I. What is PT141?
PT141 (Bremelanotide) is a synthetic melanocortin receptor (MC3R/MC4R) agonist, a derivative of α-melanocyte-stimulating hormone (α-MSH), and a metabolite of Melanotan-II (MT-II) after the removal of its C-terminal amino group. Through specific structural modifications, it can efficiently penetrate the blood-brain barrier and target the central nervous system, primarily regulating physiological processes such as libido and energy metabolism. Unlike traditional peripherally acting drugs, it is an important peptide in the fields of neuroendocrinology, sexual dysfunction, and metabolism. It has been approved by the FDA (trade name Vyleesi) and is also widely used in scientific research.
II. Product Parameters
- Product Name: PT141 (Bremelanotide)
- Category: Synthetic cyclic heptapeptide, melanocortin receptor (MC3R/MC4R) agonist
- CAS No.: 189691-06-3
- Molecular Formula: C₅₀H₆₈N₁₄O₁₀
- Molecular Weight: 1025.16
- Appearance: White lyophilized powder
- Purity: ≥98% (up to 99.73% for high-end products)
- Solubility: Easily soluble in sterile water for injection and DMSO
- Storage Conditions: Store at -20℃, sealed, protected from light, and in a dry place. The powder is stable for up to 3 years. Avoid repeated freeze-thaw cycles after dissolution. It is recommended to use as soon as possible.
- Peptide sequence: Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-OH (Side chain lactam cyclized heptapeptide)
III. Core Advantages
- Central targeting, unique mechanism: It can penetrate the blood-brain barrier and directly act on the central MC4R receptor, regulating core pathways of libido and energy metabolism. Unlike traditional peripheral vasodilators, it has a significant effect on central sexual dysfunction.
- Optimized structure, low side effects: Through N-terminal acetylation, D-Phe modification, and side chain cyclization, it significantly reduces the side effect of skin pigmentation, while improving anti-enzymatic ability and receptor affinity, exhibiting excellent biocompatibility.
- Dual efficacy, suitable for multiple scenarios: It focuses on sexual function regulation, and can also assist in regulating metabolism and suppressing appetite. It also possesses neuroprotective and anti-inflammatory potential, making it suitable for multiple scenarios in scientific research and clinical translation.
- Rapid onset of action and high compliance: Subcutaneous injection ensures high bioavailability, rapid and stable onset of action, moderate frequency of use, and no complex procedures, making it suitable for long-term research or clinical use.
- Clinically validated and highly safe: Approved by the FDA and validated through multiple phases of clinical trials, with mild and mostly transient side effects. Comprehensive safety data ensures high reliability for research use.
IV. Main Functions
- Central sexual function regulation: Activates hypothalamic MC4R receptors, promotes dopamine release, regulates the hypothalamus-pituitary-gonadal axis, enhances libido, alleviates sexual distress, suitable for both men and women, and also improves erectile dysfunction unresponsive to PDE5 inhibitors.
- Metabolic and weight regulation: Stimulates MC4R receptors, suppresses appetite, reduces food intake, and increases energy expenditure, providing a new target for research on obesity and metabolic syndrome. It can synergistically work with drugs such as telpolide for weight loss.
- Neuroprotection and Tissue Protection: Inhibits central nervous system inflammation, promotes nerve repair, and demonstrates neuroprotective effects in models of cerebral ischemia and neurodegenerative diseases. It can also help regulate mood and alleviate depression-related sexual dysfunction.
- Research Tool Value: As a highly specific MC4R agonist, it is used in basic research on the melanocortin receptor signaling pathway, neuroendocrinology, and behavioral pharmacology. It is a key tool peptide for target validation and compound screening.
V. Target Population
- Research Professionals: Researchers specializing in neuroendocrinology, the melanocortin receptor pathway, sexual dysfunction, and obesity metabolism, for basic experiments, target validation, and drug development.
- Clinical Professionals: Medical staff in andrology, gynecology, and endocrinology, for clinical research and protocol exploration in related diseases (such as female hypoactive sexual desire disorder) (must be conducted under professional guidance).
- Exercise and Rehabilitation Population: Individuals needing to regulate physical fitness, improve metabolism, and assist in restoring physical condition (must strictly follow professional guidance and control dosage). - Peptide R&D and Production Professionals: For peptide raw material R&D, formulation optimization, and related product manufacturing (for research and professional use only).
VI. Success Stories
1. FDA-Approved Clinical Case (Treatment of Hypoactive Sexual Desire in Women): In 2019, PT141 (trade name Vyleesi) was approved by the FDA for the treatment of hypoactive sexual desire disorder (HSDD) in premenopausal women, becoming the world's first centrally targeted HSDD treatment, filling a clinical gap. This approval was based on two Phase III clinical trials (enrolling a total of 1247 patients). Results showed that patients in the PT141 treatment group had significantly improved libido scores compared to the placebo group (a total increase of 0.35 points, P<0.001) and significantly reduced sexual distress scores (a total decrease of 0.33 points, P<0.001), validating its clinical efficacy and safety. It is currently being promoted for clinical research and treatment in multiple regions worldwide.
2. Research Translation Case (Obesity Combination Therapy Study): In June 2024, Palatin Technologies announced the initiation of a Phase II clinical trial of PT141 in combination with Tirzepatide for the treatment of obesity, exploring their synergistic effects on weight loss and metabolic improvement. Preliminary basic research showed that PT141 inhibits appetite by activating MC4R, and its combination with the GLP-1 receptor agonist Tirzepatide can achieve a dual effect of "weight loss + metabolic regulation," providing an important research direction for novel treatment options for obesity. This clinical trial is currently progressing smoothly.
3. Research Tool Application Case: An international research institution utilized the highly specific MC4R agonist activity of PT141 to conduct research on the melanocortin-dopamine interaction mechanism, successfully elucidating the central regulatory pathway of the libido, mood, and reward circuit. This provided key experimental data for research on the comorbidity mechanisms of depression, anxiety, and sexual dysfunction. The relevant research results have been published in core international neuroscience journals, advancing research progress in the field of neuroendocrinology.
4. Case Study: PT141, a structurally optimized derivative of Melanotan-II, significantly reduces skin pigmentation side effects while retaining central nervous system activity through modifications such as removing the C-terminal amide group and replacing amino acid residues. Its structural optimization approach provides a classic template for the design of long-acting, low-toxicity peptide drugs and has been widely applied in the development of similar melanocortin receptor agonists.
VII. Precautions
- This product is for scientific research, clinical studies, and professional formulation development only. It is not a drug or health product and should not be misused or used for therapeutic purposes in humans.
- Contraindications: This product is contraindicated in minors, pregnant women, breastfeeding women, individuals with uncontrolled hypertension or cardiovascular disease, and those allergic to PT141 or peptides. Postmenopausal women and men should use this product after professional evaluation (FDA label only applies to HSDD treatment in premenopausal women).
- Storage Requirements: Strictly store at -20℃, sealed, protected from light, and in a dry place. After dissolving, aliquot and refrigerate. Use as soon as possible. Avoid repeated freeze-thaw cycles to prevent loss of peptide activity.
- Usage Guidelines: Strictly control the dosage and frequency of administration. Aseptic technique must be observed during subcutaneous injection to avoid injection site infection. If severe nausea or persistent high blood pressure occurs after administration, discontinue use immediately and seek medical attention promptly.
- Drug Interactions: Avoid concurrent use with naltrexone (as it will reduce the efficacy of naltrexone). Use with caution when co-administering with antihypertensive drugs or PDE5 inhibitors, as there may be blood pressure-related synergistic effects; use under professional guidance.
Hot Tags: High-quality peptide drug PT141 10mg/vial, China High-quality peptide drug PT141 10mg/vial manufacturers, suppliers, factory, Original Manufacturer High Purity GHRP 2, Enhanced Snap 8, Top Quality Liraglutide, High Efficiency Ara 290, High Purity PEG MGF, High Efficiency Matrixyl
