681260-70-8
Chemical Structure
Astressin 2B
- CAS No.: 681260-70-8
- Formula:C183H307N49O53
- Molecular Weight:4041.69
SMILES: O=C(C)N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](C(N[C@H](C(NC(C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NC(C)(C(N[C@H](C(N)=O)[C@H](CC)C)=O)CC(C)C)=O)CC(O)=O)=O)CC(C)C)=O)CC(C)C)=O)CC(C)C)=O)CCCCN1)=O)CC(N)=O)=O)CC(N)=O)=O)CCC1=O)=O)C)=O)CCC(N)=O)=O)CCC(N)=O)=O)CCCCN)=O)CCC(O)=O)=O)CCCCN)=O)CCC(O)=O)=O)CCC(N)=O)=O)CCCCN)=O)CCC(O)=O)=O)[C@H](CC)C)=O)CCC(O)=O)=O)[C@H](CC)C)=O)CCCC)=O)CCCCN)=O)CCCNC(N)=N)=O)CC(C)C)=O)(C)CC(C)C)=O)CC2=CNC=N2)=O)CC3=CC=CC=C3)=O)CO)=O)CC(C)C)=O)CC(O)=O
Biological Activity:
Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2[1][2][3][4][5][6][7].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
Astressin 2B | 97.81% | Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2. |
||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
- [1]. Rivier J, et al. Potent and long-acting corticotropin releasing factor (CRF) receptor 2 selective peptide competitive antagonists. J Med Chem. 2002;45(21):4737-4747. [Content Brief]
- [2]. Hoare SR, et al. Peptide ligand binding properties of the corticotropin-releasing factor (CRF) type 2 receptor: pharmacology of endogenously expressed receptors, G-protein-coupling sensitivity and determinants of CRF2 receptor selectivity. Peptides. 2005;26(3):457-470. [Content Brief]
- [3]. Henry B, et al. The effect of lateral septum corticotropin-releasing factor receptor 2 activation on anxiety is modulated by stress. J Neurosci. 2006;26(36):9142-9152. [Content Brief]
- [4]. Kubo Y, et al. Urocortin prevents indomethacin-induced small intestinal lesions in rats through activation of CRF2 receptors. Dig Dis Sci. 2010;55(6):1570-1580. [Content Brief]
- [5]. Moffatt J D, et al. Activation of corticotropin‐releasing factor receptor‐2 causes bronchorelaxation and inhibits pulmonary inflammation in mice[J]. The FASEB journal, 2006, 20(11): 1877-1879.
- [6]. Kokkotou E, et al. Corticotropin-releasing hormone receptor 2-deficient mice have reduced intestinal inflammatory responses[J]. The Journal of Immunology, 2006, 177(5): 3355-3361.
Keywords
