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Submit ReviewK 41498 is a 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.
Sold with the permission of the Max Planck Institute
M. Wt | 3632.26 |
Formula | C162H276N48O46 |
Sequence |
FHLLRKXIEIEKQEKEKQQAANNRLLLDTI (Modifications: Phe-1 = D-Phe, X = Nle, Ile-30 = C-terminal amide) |
Storage | Store at -20°C |
Purity | ≥95% (HPLC) |
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility | Soluble to 5 mg/ml in water |
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for K 41498, please let us know.
Keywords: K 41498, K 41498 supplier, selective, potent, CRF2, antagonists, Corticotropin-Releasing, Factor2, Receptors, K41498, 2070, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for K 41498 include:
Nakamura and Sapru (2009) Cardiovascular responses to microinjections of urocortins into the NTS: role of inotropic glutamate receptors. Am J Physiol Heart Circ Physiol 296 H2022 PMID: 19395554
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.