Amino Acid Derivatives

FAM-labeled Forkhead derived peptide woodtide (ab/em = 494/521 nm) is used as a substrate for the DYRK family of kinases in in-vitro analysis. Woodtide corresponds to residues 324-334 of transcription factor FKHR with two lysine residues added at the N-terminus to facilitate binding to phosphocellulose paper.

Tos-GPK-AMC, a fluorogenic substrate for trypsin, gingipain K, and cathepsin L.

Impurity of atosiban.

<p>Bachem ID: 4037181.</p>

TGOT exhibits a 640-fold increase in oxytocic/ antidiuretic selectivity relative to oxytocin.

Endogenous kappa-receptor antagonist.

The peptide hormone osteocalcin is involved not only in bone formation, it also plays an important role in glucose metabolism and could regulate testosteron. In mice, only the completely decarboxylated form of the peptide shows the latter hormonal activities, whereas in humans, osteocalcin, partially decarboxylated osteocalcins, and the uncarboxylated peptide seem to be involved. Generally, obese individuals have been shown to have lower osteocalcin(s) levels than non-obese controls, and type 2 diabetic individuals have lower plasma osteocalcin than non-diabetic individuals.

A good substrate for carboxypeptidase Y, the Streptomyces griseus carboxypeptidase, and the membrane-associated carboxypeptidase ysc-lambda.

Most circulating ghrelin is des-octanoyl ghrelin. The non-acylated ghrelin was considered inactive at first, though biological activities such as stimulation of adipogenesis and control of cell growth could be demonstrated more recently. Both ghrelin and the more abundant endogenous form des-octanoyl ghrelin could play a role in the paracrine regulation of vascular tone in humans.

Substrate for dipeptidyl aminopeptidase I (cathepsin C).

C-Peptide 2 (rat) was shown to be effective in augmenting glucose utilization in streptozotocin diabetic rats.

Substrate for porcine cathepsin A and acid carboxypeptidases from A. niger.and A. kawachii.

The oxytocin antagonist OVTA shows enhanced affinity for rat uterine oxytocin receptors after iodination.

N-terminal amino acid of expressed proteins. The formyl moiety is removed enzymatically.

Substrate for chymotrypsin and carboxypeptidase Y.

Specific inhibitor of thimet oligopeptidase (soluble metalloendopeptidase, EC 3.4.24.15) (Ki = 0.027 ± 0.003 µM). Neprilysin (Endopeptidase-2, EC 3.4.24.11) converts Cpp-AAF-pAb into a potent inhibitor of angiotensin-converting enzyme (ACE).

<p>Bachem ID: 4068086.</p>

AC187 is a potent and selective antagonist of amylin-induced hyperglycaemia and hyperlactaemia. It has been used to demonstrate that amylin receptors mediate the anorectic action of salmon calcitonin.

<p>Bachem ID: 4003763.</p>

Ghrelin, a peptide hormone produced by the stomach oxyntic cells plays a crucial role in appetite regulation. It binds to the growth hormone secretagogue receptor (GHS-R), which stimulates the release of GH. Ghrelin, which promotes food uptake and body weight increase, acts as an antagonist of leptin. Thus, it has become an important tool in obesity research. Additionally, ghrelin is involved in the bone metabolism, in reproduction, and in the immune system.

GRF antagonist.

The chromogenic substrate Z-GGL-pNA is used alone or in combination with other substrates as Suc-LLVY-AMC for measuring the chymotrypsin-like activity of the proteasome. Z-GGL-pNA is also cleaved by proteinase yscE (kexin), subtilisins, and neutral endopeptidase 24.5.

GLP-2 administration to mice or rats promotes stimulation of crypt cell proliferation and inhibition of enterocyte apoptosis resulting in hyperplasia of the small bowel villous epithelium. It also exerts trophic effects in animal models of both small and large bowel injury such as experimental small bowel resection or chemically induced colitis. In addition to stimulation of epithelial proliferation, GLP-2 also acutely regulates gastric emptying and exerts rapid metabolic effects promoting stimulation of intestinal hexose transport. The actions of GLP-2 are transduced via the GLP-2 receptor, a member of the glucagon-secretin G protein-coupled receptor superfamily.

Z-VEID-AFC, fluorogenic substrate for caspase-6 (Mch2).

Cyclo(His-Pro), a diketopiperazine showing various biological effects in the CNS, as well as endocrine effects, has been isolated from several mammalian tissues. In some cases, it has been identified as a degradation product of thyrotropin-releasing hormone (TRH). In the presence of zinc ions, cyclo(His-Pro) showed hypoglycemic effects and induced body weight reduction in rats.

Desmopressin (DDAVP), as the first vasopressin analog with a very high and very specific antidiuretic effect, has been widely used for different therapeutic purposes. DDAVP also improves human learning and memory processes. CAS Number (desmopressin acetate): 62288-83-9.

<p>Bachem ID: 4096175.</p>

Deltorphin B, a selective δ-opioid receptor agonist isolated from the skin of Phyllomedusa bicolor.

Tertiapin (TPN), a potent inhibitor of the inward-rectifier K⁺ channels, blocked a G-protein-gated channel (GIRK1/4) and the ROMK1 channel with nanomolar affinities, however a closely related channel, IRK1, was insensitive to tertiapin. Thus, tertiapin will be a powerful ligand for purifying functional channels as well as for screening pharmaceutical agents against these channels.

Potential impurity of exenatide.

The prolyl oligopeptidase (POP) substrate Z-AP-pNA was used in combination with Z-GP-pNA and Z-AA-pNA for characterizing the prolyl oligopeptide of of the hyperthermophile Pyrococcus furiosus.

Muramyl dipeptide (MDP) inhibits HIV replication in CD4⁺ H9 lymphocytes..

<p>Bachem ID: 4030533.</p>

<p>Bachem ID: 4095874.</p>

<p>Bachem ID: 4012616.</p>

OXA 16-33 lacks the disulfide bridges of orexin A, but retains a part of the activity of full-length OXA/OXB. The peptide has been used in place of the intact neuropeptide.

Caloxin 2A1 is a selective extracellular inhibitor of the plasma membrane Ca²⁺-pump.

AFP-pNA, substrate for prolyl tripeptidyl aminopeptidases from the periodontal pathogens Porphyromonas gingivalis and Prevotella nigrescens.

<p>Bachem ID: 4029233.</p>

Substrate for human plasma carboxypeptidase N and membrane-bound carboxypeptidase D.

Tetraproline. PPPP was used as an internal standard in the quantitative determination of the antihypertensive (ACE-inhibiting) peptides IPP and VPP in cheese by HPLC-MS³.

Active molecules as peptides can be readily conjugated to this cell-permeable peptide by the mercapto moiety.

<p>Bachem ID: 4003545.</p>

The pentapeptide TRSAW, a highly conserved sequence within the pTH-related protein, is a potent inhibitor of osteoclastic bone resorption in vitro (EC₅₀ = 10⁻¹⁵ M).

<p>Bachem ID: 4014443.</p>

A hypothalamic neuropeptide which stimulates the release of LH and FSH. CAS Number (gonadorelin acetate): 34973-08-5.

Exendin-4 (exenatide), originally isolated from Heloderma suspectum venom, differs from exendin-3 by only 2 N-terminal amino acid substitutions. This polypeptide causes an increase in acinar cAMP without stimulating amylase release. Exendin-4 and glucagon-like peptide 1 (7-36) amide bind with similar affinity to the glucagon-like peptide 1 receptor. Moreover, exendin-4 is also considered for clinical use in the treatment of type 2 diabetes.

This peptide is the pp60 c-src carboxy-terminal phosphoregulatory peptide phosphorylated at Tyr⁵²⁷. The peptide fragment is involved in the regulation of kinase activity by binding intramolecularly or intermolecularly to the SH2 domain of the pp60 c-src protein.

The histone fragment was used as substrate for the protein arginine methyltransferase PRMT4.