Biological Activity
Potent and highly selective CRF2 receptor antagonist (Ki values are 0.66, 0.62 and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively). Inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. In rats in vivo, blocks urocortin-induced hypotension following systemic administration.
Licensing Information
Sold with the permission of the Max Planck Institute
Technical Data
| M. Wt | 3632.26 |
| Formula | C162H276N48O46 |
| Sequence |
FHLLRKXIEIEKQEKEKQQAANNRLLLDTI (Modifications: Phe-1 = D-Phe, X = Nle, Ile-30 = C-terminal amide) |
| Storage | Desiccate at -20°C |
| CAS Number | 434938-41-7 |
| PubChem ID | 90488734 |
| InChI Key | QJWWADQIQXXJQA-DCUOZLBZSA-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](CCCCN)C(=O)N[C@@H](CCCC)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](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)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@@H]([C@@H](C)O)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 5 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 3632.26. 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 | 1.38 mL | 2.75 mL |
| 5 mM | 0.06 mL | 0.28 mL | 0.55 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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Product Datasheets
References
References are publications that support the products' biological activity.
Ruhmann et al (2002) Design, synthesis and pharmacological characterization of new highly selective CRF2 antagonists: development of 123I-K31440 as a potential SPECT ligand. Peptides 23 453 PMID: 11835994
Lawrence et al (2002) The highly selective CRF2 receptor antagonist K41498 binds to presynaptic CRF2 receptors in rat brain. Br.J.Pharmacol. 136 896 PMID: 12110614
Keywords: K 41498, supplier, selective, potent, CRF2, antagonists, Corticotropin-Releasing, Factor2, Receptors, K41498, CRF2, Receptors, CRF2, Receptors, Tocris Bioscience
