PT-141 Pen

PT-141 (Bremelanotide) is a synthetic peptide belonging to the class of melanocortin receptor ligands; chemically, it is a cyclic heptapeptide with an intramolecular lactam bridge. In scientific research, it is studied as a model compound for melanocortin receptor pharmacology and as a reference standard in analytical work. This compound is offered as a 3 ml pre-filled injection pen containing 10 mg, exclusively for laboratory and research purposes.

What is PT-141?

PT-141 is a cyclic heptapeptide with the sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH, systematically designated as N-acetyl-L-norleucyl-L-α-aspartyl-L-histidyl-D-phenylalanyl-L-arginyl-L-tryptophyll-L-lysine-(2→7)-lactam. The ring is formed by the amide bond between the side chains of the aspartic acid and lysine, thereby fixing the molecule in a fixed spatial conformation; together with the D-configuration of the phenylalanine residue, this makes the peptide less susceptible to degradation by peptidases in vitro than a comparable linear motif. The compound is derived from the endogenous melanocortin peptide α-MSH and contains the conserved His-D-Phe-Arg-Trp core motif, described in the literature as the pharmacophore of this peptide family.

In research models, PT-141 is characterized as an agonist of the melanocortin receptors, a family of G-protein-coupled receptors referred to in the literature as MC1R through MC5R. In cell models expressing these subtypes, the measured response occurs via activation of adenylate cyclase and an increase in intracellular cAMP; this second-messenger response forms the basis for binding and activity determinations in vitro. Because the peptide does not target the subtypes equally, it serves as a comparison ligand in selectivity studies. Consequently, PT-141 is used as a model compound and reference substance within scientific research.

Raziskovalna področja

In a laboratory context, PT-141 occurs in the following research areas, among others:

• Receptor research into G-protein-coupled melanocortin receptors (MC1R to MC5R) and the subtype selectivity of cyclic α-MSH analogues in vitro.
• Signal transduction study in which the cAMP response is monitored in cell lines expressing a melanocortin receptor.
• Structure-activity relationship study into the influence of the lactam bridge and D-phenylalanine substitution on receptor affinity.
• Biophysical modeling of conformation-restricted cyclic peptides and their enzymatic stability.
• Analytical method development and validation (HPLC, LC-MS) using PT-141 as the reference standard.
• Študije stabilnosti in topnosti liofiliziranih peptidov v nadzorovanih pogojih.

Vsaka od teh aplikacij vključuje nadzorovane laboratorijske ali predklinične modelne raziskave.

PT-141 in our research range

This version belongs to the line of pre-filled injection pens: compounds contained in dissolved form in a sealed cartridge, so that a researcher does not need to go through their own dissolution step. The same compound is available elsewhere in the range as freeze-dried lyophilisate in a vial. Other compounds within the pen line act on a completely different biochemical system; the form indicates nothing about the substance class.

Specifikacije

Oblika, ravnanje in shranjevanje

Spojina se raztopi v zaprti 3 ml stekleni kartuši v peresniku z mehanizmom na klik. Pri tej različici ni potreben ločen korak raztapljanja; kartuša ostane zaprta, dokler ni vstavljena igla. Nalepka vsebuje tabelo, ki prikazuje razmerje med nastavitvami klika in iztisnjeno prostornino, kar omogoča ponovljivo beleženje odvzetih vzorcev v protokolu.

Peresnik shranjujte v hladilniku pri temperaturi med 2 in 8 °C, zaščiteno pred svetlobo in v originalni embalaži. S peresnikom ravnajte v čistem delovnem okolju, za vsak vdih uporabite novo sterilno iglo, da preprečite navzkrižno kontaminacijo, in nosite standardno osebno zaščitno opremo. Material hranite izven dosega nepooblaščenih oseb.

Sestava in laboratorijski rezultati

The raw material used has a controlled purity of ≥ 99% (HPLC). The pen contains PT-141 in a sterile aqueous base; the total amount of active substance per version is stated on the label.

Analizni certifikati ustreznih strank so na naši stran z rezultati laboratorijskih preiskav.

Pogosto zastavljena vprašanja

V katero skupino kemičnih spojin spada PT-141?
PT-141 is a synthetic cyclic heptapeptide belonging to the group of melanocortin receptor ligands, derived from the endogenous peptide α-MSH. It is therefore not a small organic molecule, but a peptide with a defined amino acid sequence.

What role does the lactam bridge play in research?
The amide bond between the side chains of aspartic acid and lysine closes the molecule into a ring. This cyclization fixes the conformation and increases resistance to enzymatic degradation in vitro, making the compound a widely used model in structure-activity research.

V kakšni obliki je dobavljena spojina?
As a pre-filled injection pen with a sealed 3 ml cartridge containing 10 mg. The box also contains ten sterile pen needles and alcohol wipes.

Kako shranim pero?
Hladite pri temperaturi med 2 in 8 °C, v temnem prostoru in v originalni embalaži. Ne zamrzujte.