PT-141 Pen

PT-141 (Bremelanotide) je syntetický peptid ze třídy ligandů melanokortinových receptorů; chemicky jde o cyklický heptapeptid s intramolekulárním laktamovým můstkem. Ve vědeckém výzkumu je studován jako modelová sloučenina pro farmakologii melanokortinových receptorů a jako referenční standard při analytické práci. Tato sloučenina je nabízena jako předplněné injekční pero o objemu 3 ml s obsahem 10 mg, výhradně pro laboratorní a výzkumné účely.

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.

Oblasti výzkumu

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.
• Studie stability a rozpustnosti lyofilizovaných peptidů za kontrolovaných podmínek.

Každá z těchto aplikací zahrnuje kontrolovaný laboratorní nebo preklinický modelový výzkum.

PT-141 in our research range

Tato varianta patří do řady předplněných injekčních per: sloučenin obsažených v rozpuštěné formě v zapečetěné zásobní vložce, takže výzkumník nemusí provádět vlastní krok rozpouštění. Stejná sloučenina je jinde v sortimentu dostupná jako lyofilizát v lahvičce. Jiné sloučeniny v řadě per působí na zcela jiný biochemický systém; forma nic nevypovídá o třídě látek.

Specifikace

Tvar, manipulace a skladování

The compound is dissolved in a sealed 3 ml glass cartridge in a pen with a click mechanism. A separate dissolution step is not required with this version; the cartridge remains closed until a needle is inserted. The label includes a table showing the relationship between click settings and dispensed volume, allowing sample collections to be reproducibly recorded in a protocol.

Store the pen refrigerated between 2 and 8 °C, protected from light and in the original packaging. Handle the pen in a clean working environment, use a new sterile needle for each draw to prevent cross-contamination, and wear standard personal protective equipment. Keep the material out of reach of unauthorized persons.

Složení a laboratorní výsledky

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.

Analysis certificates of the relevant parties are on our stránka s výsledky laboratorních testů.

Často kladené otázky

Do jaké třídy chemických látek patří 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 jaké formě je sloučenina dodávána?
Jako předplněné injekční pero se zapečetěnou zásobní vložkou o objemu 3 ml obsahující 10 mg. Balení navíc obsahuje deset sterilních jehel k peru a alkoholové ubrousky.

How do I store the pen?
Refrigerated between 2 and 8 °C, in a dark place and in the original packaging. Do not freeze.