Biological Activity
Potent corticotropin-releasing factor (CRF) receptor antagonist (Ki values are 2, 1.5 and 1 nM at CRF1, CRF2α and CRF2β). Reduces ACTH secretion, blocks delayed gastric emptying and is neuroprotective in vivo.
Licensing Information
Sold with the permission of the SALK Institute
Technical Data
| M. Wt | 3563.2 |
| Formula | C161H269N49O42 |
| Sequence |
FHLLREVLEXARAEQLAQEAHKNRKLXEII (Modifications: Phe-1 = D-Phe, X = Nle, Glu-19 = γ-Glu, Lys-22 = ε-Lys, Cyclized = Glu-19 -Lys-22, Ile-31 = C-terminal amide) |
| Storage | Store at -20°C |
| CAS Number | 170809-51-5 |
| PubChem ID | 16133798 |
| InChI Key | HPYIIXJJVYSMCV-MGDXKYBTSA-N |
| Smiles | [H]N[C@H](CC1=CC=CC=C1)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC2=CNC=N2)NC(=O)[C@H](C)NC1=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)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 10% Acetic acid / water |
Preparing Stock Solutions
The following data is based on the product molecular weight 3563.2. 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 | 0.28 mL | 1.4 mL | 2.81 mL |
| 5 mM | 0.06 mL | 0.28 mL | 0.56 mL |
| 10 mM | 0.03 mL | 0.14 mL | 0.28 mL |
| 50 mM | 0.01 mL | 0.03 mL | 0.06 mL |
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References
References are publications that support the products' biological activity.
Gulyas et al (1995) Potent, structurally constrained agonists and competitive antagonists of corticotropin-releasing factor. Proc.Natl.Acad.Sci.U.S.A. 92 10575 PMID: 7479843
Maecker et al (1997) Astressin, a novel and potent CRF antagonist, is neuroprotective in the hippocampus when administered after a seizure. Brain Res. 744 166 PMID: 9030428
Martinez et al (1999) Peripheral injection of a new corticotropin-releasing factor (CRF) antagonist, astressin, blocks peripheral CRF- and abdominal surgery-induced delayed gastric emptying in rats. J.Pharmacol.Exp.Ther. 290 629 PMID: 10411571
Perrin and Vale (1999) Corticotropin releasing factor receptors and their ligand family. Ann.N.Y.Acad.Sci. 885 312 PMID: 10816663
Keywords: Astressin, supplier, Potent, CRF, receptor, antagonists, Corticotropin-Releasing, Factor, Non-Selective, Receptors, [D-Phe12,, Nle21,38,, Glu30,, Lys33]-CRF, (12-41), Non-selective, CRF, Non-selective, CRF, Tocris Bioscience
