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说明： Potent, selective and competitive CRF2 antagonist
别名： [D-Phe11,His12]-Sauvagine (11-40)
生物活性 for Antisauvagine-30
Antisauvagine-30 is a potent, selective and competitive corticotropin-releasing factor CRF2 receptor antagonist (Kd values are 1.4 and 153.6 nM for binding to mouse CRF2β and rat CRF1 receptors respectively). Inhibits sauvagine-stimulated cAMP accumulation in HEK-mCRF2β cells (pA2 = 8.49). Prevents stress-enhanced fear conditioning and MEK 1/2-dependent activation of ERK1/2 in mice in vivo.
许可信息
Sold with the permission of the Max Planck Institute
技术数据 for Antisauvagine-30
| 分子量 | 3650.29 |
| 公式 | C161H274N48O46S |
| 序列 |
FHLLRKMIEIEKQEKEKQQAANNRLLLDTI (Modifications: Phe-1 = D-Phe, Ile-30 = C-terminal amide) |
| 储存 | Desiccate at -20°C |
| CAS Number | 220673-95-0 |
| PubChem ID | 16138449 |
| InChI Key | INBLUEDNNZCTNZ-JBNJRNGTSA-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](CCSC)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。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for Antisauvagine-30
参考文献 for Antisauvagine-30
参考文献是支持产品生物活性的出版物。
Brauns et al (2001) Pharmacological and chemical properties of astressin, antisauvagine-30 and α-helCRF: significance for behavioral experiments. Neuropharmacology 41 507 PMID: 11543771
Sananbenesi et al (2003) Mitogen-activated protein kinase signaling in the hippocampus and its modulation by corticotropin-releasing factor receptor 2: a possible link between stress and fear memory. J.Neurosci. 23 11436 PMID: 14673008
Ruhmann et al (1998) Structural requirements for peptidic antagonists of the corticotropin-releasing factor receptor (CRFR): development of CRFR2β-selective antisauvagine-30. Proc.Natl.Acad.Sci.USA 95 15264
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关键词: Antisauvagine-30, Antisauvagine-30 supplier, Potent, selective, competitive, CRF2, antagonists, Corticotropin-Releasing, Factor2, Receptors, [D-Phe11,His12]-Sauvagine, (11-40), 2071, Tocris Bioscience
2 篇 Antisauvagine-30 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Antisauvagine-30 的部分引用包括：
Zhao-Shea et al (2015) Increased CRF signalling in a ventral tegmental area-interpeduncular nucleus-medial habenula circuit induces anxiety during nicotine withdrawal. Front Cell Neurosci 6 6770 PMID: 25898242
Narla et al (2015) Suppression of piriform cortex activity in rat by corticotropin-releasing factor 1 and serotonin 2A/C receptors. Hum Mol Genet 9 200 PMID: 26074770
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Depression Poster
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.