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Submit ReviewPexacerfont is a potent and selective corticotropin-releasing factor 1 receptor (CRF1) antagonist (IC50 = 6.1 nM). Displays >150 fold selectivity for CRF1 over CRF2b. Inhibits CRF-mediated adrenocorticotropic hormone (ACTH) release from pituitary cell culture (IC50 = 129 nM). Displays anxiolytic effects in rat behavioral paradigms.
分子量 | 340.43 |
公式 | C18H24N6O |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 459856-18-9 |
PubChem ID | 9884366 |
InChI Key | LBWQSAZEYIZZCE-SNVBAGLBSA-N |
Smiles | CC[C@H](NC1=NC(C)=NC2=C(C3=C(N=C(C=C3)OC)C)C(C)=NN12)C |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 34.04 | 100 | |
ethanol | 34.04 | 100 |
以下数据基于产品分子量 340.43。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.94 mL | 14.69 mL | 29.37 mL |
5 mM | 0.59 mL | 2.94 mL | 5.87 mL |
10 mM | 0.29 mL | 1.47 mL | 2.94 mL |
50 mM | 0.06 mL | 0.29 mL | 0.59 mL |
参考文献是支持产品生物活性的出版物。
Gilligan et al (2009) Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists. J.Med.Chem. 52 3084 PMID: 19361209
If you know of a relevant reference for Pexacerfont, please let us know.
关键词: Pexacerfont, Pexacerfont supplier, BMS, 562086, BMS562086, corticotrophin, releasing, hormone, receptor, 1, antagonists, antagonism, CRF1, anxiolytic, Receptors, 6451, 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.