Amino Acid Derivatives

Suc-AAPR-pNA, a substrate for wild-type and K188D/D189K trypsins (Km = 32.8 mM respectively 50.8 mM).

<p>Bachem ID: 4039552.</p>

Amylin (20-29) (or hIAPP 20-29) forms fibrils that are ultrastructurally identical to amyloid fibrils seen in pancreatic islets. The region SNNFGAILSS appears to be the most important amyloidogenic sequence of hIAPP (human islet amyloid polypeptide).

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.

Glucagon antagonist.

Apelin-17 is an endogenous ligand of the human orphan G protein-coupled receptor APJ, reported to act as a coreceptor of CD4 for human and simian immunodeficiency viruses. Apelin-17 and apelin-13 represent the predominant molecular forms of apelin present in the whole brain, hypothalamus, and plasma. Like apelin-13, apelin-17 exhibited a high activity on extracellular acidification rate and strongly inhibited forskolin-stimulated cAMP production in CHO cells expressing the human or the rat apelin receptor. The peptide might play a crucial role in the maintenance of body fluid homeostasis by counteracting AVP (arginine vasopressin) actions through inhibition of AVP neuron activity and AVP release.

Fragment of human leptin, an adipose tissue-derived protein encoded by the obese gene. Leptin has been implicated in the control of food intake, energy expenditure and reproduction. Additional roles in the regulation of immunity, inflammation, and hematopoiesis have been proposed.

This fragment of myelin proteolipid protein is an encephalitogenic determinant, able to bind to diverse sets of T cell receptors.

Chicken GnRH I and its isoform GnRH II were detected in the chicken hypothalamus.

Highly potent synthetic mastoparan analog.

One of the most potent pentapeptides having the same qualitative effects as the parent hormone gastrin I. The effect of this cholecystokinin agonist has been studied in patients with generalized anxiety disorder. Pentagastrin is used as a diagnostic for the evaluation of gastric acid secretory function (pentagastrin test).

PEG acrylate-based hydrogels have been modified with the RGD peptide YRGDS to improve their biocompatibility. YRGDS can be radioiodinated.

The effect of IAPP (8-37) (mouse, rat), an amylin receptor antagonist, on the ANP release was attenuated in streptozotocin-treated rats.

α-Methyl-proline restores normal levels of bone collagen type I synthesis in ovariectomized rats, used as models for human postmenopausal osteoporosis.

GnRH analog used in aquaculture.

<p>Bachem ID: 4051740.</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.

Chromogenic substrate for gingipain K.

<p>Bachem ID: 4104812.</p>

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.

IAPP 1-13 does not form fibrils, the region could be involved in the binding of amylin to membranes.

A highly sensitive fluorogenic substrate for the assay of human neutrophil and porcine pancreatic elastases. MeOSuc-AAPV-AMC is also cleaved by myeloblastin.

Cell-permeable nonaarginine amide, which can be easily conjugated to a cargo molecule, e.g. by maleimide-thiol coupling.

Inhibitor of tryptophan 5-monooxygenase.

An insulinotropic peptide generated by proteolytic cleavage of its precursor GLP-1 (1-37) and secreted by L cells of the intestinal mucosa upon food ingestion.

Analog of salmon GnRH showing a very high affinity to GnRH receptors used in aquaculture. Usually applied in combination with a dopamine antagonist as domperidone or pimozide, sGnRHa induces ovulation and spawning in a large number of fish species.

FPA-pNA is cleaved by the sedolisins B, C, and D, tripeptidyl peptidases from Aspergillus fumigatus.

This synthetic oxytocin analog shows a prolonged effect due to an increased resistance to enzymatic cleavage. Carbetocin is highly effective in preventing post-partum hemorrhage after vaginal delivery.

Neuropeptide NPVF (VPNLPQRF-amide) is an endogenous anti-opioid peptide.

Impurity of atosiban.

<p>Bachem ID: 4050435.</p>

Z-GP-AMC, fluorogenic substrate for the determination of post-proline cleaving enzyme (prolyl endopeptidase).

YGRKKRRQRRR, a cell-permeable peptide (CPP) derived from the HIV-1 tat protein transduction domain (PTD), has been shown to promote the entry of nucleic acids into several cell types.

Substrate for aminopeptidase M, also used in histochemistry.

<p>Bachem ID: 4003323.</p>

[1499-46-3] (net).

The pyroglutamyl form of apelin-13 exhibited a high activity with an EC₅₀ value of 0.30 nM. pERPRLSHKGPMPF is probably the final product of the post-translational modification of apelin and the biologically active endogenous ligand. (Pyr¹)-Apelin-13 has been identified as the predominant apelin isoform in the human heart. Pyr-Apelin-13 stimulates glucose utilization in normal and obese insulin-resistant mice. It could be required for the maintenance of insulin sensitivity.

Building block for the synthesis of aspartame analogs. CAS-Number (net): 40056-18-6.

V.Paspaliaris et al. showed that daily administration of pTHrP (1-34) to rats was anabolic on bone by increasing bone formation. This treatment could inhibit the rapid decline in bone formation due to denervation.

<p>Bachem ID: 4012248.</p>

<p>Bachem ID: 4007899.</p>

Guanylin activates the guanylate cyclase in the intestine to stimulate the production of cGMP, which in turn causes a secretory diarrhoea. Therefore, this peptide may play a role in regulating fluid and electrolyte absorption in intestines.

IL-6 (88-121) competitively inhibits the binding of human IL-6 to its receptor by interacting with the IL-6 receptor to a significant degree. It is suggested that this peptide comprises a part of the receptor-binding region of IL-6.

This biotinylated ω-conotoxin GVIA is a useful ligand for the characterization of calcium channels.

Non-mammalian Arg-vasopressin/oxytocin analog.

<p>Bachem ID: 4030678.</p>

<p>Bachem ID: 4096190.</p>

Endogenous kappa-opioid receptor agonist. It is suggested that it attenuates galanin-induced impairment of memory processes through the mediation of kappa-opioid receptors.