitochondrial

Humanin is a 21-24 amino acid mitochondria-derived peptide (MDP) encoded by the MT-RNR2 gene in mitochondrial DNA. It was originally discovered in 2001 for its ability to protect neurons from Alzheimer's disease-related toxicity.

Mechanism: Humanin operates through both intracellular and extracellular mechanisms. Intracellularly, it binds pro-apoptotic proteins BAX, Bim, and tBid to inhibit caspase activation and cell death.

FDA Approved | Metabolic / GLP-1 Agonist

Liraglutide is an FDA-approved GLP-1 receptor agonist with 97% amino acid sequence homology to endogenous human GLP-1. Developed by Novo Nordisk, it is approved as Victoza for type 2 diabetes and Saxenda for chronic weight management.

Mechanism: Liraglutide binds to GLP-1 receptors on pancreatic β-cells, increasing intracellular cAMP and triggering glucose-dependent insulin secretion.

Phase III / NDA Filed | Healing & Recovery

Thymosin beta-4 (Tβ4) is a naturally occurring 43-amino acid protein found in virtually all human and animal cells. It is the most abundant member of the beta-thymosin family and plays fundamental roles in cell migration, wound healing, and tissue...

Mechanism: Thymosin beta-4 is the primary intracellular G-actin sequestering protein, maintaining actin monomer pools and regulating cytoskeletal dynamics essential for cell migration.

FDA Approved | Cardiovascular / Vasoactive

Angiotensin II is an endogenous 8-amino-acid peptide (sequence: Asp-Arg-Val-Tyr-Ile-His-Pro-Phe, MW ~1046.2 g/mol) that serves as the primary effector of the renin-angiotensin-aldosterone system (RAAS).

Mechanism: Angiotensin II binds to AT1 receptors on vascular smooth muscle cells, activating Gq-coupled signaling that increases intracellular calcium via phospholipase C and IP3, producing potent...

Preclinical / Early Research | Cardiovascular / Vasoactive

Angiotensin 1-7 is an endogenous 7-amino-acid peptide (sequence: Asp-Arg-Val-Tyr-Ile-His-Pro, MW ~899.0 g/mol) formed primarily by ACE2-mediated cleavage of angiotensin II.

Mechanism: Angiotensin 1-7 signals primarily through the Mas receptor (MasR), a G-protein-coupled receptor. Activation of MasR stimulates nitric oxide (NO) and prostaglandin release, producing vasodilation and...

Well-Characterized Endogenous Mediator | Cardiovascular / Vasoactive

Bradykinin is a 9-amino-acid vasoactive peptide (sequence: Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg, MW ~1060.2 g/mol) generated by the kallikrein-kinin system through proteolytic cleavage of high-molecular-weight kininogen by plasma kallikrein.

Mechanism: Bradykinin binds primarily to constitutively expressed B2 receptors (BDKRB2), a Gq-coupled GPCR, on endothelial cells and smooth muscle.

FDA Approved (Declining Use) | Cardiovascular / Natriuretic

Nesiritide is a recombinant form of human B-type natriuretic peptide (BNP), a 32-amino-acid peptide (MW ~3464 g/mol) with a 17-residue disulfide ring structure.

Mechanism: Nesiritide binds to natriuretic peptide receptor A (NPR-A), a particulate guanylyl cyclase receptor, stimulating intracellular cGMP production.

Approved in Japan / Established Biomarker | Cardiovascular / Natriuretic

Atrial natriuretic peptide (ANP) is a 28-amino-acid hormone (MW ~3080 g/mol) secreted primarily by atrial cardiomyocytes in response to atrial stretch from volume overload. It is a key regulator of blood volume, sodium balance, and blood pressure.

Mechanism: ANP binds to natriuretic peptide receptor A (NPR-A), a transmembrane guanylyl cyclase receptor, stimulating intracellular cGMP production.

Established Biomarker / Therapeutic Basis | Cardiovascular / Natriuretic

B-type natriuretic peptide (BNP) is a 32-amino-acid cardiac hormone (MW ~3464 g/mol) secreted primarily by ventricular cardiomyocytes in response to myocardial wall stress from volume overload or pressure overload.

Mechanism: BNP binds to natriuretic peptide receptor A (NPR-A), activating the intracellular guanylyl cyclase domain and increasing cGMP production.

Well-Characterized / ERA Drugs Approved | Cardiovascular / Vasoactive

Endothelin-1 (ET-1) is a 21-amino-acid peptide (MW ~2491.9 g/mol) produced primarily by vascular endothelial cells. It is the most potent endogenous vasoconstrictor known, with effects lasting hours.

Mechanism: ET-1 signals through two G-protein-coupled receptors: ETA and ETB. ETA receptors on vascular smooth muscle mediate sustained vasoconstriction via Gq-phospholipase C activation, increasing...