Astressin 2B (TFA)

Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B TFA antagonizes CRF2-mediated inhibition of gastric emptying[1][2][3].

Product Specifications

UNSPSC

12352209

Target

CFTR

Type

Peptides

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Others

Assay Protocol

https://www.medchemexpress.com/astressin-2b-tfa.html

Purity

99.54

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C([C@H](CCCCNC1=O)NC([C@H](CCC(N[C@H](C(N[C@H]1CC(N)=O)=O)CC(N)=O)=O)NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@](C)(NC([C@@H](NC([C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(C)=O)CC(O)=O)=O)CC(C)C)=O)CO)=O)CC2=CC=CC=C2)=O)CC3=CNC=N3)=O)CC(C)C)=O)CC(C)C)=O)CCCNC(N)=N)=O)CCCCN)=O)CCCC)=O)[C@H](CC)C)=O)CCC(O)=O)=O)[C@H](CC)C)=O)CCC(O)=O)=O)CCCCN)=O)CCC(N)=O)=O)CCC(O)=O)=O)CCCCN)=O)CCC(O)=O)=O)CCCCN)=O)CCC(N)=O)=O)CCC(N)=O)=O)C)=O)=O)N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@](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.OC(C(F)(F)F)=O.[x]

Molecular Formula

C183H307N49O53.xC2HF3O2

Molecular Weight

4041.69 (free base)

References & Citations

[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.|[2]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.|[3]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.