Buy PT-141 (Bremelanotide) – Peptide Partners

Product Overview & Specifications

PT-141 (Bremelanotide) is a synthetic heptapeptide melanocortin receptor agonist investigated for its activity at MC1R, MC3R, and MC4R subtypes in preclinical research. Peptide Partners supplies this research-grade material for in-vitro testing, laboratory experimentation, receptor pharmacology, structural biology, and G-protein coupled receptor (GPCR) research.

Published studies have examined bremelanotide using HEK-293 cell lines expressing melanocortin receptors, glioblastoma cell culture models, cryo-electron microscopy structural analyses, cAMP signaling assays, survivin expression profiling, and receptor-ligand binding studies. Research areas include melanocortin receptor subtype selectivity, Gs protein coupling mechanisms, intracellular cAMP accumulation, apoptotic pathway modulation, and molecular recognition of peptidic agonists.

The product name supplied for this listing is “PT-141 (Bremelanotide).” Researchers should verify the exact identity, sequence, formulation, and batch-specific certificate of analysis before beginning any experiment. Findings from published bremelanotide studies should not be assumed to apply to every commercial batch or formulation.

Product Specifications

Specification	Details
Product name	PT-141 (Bremelanotide)
Compound type	Synthetic heptapeptide melanocortin receptor agonist
Primary molecular targets	Melanocortin receptors MC1R, MC3R, and MC4R (higher affinity for MC4R)
Primary research areas	Melanocortin receptor pharmacology, cAMP signaling, GPCR activation, survivin expression modulation, glioblastoma cell biology, and receptor-ligand structural interactions
Product format	10 mg vials
Vial size	10 mg
Vial capacity	3 mL
Available box combinations	20 mg, 50 mg, and 100 mg
Multi-vial purity	99.74%
Independent testing	Yes
Endotoxin screening	Passed
Heavy-metals screening	Passed
Purity screening	Passed
Manufacturer ID	VI32
Batch ID	PT202605
Cost per milligram	$3.20–$4.20

The stated 99.74% purity is based on multi-vial testing. Researchers should review the batch-specific certificate of analysis before beginning any experiment.

Primary Research Studies & Findings

Melanocortin Receptors, Melanotropic Peptides and Penile Erection

Authors: Stephen H. King, Alexander V. Mayorov, Preeti Balse-Srinivasan, Victor J. Hruby, Todd W. Vanderah, and Hunter Wessells

Publication: Current Topics in Medicinal Chemistry, 2007;7(11):1098–1106

PMCID: PMC2694735

Reference: View publication

PT-141 (Bremelanotide) is a synthetic heptapeptide that represents a deaminated derivative and likely metabolite of melanotan-II (MT-II). This compound demonstrates strong binding affinity to melanocortin receptors 1, 3, and 4, with a higher affinity for MC4R over MC3R. Application of PT-141 to HEK-293 cells expressing MC4R increases cyclic adenosine monophosphate (cAMP) production, indicating that this compound, like MT-II, acts as an agonist at melanocortin receptors.

This in vitro cell culture study demonstrated receptor activation through the cAMP signaling pathway, which is a key second messenger system in G-protein coupled receptor signaling. The study utilized human embryonic kidney cells (HEK-293) transfected to express the melanocortin-4 receptor, providing direct evidence of PT-141’s agonist activity at this receptor subtype through measurement of intracellular cAMP accumulation.

The findings establish PT-141 as a functional melanocortin receptor agonist with subtype selectivity favoring MC4R. The research provides mechanistic insights into how peptidic melanocortin ligands activate GPCR signaling cascades through cAMP second messenger systems.

Plain-English Research Summary

This research showed that PT-141 works by binding to and activating specific protein receptors on cell surfaces called melanocortin receptors. When PT-141 attaches to these receptors on cells grown in laboratory dishes, it triggers a chain reaction inside the cells that produces more of a chemical messenger called cAMP. This proves that PT-141 functions as an activator (agonist) of these receptors, particularly the MC4R type, which is important for understanding how the drug might work in the body to affect sexual function and other processes controlled by these receptors.

Melanocortin Receptor Agonist Bremelanotide Induces Cell Death and Growth Inhibition in Glioblastoma Cells via Suppression of Survivin Expression

Authors: Shuhei Suzuki, Chifumi Kitanaka, and Masashi Okada

Publication: Anticancer Research, 2024;44(9):3875–3883

DOI: 10.21873/anticanres.17234

Reference: View publication

The effects of bremelanotide, a melanocortin receptor agonist, were investigated in human glioblastoma cell lines using in vitro methodologies. Bremelanotide reduced survivin expression and induced cell death in glioblastoma cells at concentrations that were not toxic to normal human cells. Both of these effects were canceled in the presence of an antagonist of melanocortin receptors 3 and 4, confirming receptor-mediated mechanisms.

Bremelanotide-induced cell death was prevented by forced over-expression of survivin in glioblastoma cells, suggesting that bremelanotide induces glioblastoma cell death by inhibiting the expression of survivin, an anti-apoptotic protein. Additionally, bremelanotide promoted cell death induced by chemotherapeutic agents such as temozolomide and osimertinib.

The study utilized human glioblastoma cell lines (U-87, GS-Y01, and GS-Y03) and normal human fibroblasts (IMR-90) to assess cell viability, survivin protein expression, and apoptotic markers through western blotting, cell viability assays, and molecular biology techniques. The findings demonstrate that bremelanotide selectively targets glioblastoma cells through melanocortin receptor-mediated survivin suppression.

Plain-English Research Summary

This study discovered that bremelanotide can kill brain cancer cells (glioblastoma) grown in laboratory culture dishes without harming normal cells. The drug works by reducing levels of a protein called survivin that helps cancer cells stay alive. When survivin levels drop, the cancer cells die through a natural cell death process. The researchers proved this by showing that when they artificially increased survivin levels in the cancer cells, bremelanotide could no longer kill them. Importantly, bremelanotide also made standard chemotherapy drugs work better against these brain cancer cells, suggesting it could potentially be used alongside existing cancer treatments.

Structural Insights Into Ligand Recognition and Activation of the Melanocortin-4 Receptor

Authors: Huibing Zhang, Li-Nan Chen, Dehua Yang, Chunyou Mao, Qingya Shen, Wenbo Feng, Dan-Dan Shen, Antao Dai, Shanshan Xie, Yan Zhou, Jiao Qin, Jin-Peng Sun, Daniel H. Scharf, Tingjun Hou, Tianhua Zhou, Ming-Wei Wang, and Yan Zhang

Publication: Cell Research, 2021;31:1163–1175

DOI: 10.1038/s41422-021-00552-3

Reference: View publication

This study reports four high-resolution structures of full-length melanocortin-4 receptor (MC4R) in complex with the heterotrimeric Gs protein stimulated by different ligands, including the FDA-approved drug bremelanotide (Vyleesi™). The structures were determined using single-particle cryo-electron microscopy (cryo-EM), an advanced in vitro structural biology technique that allows visualization of protein complexes at near-atomic resolution.

The bremelanotide-MC4R-Gs complex structure was deposited in the Protein Data Bank under accession number 7F55 and Electron Microscopy Data Bank under accession code 31458, at a resolution of 3.1 Ångströms. Together with pharmacological studies, the results reveal the conserved binding mode of peptidic agonists and provide molecular details of agonist recognition underlying receptor subtype selectivity.

The study demonstrates a distinct activation mechanism for MC4R, offering new insights into G protein coupling and receptor activation at the molecular level. The structural data provide a framework for understanding how peptidic ligands achieve receptor subtype selectivity and for designing improved melanocortin receptor modulators.

Plain-English Research Summary

Scientists used a powerful microscopy technique to take extremely detailed pictures of bremelanotide attached to its target receptor (MC4R) in cells. These images are so detailed that they can see the exact shape and position of individual atoms in the drug-receptor complex. This is like getting a blueprint showing exactly how a key fits into a lock. By understanding the precise three-dimensional structure of how bremelanotide binds to and activates the MC4R receptor, researchers can better understand why the drug works and potentially design improved medications that are more selective and effective.

Standard Research Disclaimer

Research Use Only. Not for use in diagnostic tests.

This product is solely intended for research purposes as a chemical compound. It is designated exclusively for in-vitro testing and laboratory experimentation. All information provided about this product is educational and should be evaluated by appropriately qualified research personnel.

By law, bodily introduction of this product into humans or animals is strictly prohibited. This compound must not be used, administered, or represented as a drug, food, dietary supplement, sexual dysfunction treatment, cancer treatment, melanocortin therapy, diagnostic material, or medical treatment. It is not intended to diagnose, treat, cure, or prevent any disease. It should be handled only by licensed and qualified professionals in an appropriately equipped laboratory and in accordance with applicable laws, institutional procedures, and relevant safety requirements.