UFP 101 peptide

UFP 101 peptide

• Handling and Storage of Synthetic Peptides
• Material Safety Data Sheets (MSDS)

Bn-GGGFTGARKSARKRKNQ-NH2

Bn-Gly-Gly-Gly-Phe-Thr-Gly-Ala-Arg-Lys-Ser-Ala-Arg-Lys-Arg-Lys-Asn-Gln-NH2

17

95.74%

C₈₂H₁₃₈N₃₂O₂₁

1908.19

Synthetic

Powder

UFP 101 is a potent, selective and competitive antagonist at the nociceptin receptor. UFP 101 binds to nociceptin receptors with high affinity (pKi 10.24) and possesses ~3000 fold selectivity over the classical opioid receptors. UFP 101 is antinociceptive and opposes the action of nociceptin in vivo, with an antinociceptive effect when given i.c.v. while being inactive following spinal administration in mice. UFP 101 also shows antidepressant effects in distinct species and can reduce microvascular inflammation to lipopolysaccharide in vivo.

Normally, this peptide will be delivered in lyophilized form and should be stored in a freezer at or below -20 °C. For more details, please refer to the manual:Handling and Storage of Synthetic Peptides

• Calo et al (2002) [Nphe1,Arg14,Lys15]Nociceptin-NH2, a novel potent and selective antagonist of the nociceptin/orphanin FQ receptor. Br.J.Pharmacol. 136 303 PMID: 12010780
• Calo et al (2005) UFP-101, a peptide antagonist selective for the nociceptin/orphanin FQ receptor. CNS Drug Rev. 11(2) 97 PMID: 16007234
• Brookes et al (2013) The nociceptin/orphanin FQ receptor antagonist UFP-101 reduces microvascular inflammation to lipopolysaccharide in vivo. PLoS One 8(9) e74943 PMID: 24086402

Trifluoroacetic acid (TFA) has a significant impact on peptides due to its role in the peptide synthesis process.

TFA is essential for the protonation of peptides that lack basic amino acids such as Arginine (Arg), Histidine (His), and Lysine (Lys), or ones that have blocked N-termini. As a result, peptides often contain TFA salts in the final product.

TFA residues, when present in custom peptides, can cause unpredictable fluctuations in experimental data. At a nanomolar (nM) level, TFA can influence cell experiments, hindering cell growth at low concentrations (as low as 10 nM) and promoting it at higher doses (0.5–7.0 mM). It can also serve as an allosteric regulator on the GlyR of glycine receptors, thereby increasing receptor activity at lower glycine concentrations.

In an in vivo setting, TFA can trifluoroacetylate amino groups in proteins and phospholipids, inducing potentially unwanted antibody responses. Moreover, TFA can impact structure studies as it affects spectrum absorption.