Bremelanotide
Also known as PT-141 · PT 141 · Bremelanotide acetate · Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH
Bremelanotide is a synthetic cyclic heptapeptide analog of alpha-MSH that acts as a non-selective agonist at melanocortin receptors, with characterized activity at MC1R, MC3R, and MC4R subtypes.
The overview
What is Bremelanotide?
Bremelanotide is a synthetic cyclic heptapeptide analog of alpha-MSH that acts as a non-selective agonist at melanocortin receptors, with characterized activity at MC1R, MC3R, and MC4R subtypes. The peptide's N-acetyl-Nle cap and the Asp-Lys lactam bridge constrain its conformation, stabilizing the His-D-Phe-Arg-Trp pharmacophore that engages the receptor orthosteric pocket. In vitro, receptor occupancy promotes coupling to Gs and activation of adenylate cyclase, raising intracellular cAMP. In recombinant systems such as HEK-293 cells expressing human MC4R, application of bremelanotide produces concentration-dependent cAMP accumulation in functional reporter assays, and the peptide competes with radiolabeled NDP-alpha-MSH in competitive-binding assays, indices used to quantify agonist potency and affinity. Reported binding favors MC4R over MC3R, with additional MC1R interaction. The D-Phe substitution and cyclic backbone confer resistance to enzymatic degradation relative to linear melanocortin peptides, a structure-activity feature studied in receptor-pharmacology and NMR conformational work. These properties make it a reference ligand for probing melanocortin GPCR signaling and second-messenger cascades in cell-based models.
In the research
Where Bremelanotide shows up
The areas researchers focus on with Bremelanotide - and why it has the science community paying attention.
- Melanocortin (MC1R/MC3R/MC4R) receptor pharmacology and competitive radioligand binding assays
- Gs/adenylate-cyclase/cAMP second-messenger signaling in recombinant GPCR cell models
- Structure-activity relationships of cyclic lactam-bridged alpha-MSH analogs (D-Phe, Nle substitutions)
- NMR/conformational analysis of melanocortin peptide-receptor interactions
- Enzymatic-stability and conformational-constraint studies of cyclic peptides versus linear melanocortins
By the numbers
The facts that matter
To the molecule
Molecular specifications
Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH (N-acetyl-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys], lactam-bridged between Asp and Lys side chains)Sourced, not claimed
The science behind it
The peer-reviewed studies behind Bremelanotide, linked so you can read them yourself.
- Molinoff PB, Shadiack AM, Earle D, Diamond LE, Quon CY (2003). PT-141: a melanocortin agonist for the treatment of sexual dysfunction Annals of the New York Academy of Sciences.
“PT-141, a synthetic peptide analogue of alpha-MSH, is an agonist at melanocortin receptors including the MC3R and MC4R, which are expressed primarily in the central nervous system.”
- Kingsberg SA, Clayton AH, Portman D, Williams LA, Krop J, Jordan R, Lucas J, Simon JA (2019). Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder: Two Randomized Phase 3 Trials Obstetrics & Gynecology.
“Two identical phase 3, randomized, double-blind, placebo-controlled, multicenter clinical trials (RECONNECT) evaluated the safety [and efficacy of bremelanotide in premenopausal women].”
- White WB, Myers MG, Jordan R, Lucas J (2017). Usefulness of ambulatory blood pressure monitoring to assess the melanocortin receptor agonist bremelanotide Journal of Hypertension.
“The effects of bremelanotide administration on ambulatory BP and heart rate were assessed in a randomized, double-blind, placebo-controlled trial; small transient increases in systolic and diastolic blood pressure were observed following bremelanotide doses.”
- Safarinejad MR, Hosseini SY (2008). Salvage of sildenafil failures with bremelanotide: a randomized, double-blind, placebo controlled study The Journal of Urology.
“We evaluated the safety and efficacy of intranasal bremelanotide in men with erectile dysfunction who did not respond to sildenafil... Bremelanotide can be an alternative treatment for erectile dysfunction with a potentially broad patient base.”
- Diamond LE, Earle DC, Rosen RC, Willett MS, Molinoff PB (2004). Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction International Journal of Impotence Research.
“This randomized, double-blind, placebo-controlled study evaluated the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction.”
Straight answers
Questions, answered
Is Bremelanotide approved by the FDA?
No. Bremelanotide is not an FDA-approved drug. We supply it as a research-use-only reference compound, identity-verified for purity with a COA on every vial.
What class of compound is Bremelanotide?
Bremelanotide is classified as: Synthetic cyclic heptapeptide; alpha-melanocyte-stimulating hormone (alpha-MSH) analog; melanocortin receptor agonist.
What is the molecular weight of Bremelanotide?
The molecular weight of Bremelanotide is 1025.2 g/mol (free base; monoisotopic ~1024.5), with a molecular formula of C50H68N14O10.
What is the CAS number for Bremelanotide?
The CAS Registry Number for Bremelanotide is 189691-06-3.
What is the amino acid sequence of Bremelanotide?
Bremelanotide has the sequence: Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH (N-acetyl-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys], lactam-bridged between Asp and Lys side chains).
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For in-vitro laboratory research use only. Not for human or animal consumption. Bodily introduction into humans or animals is strictly prohibited by law. Bremelanotide is not a drug and is not intended to diagnose, treat, cure, or prevent any disease. These statements have not been evaluated by the FDA.