Pasireotide Diaspartate is a peptide analog containing multiple residues that influence helical stability and charged surface interactions. The diaspartate form enhances solubility and modulates electrostatic behavior. Researchers use it to examine ligand-receptor binding determinants and conformational shifts. Its stability supports advanced biophysical and structural analyses.
CAT No: R2221
CAS No:820232-50-6
Synonyms/Alias:Pasireotide diaspartate;Signifor;UNII-I4P76SY3N4;I4P76SY3N4;Pasireotide diaspartate [EMA EPAR];Pasireotide (as diaspartate);820232-50-6;Pasireotide (diaspartate);Cyclo((2R)-2-phenylglycyl-d-tryptophyl-l-lysyl-o-(phenylmethyl)-l-tyrosyl-l-phenylalanyl-(4R)-4-((((2-aminoethyl)amino)carbonyl)oxy)-l-prolyl), l-aspartate (1:2);(2S)-2-aminobutanedioic acid;[(3S,6S,9S,12R,15S,18S,20R)-9-(4-aminobutyl)-3-benzyl-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-15-phenyl-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-(2-aminoethyl)carbamate;DTXSID40231533;pasireotide aspartate;Pasireotide (aspartate);CHEMBL5314380;CHEBI:72313;DTXCID70154024;HY-16381B;PASIREOTIDE DIASPARTATE [WHO-DD];CS-0082821;PASIREOTIDE DIASPARTATE [ORANGE BOOK];Q21547171;cyclo[(2S)-2-phenylglycyl-D-tryptophyl-6-azaniumyl-L-norleucyl-O-benzyl-L-tyrosyl-L-phenylalanyl-(4R)-4-{[(2-ammonioethyl)carbamoyl]oxy}-L-prolyl] bis[(2S)-2-azaniumylsuccinate];cyclo[(2S)-2-phenylglycyl-D-tryptophyl-L-lysyl-O-benzyl-L-tyrosyl-L-phenylalanyl-(4R)-4-{[(2-aminoethyl)carbamoyl]oxy}-L-prolyl] bis-(L-aspartate);
Pasireotide Diaspartate is a synthetic peptide analog structurally related to somatostatin, designed to exhibit enhanced receptor binding affinity and extended biological activity. As a member of the somatostatin analog family, it is distinguished by its ability to interact with multiple somatostatin receptor subtypes, particularly SSTR1, SSTR2, SSTR3, and SSTR5. This multifaceted receptor engagement underpins its significance in biochemical research, especially in studies focused on neuroendocrine regulation, peptide-receptor interactions, and cellular signaling pathways. Its aspartate salt form confers improved solubility and handling characteristics, making it a valuable tool for peptide-based investigations and experimental assay development.
Receptor Binding Studies: Pasireotide Diaspartate is widely utilized in receptor-ligand binding assays to investigate the pharmacological properties and selectivity profiles of somatostatin analogs. Its high affinity for several somatostatin receptor subtypes enables detailed characterization of receptor binding kinetics, competitive displacement, and receptor subtype discrimination. These studies are critical for elucidating the molecular mechanisms underlying somatostatin receptor modulation and for advancing the understanding of G-protein coupled receptor (GPCR) signaling in various cellular contexts.
Signal Transduction Research: The compound serves as a robust model for probing downstream signaling events following somatostatin receptor activation. By applying this peptide analog to cultured cells or tissue systems, researchers can dissect the effects on intracellular second messenger pathways, such as inhibition of adenylyl cyclase activity, modulation of cyclic AMP levels, and regulation of calcium flux. These investigations yield valuable insights into the broader physiological roles of somatostatin receptors and inform the development of targeted modulators for research purposes.
Peptide Structure-Activity Relationship (SAR) Analysis: Pasireotide Diaspartate is instrumental in structure-activity relationship studies aimed at optimizing peptide analogs for receptor specificity and functional potency. Its unique sequence and conformational stability provide a benchmark for comparing the biological activity of novel somatostatin analogs and for mapping critical residues involved in receptor recognition. Such SAR analyses support rational peptide design and facilitate the discovery of new analogs with tailored biological profiles for experimental applications.
Endocrine Pathway Modeling: In endocrine research, this peptide is employed to simulate somatostatin-mediated regulatory effects on hormone secretion in in vitro and ex vivo systems. Through controlled exposure, investigators can assess the compound's influence on the release of hormones such as growth hormone, insulin, and glucagon from relevant cell models. These studies contribute to a deeper understanding of endocrine feedback loops and the modulation of secretory pathways by somatostatin analogs.
Peptide Stability and Degradation Studies: The aspartate salt form of this analog offers a practical system for evaluating peptide stability, degradation kinetics, and protease susceptibility under various experimental conditions. Researchers utilize it to examine the impact of formulation variables, enzymatic environments, and storage parameters on peptide integrity. Such data are essential for optimizing peptide handling protocols, improving formulation strategies, and ensuring reproducibility in biochemical assays involving synthetic peptides.
1. The spatiotemporal control of signalling and trafficking of the GLP-1R
3. High fat diet and GLP-1 drugs induce pancreatic injury in mice
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