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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
分子量 | 3632.26 |
公式 | C162H276N48O46 |
序列 |
FHLLRKXIEIEKQEKEKQQAANNRLLLDTI (Modifications: Phe-1 = D-Phe, X = Nle, Ile-30 = C-terminal amide) |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
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溶解性 | Soluble to 5 mg/ml in water |
参考文献是支持产品生物活性的出版物。
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.
关键词: K 41498, K 41498 supplier, selective, potent, CRF2, antagonists, Corticotropin-Releasing, Factor2, Receptors, K41498, 2070, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 K 41498 的部分引用包括:
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.