PACAP (6-38), human, ovine, rat is a potent PACAP receptor antagonist with IC50s of 30, 600, and 40 nM for PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2, respectively.
CAT No: R1593
CAS No:143748-18-9
Synonyms/Alias:PACAP 6-38;143748-18-9;CHEMBL525267;PACAP-38 (6-38) (human, chicken, mouse, ovine, porcine, rat) trifluoroacetate salt;AKOS024457498;NCGC00167165-01;DA-66445;FP108759;H-Phe-Thr-Asp-Ser-Tyr-Ser-Arg-Tyr-Arg-Lys-Gln-Met -Ala-Val-Lys-Lys-Tyr-Leu-Ala-Ala-Val-Leu-Gly-Lys-Arg-Tyr-Lys-Gln-Arg-Val-Lys-Asn-L ys-NH2; H-FTDSYSRYRKQMAVKKYLAAVLGKRYKQRVKNK-NH2;
PACAP (6-38), human, ovine, rat is a synthetic peptide fragment derived from the pituitary adenylate cyclase-activating polypeptide (PACAP) sequence, encompassing amino acids 6 through 38. As a well-characterized PACAP receptor antagonist, it plays a pivotal role in experimental neurobiology, endocrinology, and receptor pharmacology. Its utility stems from its high affinity for PAC1 receptors, where it effectively inhibits PACAP-mediated signaling. This selectivity and functional specificity make PACAP (6-38) a valuable molecular tool for dissecting the physiological and pathophysiological roles of PACAP and its receptors across multiple mammalian systems.
Receptor Antagonism Studies: PACAP (6-38) is widely employed in research focused on the functional analysis of PAC1 receptor-mediated signaling pathways. By competitively inhibiting endogenous PACAP binding, it enables precise delineation of PACAP's contribution to cyclic AMP production, intracellular calcium mobilization, and downstream transcriptional responses. This application is particularly crucial for studies aiming to unravel the mechanistic basis of neuropeptide action in neuronal and endocrine tissues, where PACAP signaling is implicated in diverse regulatory processes.
Neurophysiological Research: As a potent PAC1 antagonist, this peptide is instrumental in probing the neuromodulatory functions of PACAP in central and peripheral nervous system models. Researchers utilize it to investigate synaptic plasticity, neurotransmitter release, and neuronal excitability under both physiological and experimentally induced conditions. Its use facilitates the identification of PACAP-dependent pathways involved in neuroprotection, stress response, and neural circuit modulation, thereby advancing the understanding of complex neurobiological phenomena.
Endocrine Function Analysis: PACAP (6-38) serves as a critical tool in studies exploring the regulatory roles of PACAP in hormone secretion and endocrine feedback mechanisms. By blocking PACAP-induced signaling in pituitary, pancreatic, and adrenal models, it enables the assessment of receptor-specific contributions to hormone synthesis, release, and regulation. This is especially relevant for elucidating the interplay between neuropeptide signaling and metabolic or stress-related endocrine functions.
Signal Transduction Mapping: The peptide is frequently used in experiments designed to map intracellular signaling cascades downstream of PAC1 receptor activation. Its antagonistic properties allow for the selective inhibition of PACAP-triggered pathways, facilitating the identification of key molecular intermediates and regulatory nodes. Such studies are essential for constructing detailed models of G protein-coupled receptor (GPCR) signaling in both normal and pathological contexts.
Pharmacological Profiling: PACAP (6-38) is also valuable in pharmacological assays aimed at characterizing receptor subtype selectivity, ligand-receptor interactions, and structure-activity relationships within the PACAP family. By serving as a reference antagonist, it aids in the comparative evaluation of novel peptide analogs, small-molecule modulators, and engineered receptor variants. These investigations support drug discovery efforts and the development of selective modulators targeting PACAP-related pathways for research use.
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