Biological Activity
Potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist (IC50 values are 1.3 and > 500 nM for CRF2 and CRF1 respectively). Antagonizes CRF2-mediated inhibition of gastric emptying.
Technical Data
| M. Wt | 4041.69 |
| Formula | C183H307N49O53 |
| Sequence |
DLSFHLLRKXIEIEKQEKEKQQAENNKLLLDLI (Modifications: Asp-1 = N-terminal Ac, Phe-4 = D-Phe, Leu-6 = α-methyl-Leu, X = Nle, Glu-24 = γ-Glu, Lys-27 = ε-Lys, Leu-32 = α-methyl-Leu, Lactam Bridge = Glu-24 - Lys-27) |
| Storage | Store at -20°C |
| CAS Number | 681260-70-8 |
| PubChem ID | 90488758 |
| InChI Key | IVIBPRHVUKMKSX-YJHXGIRISA-N |
| Smiles | CCCC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@](C)(CC(C)C)NC(=O)[C@H](CC1=CNC=N1)NC(=O)[C@@H](CC1=CC=CC=C1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(C)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H]1CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@](C)(CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(N)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 1 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 4041.69. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.25 mL | 1.24 mL | 2.47 mL |
| 5 mM | 0.05 mL | 0.25 mL | 0.49 mL |
| 10 mM | 0.02 mL | 0.12 mL | 0.25 mL |
| 50 mM | 0 mL | 0.02 mL | 0.05 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Rivier et al (2002) Potent and long-acting corticotropin releasing factor (CRF) receptor 2 selective peptide competitive antagonists. J.Med.Chem. 45 4737 PMID: 12361401
Hoare et al (2005) Peptide ligand binding properties of the corticotropin-releasing factor (CRF) type 2 receptor: pharmacology of endogenously expressed receptors, G-protein-coupled sensitivity and determinants of CRF2 receptor selectivity. Peptides 26 457 PMID: 15652653
Henry et al (2006) The effect of lateral septum corticotropin-releasing factor receptor 2 activation on anxiety is modulated by stress. J.Neurosci. 26 9142 PMID: 16957071
Keywords: Astressin 2B, supplier, Selective, CRF2, antagonists, Corticotropin-Releasing, Factor2, Receptors, Astressin2B, CRF2, Receptors, CRF2, Receptors, Tocris Bioscience
