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Submit ReviewAstressin is a 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.
Sold with the permission of the SALK Institute
分子量 | 3563.2 |
公式 | C161H269N49O42 |
序列 |
FHLLREVLEXARAEQLAQEAHKNRKLXEII (Modifications: Phe-1 = D-Phe, X-10 = X-27 = Nle, Glu-19 = γ-Glu, Lys-22 = ε-Lys, Cyclized: Glu-19 - Lys-22, Ile-30 = C-terminal amide) |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
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 |
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 1 mg/ml in 10% Acetic acid / water |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for Astressin, please let us know.
关键词: Astressin, Astressin supplier, Potent, CRF, receptor, antagonists, Corticotropin-Releasing, Factor, Non-Selective, Receptors, [D-Phe12,, Nle21,38,, Glu30,, Lys33]-CRF, (12-41), Non-selective, 1606, Tocris Bioscience
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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.