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Submit ReviewTCS OX2 29
说明： Potent and selective OX2 antagonist
化学名： (2S)-1-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanone hydrochloride
纯度： ≥98% (HPLC)
生物活性 for TCS OX2 29
TCS OX2 29 is a potent and selective OX2 receptor antagonist (IC50 = 40 nM). Displays >250-fold selectivity for OX2 over OX1 and a range of receptors, ion channels and transporters. Inhibits orexin A induced IP3 accumulation and ERK1/2 phosphorylation in CHO cells transfected with the OX2 receptor.
化合物库 for TCS OX2 29
TCS OX2 29 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for TCS OX2 29
| 分子量 | 433.97 |
| 公式 | C23H31N3O3.HCl |
| 储存 | Desiccate at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1610882-30-8 |
| PubChem ID | 53302033 |
| InChI Key | NHKNHFJTMINMBP-ZMBIFBSDSA-N |
| Smiles | C[C@@](C)(C)[C@H](NCC3=CC=NC=C3)C(N(C2)CCC1=C2C=C(OC)C(OC)=C1)=O.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.
溶解性数据 for TCS OX2 29
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 43.4 | 100 | |
| DMSO | 10.85 | 25 |
制备储备液 for TCS OX2 29
以下数据基于产品分子量 433.97。 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 | 2.3 mL | 11.52 mL | 23.04 mL |
| 5 mM | 0.46 mL | 2.3 mL | 4.61 mL |
| 10 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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产品说明书 for TCS OX2 29
参考文献 for TCS OX2 29
参考文献是支持产品生物活性的出版物。
Hirose et al (2003) N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: The first orexin-2 receptor selective non-peptidic antagonist. Bioorg.Med.Chem.Lett. 13 4497 PMID: 14643355
Mould et al (2014) Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands. Br.J.Pharmacol. 171 351 PMID: 23692283
If you know of a relevant reference for TCS OX2 29, please let us know.
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关键词: TCS OX2 29, TCS OX2 29 supplier, Potent, selective, OX2, antagonists, Orexin2, Receptors, TCSOX229, Receptor, 3371, Tocris Bioscience
9 篇 TCS OX2 29 的引用文献
引用文献是使用了 Tocris 产品的出版物。 TCS OX2 29 的部分引用包括：
Zhou et al (2015) Upregulation of orexin receptor in paraventricular nucleus promotes sympathetic outflow in obese Zucker rats. Neuropharmacology 99 481 PMID: 26277341
Plaza-Zabala et al (2013) A role for hypocretin/orexin receptor-1 in cue-induced reinstatement of nicotine-seeking behavior. J Mol Neurosci 38 1724 PMID: 23518606
Bian et al (2021) Orexin-B exerts excitatory effects on nigral dopaminergic neurons and alleviates motor disorders in MPTP parkinsonian mice Neurosci Lett 765 136291 PMID: 34666119
Beig et al (2015) Both Ox1R and Ox2R orexin receptors contribute to the cardiorespiratory response evoked from the perifornical hypothalamus. Clin.Exp.Pharmacol.Physiol. 42 1059 PMID: 26174505
Brown et al (2013) Central orexin (hypocretin) 2 receptor antagonism reduces ethanol self-administration, but not cue-conditioned ethanol-seeking, in ethanol-preferring rats. Int.J.Neuropsychopharmacol. 16 2067 PMID: 23601187
Huang et al (2010) Orexins depolarize rostral ventrolateral medulla neurons and increase arterial pressure and heart rate in rats mainly via orexin 2 receptors. J Pharmacol Exp Ther 334 522 PMID: 20494957
Asadi (2018) The effect of intracerebroventricular administration of orexin receptor type 2 antagonist on pentylenetetrazol-induced kindled seizures and anxiety in rats. BMC Neurosci 19 49 PMID: 30103703
Urbańska et al (2012) Orexins/hypocretins acting at Gi protein-coupled OX 2 receptors inhibit cyclic AMP synthesis in the primary neuronal cultures. PLoS One 46 42561 PMID: 21547533
Shu et al (2014) Orexin-A promotes cell migration in cultured rat astrocytes via Ca2+-dependent PKCα and ERK1/2 signals. PLoS One 9 e95259 PMID: 24748172
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