Pasireotide Diaspartate

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.

Designed for biological research and industrial applications, not intended for individual clinical or medical purposes.
Pasireotide Diaspartate(CAS 820232-50-6)

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);

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M.F/Formula
C66H80N12O17
M.W/Mr.
1313.4

Pasireotide Diaspartate is a synthetic cyclohexapeptide analog of somatostatin, designed to exhibit enhanced receptor binding affinities and prolonged biological activity compared to native somatostatin. Distinguished by its ability to target multiple somatostatin receptor subtypes, particularly SSTR1, SSTR2, SSTR3, and SSTR5, this compound offers a versatile platform for research applications that require precise modulation of endocrine and neuroendocrine signaling pathways. Its unique structure and pharmacological profile make Pasireotide Diaspartate an invaluable tool in the exploration of peptide-receptor interactions, signaling cascades, and regulatory feedback mechanisms in various biological systems. The compound's stability, solubility, and receptor selectivity have enabled researchers to probe complex physiological processes with a high degree of specificity and reproducibility, supporting advanced studies in cellular and molecular biology.

Endocrine Research: Pasireotide Diaspartate is widely utilized in the investigation of pituitary and hypothalamic hormone regulation, given its potent activity at multiple somatostatin receptor subtypes. By modulating the secretion of growth hormone, adrenocorticotropic hormone, and other pituitary-derived factors, the compound enables researchers to dissect feedback loops and regulatory networks that govern endocrine homeostasis. Its broad receptor affinity profile provides a means to differentiate the contributions of individual receptor subtypes to hormone synthesis, release, and downstream signaling events, thereby advancing the understanding of neuroendocrine integration and dysfunction.

Signal Transduction Studies: In cellular signaling research, Pasireotide Diaspartate serves as a valuable probe for delineating the molecular mechanisms underlying somatostatin receptor-mediated signal transduction. By selectively activating or inhibiting specific receptor isoforms, scientists can map the downstream pathways involved in cyclic AMP regulation, calcium flux, and kinase activation. These studies facilitate the identification of novel intracellular targets and feedback regulators, offering insights into the modulation of cellular proliferation, apoptosis, and metabolic processes in response to peptide hormones.

Cancer Biology: Research into neuroendocrine tumors and other malignancies has benefited from the application of Pasireotide Diaspartate, particularly in elucidating the role of somatostatin receptors in tumor growth and progression. The compound's ability to inhibit hormone secretion and cell proliferation through receptor-mediated mechanisms allows for the exploration of autocrine and paracrine signaling loops within tumor microenvironments. By leveraging its multi-receptor targeting properties, investigators can assess the differential effects of receptor subtype engagement on tumor cell behavior, angiogenesis, and metastatic potential.

Metabolic Regulation: Studies focusing on glucose metabolism and insulin signaling have employed Pasireotide Diaspartate to investigate the interplay between somatostatin analogs and pancreatic islet function. The compound's modulatory effects on insulin, glucagon, and other metabolic hormones provide a platform for dissecting the regulatory circuits that maintain glucose homeostasis. Through in vitro and in vivo models, researchers can explore the impact of somatostatin receptor modulation on beta-cell activity, insulin sensitivity, and metabolic adaptation under physiological and pathophysiological conditions.

Receptor Pharmacology: Pasireotide Diaspartate is instrumental in the characterization of somatostatin receptor pharmacology, including receptor binding kinetics, desensitization, and internalization. By employing radioligand binding assays, fluorescence-based imaging, and functional readouts, scientists can quantify receptor-ligand interactions and assess the dynamic regulation of receptor expression and signaling competence. These studies are critical for understanding the molecular determinants of receptor selectivity and efficacy, informing the design of next-generation peptide analogs with tailored pharmacological profiles.

Neurobiology: Within the field of neurobiology, Pasireotide Diaspartate has been applied to investigations of neurotransmitter release, synaptic plasticity, and neuroprotective signaling. Its capacity to modulate neuronal excitability and synaptic transmission through somatostatin receptor engagement supports research into the mechanisms underlying neural circuit modulation, neurodegeneration, and adaptive responses to injury. By integrating electrophysiological, biochemical, and imaging approaches, researchers are able to delineate the contributions of somatostatinergic signaling to central and peripheral nervous system function, providing a foundation for future studies in brain health and disease.

InChI
InChI=1S/C58H66N10O9.2C4H7NO4/c59-27-13-12-22-46-52(69)64-47(30-38-23-25-42(26-24-38)76-36-39-16-6-2-7-17-39)53(70)66-49(31-37-14-4-1-5-15-37)57(74)68-35-43(77-58(75)61-29-28-60)33-50(68)55(72)67-51(40-18-8-3-9-19-40)56(73)65-48(54(71)63-46)32-41-34-62-45-21-11-10-20-44(41)45;2*5-2(4(8)9)1-3(6)7/h1-11,14-21,23-26,34,43,46-51,62H,12-13,22,27-33,35-36,59-60H2,(H,61,75)(H,63,71)(H,64,69)(H,65,73)(H,66,70)(H,67,72);2*2H,1,5H2,(H,6,7)(H,8,9)/t43-,46+,47+,48-,49+,50+,51+;2*2-/m100/s1
InChI Key
NEEFMPSSNFRRNC-HQUONIRXSA-N

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