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 |
Molarity Calculator
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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
Tocris Bioscience是一家专卖生命科学研究chemicals, peptides and antibodies的知名品牌，其产品也广为各大药厂、大学、研究机构，超过五万名科学研究者所采用。 目前，產品內容已超過一千六百種以上，並每年持續不斷的增加新的產品。目前，产品内容已超过一千六百种以上，并每年持续不断的增加新的产品。
Tocris bioscience是位于英国布里斯托尔（Bristol）的高品质试剂提供商，共有2000多种产品，主要集中在神经科学和信号传导领域，产品类型包括小分子、多肽、抗体、配体和化合物筛选文库等，主要产品包括GPCR ligands，神经传递素，离子通道调控剂，信号通路抑制剂等，这些产品被广泛选择性地用于阻断或激活生物学通路。Tocris是世界上神经科学研究领域无可争议的领导者，其生产的影响神经系统的化学物质被多次引用，这些物质很多都来自Jeff Watkins（Tocris 的创立人）在Bristol大学原创性的研究工作。
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