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Submit ReviewCP 376395 hydrochloride is a potent and selective CRF1 receptor antagonist (Ki values are 12 and >10000 nM for CRF1 and CRF2 receptors respectively). Binds at an allosteric site. Attenuates CRF-induced activation of the HPA axis in vivo following i.v. administration. Orally active.
CP 376395 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 362.94 |
公式 | C21H30N2O.HCl |
储存 | Desiccate at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 1013933-37-3 |
PubChem ID | 24806455 |
InChI Key | UDIOZDHQQNYISB-UHFFFAOYSA-N |
Smiles | CC1=CC(NC(CC)CC)=C(C)C(OC2=C(C)C=C(C)C=C2C)=N1.Cl |
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 | |||
water | 18.15 | 50 | |
DMSO | 36.29 | 100 |
以下数据基于产品分子量 362.94。 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 | 2.76 mL | 13.78 mL | 27.55 mL |
5 mM | 0.55 mL | 2.76 mL | 5.51 mL |
10 mM | 0.28 mL | 1.38 mL | 2.76 mL |
50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
参考文献是支持产品生物活性的出版物。
Chen et al (2008) 2-Aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists. J.Med.Chem. 51 1385 PMID: 18288792
Hollenstein et al (2013) Structure of class B GPCR corticotropin-releasing factor receptor 1. Nature 499 438 PMID: 23863939
Lu et al (2019) Small molecule allosteric modulators of G-protein-coupled receptors: drug-target interactions. J.Med.Chem. 62 24 PMID: 29457894
If you know of a relevant reference for CP 376395 hydrochloride, please let us know.
关键词: CP 376395 hydrochloride, CP 376395 hydrochloride supplier, Potent, selective, CRF1, antagonists, Corticotropin-Releasing, Factor1, Receptors, CP376395, hydrochloride, negative, allosteric, modulator, NAM, 3212, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 CP 376395 hydrochloride 的部分引用包括:
Tran et al (2014) Importance of CRF receptor-mediated mechanisms of the bed nucleus of the stria terminalis in the processing of anxiety and pain. Neuropsychopharmacology 39 2633 PMID: 24853772
Kean et al (2015) Conformational thermostabilisation of cortico. releasing factor receptor 1. Mol Pain 5 11954 PMID: 26159865
Boyson et al (2014) Social stress and CRF-DA interactions in the VTA: role in long-term escalation of cocaine self-administration. J Neurosci 34 6659 PMID: 24806691
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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.