Drug intelligence / Profile preview

astressin 2b

Development stage
Phase 1
Modality
Peptides
Administration
Intraperitoneal (preclinical), Subcutaneous (preclinical)
01

Overview

Astressin 2B is a potent and highly selective peptide antagonist of the corticotropin-releasing factor receptor 2 (CRF2). It exhibits an IC50 of approximately 1.3 nM for CRF2 and greater than 500 nM for CRF1, indicating strong selectivity for the CRF2 subtype[1][3][5][9]. By blocking CRF2 receptors, Astressin 2B antagonizes physiological processes mediated by this receptor—including inhibition of gastric emptying and modulation of stress responses. It has been widely used in preclinical research to dissect the role of CRF signaling in gastrointestinal function, inflammation models (such as colitis), anxiety-related behaviors, and vascular biology[6]. The compound is a synthetic cyclic peptide with several non-natural amino acid modifications to enhance stability and selectivity.

Other names
astressin 2-Bastressin2-Bastressin-2-Bcyclo(31-34)[DPhe(11),His(12),C(alpha)MeLeu(13,39),Nle(17),Glu(31),Lys(34)]Ac-sauvagine(8-40)
02

Targets

CRHR2 (Corticotropin-releasing hormone receptor 2)

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